1. GPCR/G Protein Neuronal Signaling
  2. Melanocortin Receptor
  3. α-MSH

α-MSH  (Synonyms: α-Melanocyte-Stimulating Hormone)

目录号: HY-P0252 纯度: 99.57%
COA 产品使用指南

α-MSH (alpha-melanocyte-stimulating hormone) 作为内源性神经肽,是一种内源性 melanocortin receptor 4 (MC4R) 激动剂,具有抗炎、解热作用。α-MSH 是前阿皮黑素皮质激素 (POMC) 的翻译后衍生物。

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Custom Peptide Synthesis

α-MSH Chemical Structure

α-MSH Chemical Structure

CAS No. : 581-05-5

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Other Forms of α-MSH:

查看 Melanocortin Receptor 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

α-MSH (α-Melanocyte-Stimulating Hormone), an endogenous neuropeptide, is an endogenous melanocortin receptor 4 (MC4R) agonist with anti-inflammatory and antipyretic activities. α-MSH is a post-translational derivative of pro-opiomelanocortin (POMC)[1][2].

IC50 & Target

MC4R

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO EC50
0.0027 μM
Compound: alpha-MSH
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
Agonist activity at human recombinant MC3 receptor expressed in CHO cells assessed as cAMP accumulation by enzyme fragment complementation assay
[PMID: 20329799]
CHO EC50
1.1 nM
Compound: Alpha-MSH
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 3 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 3 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
[PMID: 15982875]
CHO EC50
1.9 nM
Compound: Alpha-MSH
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
[PMID: 15982875]
CHO IC50
118 nM
Compound: Alpha-MSH
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
[PMID: 15982875]
CHO EC50
17 nM
Compound: Alpha-MSH
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
Inhibition concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells)
[PMID: 15982875]
CHO IC50
19 nM
Compound: alpha-MSH
Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
Concentration for 50% inhibition of human melanocortin-4 receptor expressed in CHO cells using [125I]NDP-alpha-MSH as radioligand
[PMID: 15582434]
CHO IC50
19 nM
Compound: Alpha-MSH
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
[PMID: 15982875]
CHO IC50
19 nM
Compound: Alpha-MSH
Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells
[PMID: 15982875]
CHO EC50
2.2 nM
Compound: alpha-MSH
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
Agonist activity at human recombinant MC4 receptor expressed in CHO cells by cAMP responsive beta lactamase reporter gene assay
[PMID: 20329799]
HEK293 EC50
0.0009 μM
Compound: alpha-MSH
Agonist activity at human recombinant MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by enzyme fragment complementation assay
Agonist activity at human recombinant MC1 receptor expressed in HEK293 cells assessed as cAMP accumulation by enzyme fragment complementation assay
[PMID: 20329799]
HEK293 EC50
0.04 nM
Compound: alpha-MSH
Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP AlphaScreen assay
Agonist activity at mouse melanocortin receptor 1 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP AlphaScreen assay
[PMID: 32184956]
HEK293 EC50
0.14 nM
Compound: alpha-MSH
Agonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
Agonist activity at mouse melanocortin 1 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
[PMID: 26433448]
HEK293 EC50
0.15 nM
Compound: alpha-MSH
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
[PMID: 26959173]
HEK293 EC50
0.22 nM
Compound: alpha-MSH
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
Agonist activity at mouse melanocortin receptor 3 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
[PMID: 32184956]
HEK293 EC50
0.22 nM
Compound: alpha-MSH
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
Agonist activity at mouse melanocortin receptor 5 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
[PMID: 32184956]
HEK293 EC50
0.22 nM
Compound: alpha-MSH
Agonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
Agonist activity at mouse MC5 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
[PMID: 26005535]
HEK293 EC50
0.28 nM
Compound: alpha-MSH
Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase assay
Agonist activity at mouse MC1R expressed in HEK293 cells by beta-galactosidase assay
[PMID: 15615519]
HEK293 EC50
0.3 nM
Compound: alpha-MSH
Agonist activity at mouse MC1 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
Agonist activity at mouse MC1 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
[PMID: 26005535]
HEK293 EC50
0.36 μM
Compound: alpha-MSH
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
Agonist activity at human recombinant MC5 receptor expressed in HEK293 cells assessed as cAMP accumulation by beta lactamase reporter gene assay
[PMID: 20329799]
HEK293 EC50
0.4 nM
Compound: alpha-MSH
Agonist activity at mouse MC3 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
Agonist activity at mouse MC3 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
[PMID: 26005535]
HEK293 EC50
0.5 nM
Compound: alpha-MSH
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
Agonist activity at mouse melanocortin 3 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
[PMID: 26433448]
HEK293 EC50
0.51 nM
Compound: alpha-MSH
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
Agonist activity at mouse melanocortin 5 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
[PMID: 26433448]
HEK293 EC50
0.52 nM
Compound: alpha-MSH
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay
Agonist activity at mouse MC3R expressed in HEK293 cells by beta-galactosidase assay
[PMID: 15615519]
HEK293 EC50
0.59 nM
Compound: alpha-MSH
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
[PMID: 26959173]
HEK293 EC50
0.65 nM
Compound: alpha-MSH
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
[PMID: 24517312]
HEK293 EC50
0.7 nM
Compound: alpha-MSH
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
Agonist activity at mouse MC1R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
[PMID: 18271518]
HEK293 EC50
0.76 nM
Compound: alpha-MSH
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
[PMID: 26959173]
HEK293 EC50
1.12 nM
Compound: alpha-MSH
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
Agonist activity at mouse MC5R expressed in HEK293 cells by beta-galactosidase assay
[PMID: 15615519]
HEK293 EC50
1.7 nM
Compound: alpha-MSH
Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
Agonist activity at mouse MC4 receptor expressed in HEK-293 cells assessed as cAMP response measured after 2 hrs incubation by cAMP Alphascreen assay
[PMID: 26005535]
HEK293 EC50
1.8 nM
Compound: alpha-MSH
Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation
Agonist activity at the mutant MC4R F184A expressed in HEK293 cells by cAMP accumulation
[PMID: 16451057]
HEK293 EC50
1.89 nM
Compound: alpha-MSH
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay
Agonist activity at mouse MC4R expressed in HEK293 cells by beta-galactosidase assay
[PMID: 15615519]
HEK293 EC50
156 nM
Compound: alpha-MSH
Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation
Agonist activity at the mutant MC4R Y287A expressed in HEK293 cells by cAMP accumulation
[PMID: 16451057]
HEK293 EC50
16.7 nM
Compound: alpha-MSH
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
Agonist activity at EYFP-fused human MC3R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
[PMID: 28972753]
HEK293 EC50
18 nM
Compound: alpha-MSH
Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation
Agonist activity at the mutant MC4R F184L expressed in HEK293 cells by cAMP accumulation
[PMID: 16451057]
HEK293 EC50
2 nM
Compound: alpha-MSH
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
Agonist activity at mouse MC5R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
[PMID: 18271518]
HEK293 EC50
2.14 nM
Compound: alpha-MSH
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
Agonist activity at mouse MC3R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
[PMID: 18271518]
HEK293 EC50
2.56 nM
Compound: alpha-MSH
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as forskolin-stimulated response by beta-galactosidase reporter gene assay
[PMID: 18271518]
HEK293 EC50
2.6 nM
Compound: alpha-MSH
Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation
Agonist activity at the mutant MC4R Y287F expressed in HEK293 cells by cAMP accumulation
[PMID: 16451057]
HEK293 EC50
2.9 nM
Compound: alpha-MSH
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
Agonist activity at mouse melanocortin 4 receptor expressed in HEK293 cells by AlphaScreen cAMP assay
[PMID: 26433448]
HEK293 EC50
2.9 nM
Compound: alpha-MSH
Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation
Agonist activity at the human wild type MC4R expressed in HEK293 cells by cAMP accumulation
[PMID: 16451057]
HEK293 EC50
21 nM
Compound: alpha-MSH
Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation
Agonist activity at the mutant MC4R Y268A expressed in HEK293 cells by cAMP accumulation
[PMID: 16451057]
HEK293 EC50
21 nM
Compound: alpha-MSH
Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation
Agonist activity at the mutant MC4R I125A expressed in HEK293 cells by cAMP accumulation
[PMID: 16451057]
HEK293 EC50
24.4 nM
Compound: alpha-MSH
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells assessed as increase in cAMP accumulation after 30 mins by luminescent enzymatic complementation based assay
[PMID: 28972753]
HEK293 EC50
27 nM
Compound: alpha-MSH
Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation
Agonist activity at the mutant MC4R I129A expressed in HEK293 cells by cAMP accumulation
[PMID: 16451057]
HEK293 EC50
3.7 nM
Compound: alpha-MSH
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
Agonist activity at mouse melanocortin receptor 4 expressed in HEK293 cells assessed as stimulation of cAMP accumulation incubated for 2 hrs by cAMP Alpha-screen assay
[PMID: 32184956]
HEK293 EC50
35.3 nM
Compound: alpha-MSH
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
Agonist activity at EYFP-fused human MC5R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
[PMID: 28972753]
HEK293 EC50
4 nM
Compound: alpha-MSH
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
Agonist activity at mouse MC4R expressed in HEK293 cells assessed as cAMP accumulation incubated for 2 hrs by alphascreen assay
[PMID: 26959173]
HEK293 EC50
7.1 nM
Compound: alpha-MSH
Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation
Agonist activity at the mutant MC4R Y268F expressed in HEK293 cells by cAMP accumulation
[PMID: 16451057]
HEK293 EC50
89 nM
Compound: alpha-MSH
Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation
Agonist activity at the mutant MC4R I291A expressed in HEK293 cells by cAMP accumulation
[PMID: 16451057]
HEK293 EC50
9.2 nM
Compound: alpha-MSH
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
Agonist activity at EYFP-fused human MC4R expressed in HEK293 cells after 16 to 20 hrs by CRE-driven reporter assay
[PMID: 28972753]
SAOS-2 EC50
1.8 nM
Compound: alpha-MSH
Activity at human MC1R by cAMP accumulation in SaoS2 cells
Activity at human MC1R by cAMP accumulation in SaoS2 cells
[PMID: 16678415]
SAOS-2 EC50
72.9 nM
Compound: alpha-MSH
Activity at human MC4R by cAMP accumulation in SaoS2 cells
Activity at human MC4R by cAMP accumulation in SaoS2 cells
[PMID: 16678415]
体外研究
(In Vitro)

α-MSH 通过直接作用于神经胶质细胞中的黑皮质素受体来调节 CNS 炎症。α-MSH 调节 NFκB 激活。α-MSH 抑制转录因子 κB 转运至细胞核[3]

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

体内研究
(In Vivo)

全身给予 α-MSH (50 μg/0.2 ml 生理盐水;ip) 可有效调节炎症反应[3]

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

Animal Model: IL-10–deficient mice[3]
Dosage: 50 µg/0.2 ml saline
Administration: I.p.
Result: Given systemically effectively modulated inflammatory reactions.
分子量

1664.88

Formula

C77H109N21O19S

CAS 号
性状

固体

颜色

White to off-white

Sequence

Ac-Ser-Tyr-Ser-Met-Glu-His-Phe-Arg-Trp-Gly-Lys-Pro-Val-NH2

Sequence Shortening

Ac-SYSMEHFRWGKPV-NH2

中文名称

α-黑素细胞刺激激素 (MSH),酰胺

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture and light, under nitrogen

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (60.06 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : ≥ 12.5 mg/mL (7.51 mM)

* "≥" 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 0.6006 mL 3.0032 mL 6.0064 mL
5 mM 0.1201 mL 0.6006 mL 1.2013 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 (sealed storage, away from moisture and light, under nitrogen)。-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。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 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
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.57%

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 (sealed storage, away from moisture and light, under nitrogen)。-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
H2O / DMSO 1 mM 0.6006 mL 3.0032 mL 6.0064 mL 15.0161 mL
5 mM 0.1201 mL 0.6006 mL 1.2013 mL 3.0032 mL
DMSO 10 mM 0.0601 mL 0.3003 mL 0.6006 mL 1.5016 mL
15 mM 0.0400 mL 0.2002 mL 0.4004 mL 1.0011 mL
20 mM 0.0300 mL 0.1502 mL 0.3003 mL 0.7508 mL
25 mM 0.0240 mL 0.1201 mL 0.2403 mL 0.6006 mL
30 mM 0.0200 mL 0.1001 mL 0.2002 mL 0.5005 mL
40 mM 0.0150 mL 0.0751 mL 0.1502 mL 0.3754 mL
50 mM 0.0120 mL 0.0601 mL 0.1201 mL 0.3003 mL
60 mM 0.0100 mL 0.0501 mL 0.1001 mL 0.2503 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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:
α-MSH
目录号:
HY-P0252
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