1. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Autophagy
  2. PPAR Autophagy
  3. GW 501516

GW 501516  (Synonyms: GW 1516; GSK-516)

目录号: HY-10838 纯度: 99.43%
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GW 501516 (GW 1516) 是 PPARδ 的激动剂,EC50 值为 1.1 nM。

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GW 501516 Chemical Structure

GW 501516 Chemical Structure

CAS No. : 317318-70-0

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10 mM * 1 mL in DMSO ¥495
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1 mg ¥225
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5 mg ¥450
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10 mg ¥730
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Customer Review

Other Forms of GW 501516:

    GW 501516 purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Jun 28;9:648.  [Abstract]

    Western blot analysis of the protein expression of caspase and Bcl-2 family members in response to GW501516.

    查看 PPAR 亚型特异性产品:

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    GW 501516 (GW 1516) is a PPARδ agonist with an EC50 of 1.1 nM[1].

    IC50 & Target[1]

    PPARδ

    1.1 nM (EC50)

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    COS-1 EC50
    > 1000 nM
    Compound: 1, GW-501516
    Agonist activity at human PPARalpha ligand binding domain expressed in COS-1 cells co-transfected with Gal4 after 24 hrs by luciferase reporter gene assay
    Agonist activity at human PPARalpha ligand binding domain expressed in COS-1 cells co-transfected with Gal4 after 24 hrs by luciferase reporter gene assay
    [PMID: 22051054]
    COS-1 EC50
    0.5 nM
    Compound: 1, GW501516
    Agonist activity at pSG5-Gal4-tagged human PPAR-beta/delta ligand binding domain expressed in COS1 cells assessed as receptor activation incubated for 19 hrs by pGL3-5XUAS-SV40 luciferase reporter gene assay
    Agonist activity at pSG5-Gal4-tagged human PPAR-beta/delta ligand binding domain expressed in COS1 cells assessed as receptor activation incubated for 19 hrs by pGL3-5XUAS-SV40 luciferase reporter gene assay
    [PMID: 25768705]
    COS-1 EC50
    2.9 nM
    Compound: 1, GW-501516
    Agonist activity at human PPARdelta ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometric analysis
    Agonist activity at human PPARdelta ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometric analysis
    [PMID: 22051054]
    COS-1 EC50
    912 nM
    Compound: 1, GW-501516
    Agonist activity at human PPARgamma ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometric analysis
    Agonist activity at human PPARgamma ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometric analysis
    [PMID: 22051054]
    COS-7 EC50
    1 nM
    Compound: GW-501516
    Activity at PPARbeta/delta by luciferase reporter gene transactivation assay in COS7 cells
    Activity at PPARbeta/delta by luciferase reporter gene transactivation assay in COS7 cells
    [PMID: 16797985]
    COS-7 EC50
    10000 nM
    Compound: GW-501516
    Activity at PPARalpha by luciferase reporter gene transactivation assay in COS7 cells
    Activity at PPARalpha by luciferase reporter gene transactivation assay in COS7 cells
    [PMID: 16797985]
    COS-7 EC50
    10000 nM
    Compound: GW-501516
    Activity at PPARgamma by luciferase reporter gene transactivation assay in COS7 cells
    Activity at PPARgamma by luciferase reporter gene transactivation assay in COS7 cells
    [PMID: 16797985]
    CV-1 EC50
    > 1.2 μM
    Compound: GW501516
    Transactivation activity at human PPARgamma expressed in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay
    Transactivation activity at human PPARgamma expressed in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay
    [PMID: 22534184]
    CV-1 EC50
    0.001 μM
    Compound: 1, GW-501516
    Agonist potency at PPARdelta in CV1 cells by cell based transient transfection assay
    Agonist potency at PPARdelta in CV1 cells by cell based transient transfection assay
    [PMID: 17243659]
    CV-1 EC50
    0.0012 μM
    Compound: GW501516
    Transactivation of human PPARdelta expressed in african green monkey CV1 cells by luciferase reporter gene assay
    Transactivation of human PPARdelta expressed in african green monkey CV1 cells by luciferase reporter gene assay
    [PMID: 22579420]
    CV-1 EC50
    0.0017 μM
    Compound: 1, GW-501516
    Agonist activity at human PPARdelta-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay
    Agonist activity at human PPARdelta-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay
    [PMID: 21515063]
    CV-1 EC50
    0.0017 μM
    Compound: GW-501516
    Transactivation of Gal4-fused human PPARdelta DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay
    Transactivation of Gal4-fused human PPARdelta DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay
    [PMID: 21112784]
    CV-1 EC50
    0.99 μM
    Compound: 1, GW-501516
    Agonist activity at human PPARalpha-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay
    Agonist activity at human PPARalpha-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay
    [PMID: 21515063]
    CV-1 EC50
    0.99 μM
    Compound: GW-501516
    Transactivation of Gal4-fused human PPARalpha DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay
    Transactivation of Gal4-fused human PPARalpha DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay
    [PMID: 21112784]
    CV-1 EC50
    1.888 μM
    Compound: 1, GW-501516
    Agonist potency at PPARalpha in CV1 cells by cell based transient transfection assay
    Agonist potency at PPARalpha in CV1 cells by cell based transient transfection assay
    [PMID: 17243659]
    CV-1 EC50
    2.5 nM
    Compound: GW501516
    Transactivation activity at human PPARdelta expressed in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay
    Transactivation activity at human PPARdelta expressed in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay
    [PMID: 22534184]
    CV-1 EC50
    229 nM
    Compound: GW501516
    Transactivation activity at human PPARalpha expressed in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay
    Transactivation activity at human PPARalpha expressed in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay
    [PMID: 22534184]
    CV-1 EC50
    4.1 μM
    Compound: 1, GW-501516
    Agonist activity at human PPARgamma-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay
    Agonist activity at human PPARgamma-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay
    [PMID: 21515063]
    CV-1 EC50
    4.1 μM
    Compound: GW-501516
    Transactivation of Gal4-fused human PPARgamma DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay
    Transactivation of Gal4-fused human PPARgamma DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay
    [PMID: 21112784]
    CV-1 EC50
    8.9 μM
    Compound: 1, GW-501516
    Agonist potency at PPARgamma in CV1 cells by cell based transient transfection assay
    Agonist potency at PPARgamma in CV1 cells by cell based transient transfection assay
    [PMID: 17243659]
    HEK293 EC50
    > 10 μM
    Compound: GW-501516
    Activity at human adipose tissue PPAR gamma expressed in HEK293 cells by PPAR-GAL4 transactivation assay
    Activity at human adipose tissue PPAR gamma expressed in HEK293 cells by PPAR-GAL4 transactivation assay
    [PMID: 17343371]
    HEK293 EC50
    0.002 μM
    Compound: 1, GW-501516
    Agonist activity at Gal4-fused human PPARdelta DNA binding domain expressed in HEK293 cells by luciferase reporter gene assay
    Agonist activity at Gal4-fused human PPARdelta DNA binding domain expressed in HEK293 cells by luciferase reporter gene assay
    [PMID: 21094606]
    HEK293 EC50
    0.0044 μM
    Compound: GW501516
    Agonist activity at GAL4N fused human PPARdelta LBD expressed in HEK293 cells co-expressing TK-MH100x4-Luc after 24 hrs by luciferase reporter gene assay
    Agonist activity at GAL4N fused human PPARdelta LBD expressed in HEK293 cells co-expressing TK-MH100x4-Luc after 24 hrs by luciferase reporter gene assay
    [PMID: 28539218]
    HEK293 EC50
    0.0059 μM
    Compound: GW501516
    Agonist activity at N-terminal Gal4 fused human PPARdelta LBD transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay
    Agonist activity at N-terminal Gal4 fused human PPARdelta LBD transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay
    [PMID: 27622746]
    HEK293 EC50
    0.0059 μM
    Compound: GW501516
    Agonist activity at GAL4-tagged human PPARdelta ligand binding domain chimeric receptor expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay
    Agonist activity at GAL4-tagged human PPARdelta ligand binding domain chimeric receptor expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay
    [PMID: 27591006]
    HEK293 EC50
    0.0079 μM
    Compound: GW-501516
    Activity at human placenta PPAR delta expressed in HEK293 cells by PPAR-GAL4 transactivation assay
    Activity at human placenta PPAR delta expressed in HEK293 cells by PPAR-GAL4 transactivation assay
    [PMID: 17343371]
    HEK293 EC50
    0.054 μM
    Compound: GW-501516
    Agonist activity at mouse PPAR delta expressed in HEK293 cells by PPAR-GAL4 transactivation assay
    Agonist activity at mouse PPAR delta expressed in HEK293 cells by PPAR-GAL4 transactivation assay
    [PMID: 17343371]
    HEK293 EC50
    0.085 μM
    Compound: GW-501516
    Agonist activity at human PPARdelta receptor expressed in HEK293 cells by GAL4 transactivation assay
    Agonist activity at human PPARdelta receptor expressed in HEK293 cells by GAL4 transactivation assay
    [PMID: 17524643]
    HEK293 EC50
    0.18 nM
    Compound: GW501516
    Agonist activity at human PPARbeta expressed in HEK293 cells by luciferase reporter gene assay
    Agonist activity at human PPARbeta expressed in HEK293 cells by luciferase reporter gene assay
    [PMID: 25305688]
    HEK293 EC50
    3.9 μM
    Compound: GW-501516
    Activity at human liver PPAR alpha expressed in HEK293 cells by PPAR-GAL4 transactivation assay
    Activity at human liver PPAR alpha expressed in HEK293 cells by PPAR-GAL4 transactivation assay
    [PMID: 17343371]
    HeLa EC50
    > 10000 nM
    Compound: 27, GW-501516
    Agonist activity at PPARalpha ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay
    Agonist activity at PPARalpha ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay
    [PMID: 19275963]
    HeLa EC50
    > 10000 nM
    Compound: 27, GW-501516
    Agonist activity at PPARgamma ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay
    Agonist activity at PPARgamma ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay
    [PMID: 19275963]
    HeLa EC50
    8 nM
    Compound: 27, GW-501516
    Agonist activity at PPARdelta ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay
    Agonist activity at PPARdelta ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay
    [PMID: 19275963]
    HepG2 EC50
    0.0012 μM
    Compound: GW-501516
    Agonist activity at human PPARdelta expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay
    Agonist activity at human PPARdelta expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay
    [PMID: 21215640]
    HepG2 EC50
    0.8 μM
    Compound: GW-501516
    Agonist activity at human PPARgamma expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay
    Agonist activity at human PPARgamma expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay
    [PMID: 21215640]
    HepG2 EC50
    1.1 μM
    Compound: GW-501516
    Agonist activity at human PPARalpha expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay
    Agonist activity at human PPARalpha expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay
    [PMID: 21215640]
    HepG2 EC50
    4 nM
    Compound: GW-501516
    Agonist activity at human PPARdelta in HepG2 cells by GAL4-luciferase reporter gene assay
    Agonist activity at human PPARdelta in HepG2 cells by GAL4-luciferase reporter gene assay
    [PMID: 17512197]
    体外研究
    (In Vitro)

    GW 501516 is shown to be the most potent and selective PPARδ agonists known with an EC50 of 1.1 nM against PPARδ and 1000-fold selectivity over the other human subtypes, PPARα and-γ[1].
    GW 501516 exerts anti-inflammatory effects in mouse cultured proximal tubular (mProx) cells. GW 501516 inhibits palmitate- and TNFα-induced increases in MCP-1 mRNA expression in a dose-dependent manner[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    GW 501516 causes impaired bone formation, leading to decreased BMD and deterioration of bone properties in OVX rats[2].
    GW 501516 attenuates interstitial inflammation and proximal tubular cell damage in a protein-overload mouse nephropathy model[3].
    GW 501516 treatment enhances running endurance and the proportion of succinate dehydrogenase (SDH)-positive muscle fibres in both trained and untrained mice[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    分子量

    453.50

    Formula

    C21H18F3NO3S2

    CAS 号
    性状

    固体

    颜色

    White to off-white

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : ≥ 100 mg/mL (220.51 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.2051 mL 11.0254 mL 22.0507 mL
    5 mM 0.4410 mL 2.2051 mL 4.4101 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.51 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (5.51 mM); 悬浊液; 超声助溶

      此方案可获得 2.5 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.43%

    参考文献
    Cell Assay
    [3]

    GW 501516 is dissolved in DMSO. Cells are starved by incubation in 0.2% FCS DMEM for 9 h, then pre-incubated with GW 501516, at a final concentration of 2.5 and 5 µM, or 0.05% DMSO as control for 3 hours, followed by stimulation with 150 µM palmitate bound to 8.0% BSA for 12 h[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2][3]

    Rats: Female Sprague Dawley rats, 12 weeks of age, are allocated to a sham-operated group and 3 OVX groups; high-dose GW 501516 (OVX-GW5), low-dose GW 501516 (OVX-GW1), and a control group (OVX-CTR), respectively. Animals receive GW 501516 or vehicle (methylcellulose) daily for 4 months by gavage. Bone mineral density (BMD) is assessed by dual x-ray absorptiometry at the femur, spine, and whole body[2].

    Mice: Mice are randomly allocated to different groups and receive therapeutic diet and treatment. The GW 501516-containing rodent diet is made by evenly adding GW 501516 to the control diet to a final concentration of 0.04% w/w. In the control diet, 10% of the total calories are from fat (5.5% from soybean oil and 4.5% from lard)[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2051 mL 11.0254 mL 22.0507 mL 55.1268 mL
    5 mM 0.4410 mL 2.2051 mL 4.4101 mL 11.0254 mL
    10 mM 0.2205 mL 1.1025 mL 2.2051 mL 5.5127 mL
    15 mM 0.1470 mL 0.7350 mL 1.4700 mL 3.6751 mL
    20 mM 0.1103 mL 0.5513 mL 1.1025 mL 2.7563 mL
    25 mM 0.0882 mL 0.4410 mL 0.8820 mL 2.2051 mL
    30 mM 0.0735 mL 0.3675 mL 0.7350 mL 1.8376 mL
    40 mM 0.0551 mL 0.2756 mL 0.5513 mL 1.3782 mL
    50 mM 0.0441 mL 0.2205 mL 0.4410 mL 1.1025 mL
    60 mM 0.0368 mL 0.1838 mL 0.3675 mL 0.9188 mL
    80 mM 0.0276 mL 0.1378 mL 0.2756 mL 0.6891 mL
    100 mM 0.0221 mL 0.1103 mL 0.2205 mL 0.5513 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    产品名称:
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    目录号:
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