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  3. Palmatine chloride

Palmatine chloride  (Synonyms: 盐酸巴马汀)

目录号: HY-N0110 纯度: 99.81%
COA 产品使用指南

Palmatine chloride 是一种具有口服活性的、不可逆的 IDO-1 抑制剂,对 HEK 293-hIDO-1 和 rhIDO-1 的 IC50 分别为 3 μM 和 157 μM。Palmatine chloride 也能非竞争性抑制西尼罗病毒 (WNV) NS2B-NS3 蛋白酶,IC50 为 96 μM。Palmatine chloride 具有抗癌、抗炎、神经保护、抗细菌、抗病毒活性。

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Palmatine chloride Chemical Structure

Palmatine chloride Chemical Structure

CAS No. : 10605-02-4

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10 mM * 1 mL in DMSO ¥220
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250 mg ¥200
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1 g ¥500
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Other Forms of Palmatine chloride:

查看 mAChR 亚型特异性产品:

查看 Indoleamine 2,3-Dioxygenase (IDO) 亚型特异性产品:

查看 Aurora Kinase 亚型特异性产品:

查看 Parasite 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

Palmatine chloride is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC50s of 3 μM and 157μM against HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine chloride can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC50 of 96 μM. Palmatine chloride shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities[1][2][3][4][5].

IC50 & Target[1]

IDO-1

3 μM (IC50, HEK 293-hIDO-1)

IDO-1

157 μM (IC50, rhIDO-1)

WNV NS2B-NS3

96 μM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
G-402 GI50
83.14 μM
Compound: 3
Growth inhibition against human G402 cells after 48 hrs by MTT assay
Growth inhibition against human G402 cells after 48 hrs by MTT assay
[PMID: 21401114]
HCT-116 IC50
> 100 μM
Compound: Palmatine Chloride
Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
[PMID: 28359045]
HepG2 IC50
> 100 μM
Compound: Palmatine Chloride
Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay
[PMID: 28359045]
HL-60 IC50
> 100 μM
Compound: Palmatine Chloride
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
[PMID: 28359045]
KM12C IC50
393 μM
Compound: B-11
Inhibition of cell proliferation of human KM12C cells incubated for 15 hrs by MTT assay
Inhibition of cell proliferation of human KM12C cells incubated for 15 hrs by MTT assay
[PMID: 32391701]
L02 IC50
> 100 μM
Compound: Palmatine Chloride
Cytotoxicity against human LO2 cells after 72 hrs by MTT assay
Cytotoxicity against human LO2 cells after 72 hrs by MTT assay
[PMID: 28359045]
SMMC-7721 IC50
> 100 μM
Compound: Palmatine Chloride
Cytotoxicity against human SMMC7721 cells after 72 hrs by MTT assay
Cytotoxicity against human SMMC7721 cells after 72 hrs by MTT assay
[PMID: 28359045]
体外研究
(In Vitro)

Palmatine (0-100 μM; 42 h) suppresses WNV with an EC50 value of 3.6 μM, and reduce the viral titers of DENV-2 and YFV with EC50 values of 26.4 μM and 7.3 μM, respectively[3].
? Palmatine (0-1128 μM; 24-72 h) inhibits colon cancer cell proliferation[5].
? Palmatine (0-704 μM; 24 h) reduces AURKA protein levels, induces G2/M phase arrest, and induces apoptosis in colon cancer cells via the mitochondrial associated pathway[5].

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

Cell Proliferation Assay[5]

Cell Line: HCT-116, SW480, HT-29
Concentration: 0, 88, 176, 352, and 704 μM (HCT-116, SW480); 0, 141, 282, 564, and 1128 μM (HT-29)
Incubation Time: 24, 48 and 72 h
Result: Decreased cell viability in a dose-dependent manner.

Western Blot Analysis[5]

Cell Line: HCT-116, SW480, HT-29
Concentration: 100 nM for HCT-116, 500 nM for SW480 and HT-29
Incubation Time: 24 h
Result: Promoted the expression of apoptosis markers such as P53 / P73, Caspase3, and Caspase9. Reduced AURKA protein levels. Increased cyt. c in the cytoplasm while reduced Bcl2 and Bcl-xl in a dose-dependent manner.

Cell Cycle Analysis[5]

Cell Line: HCT-116, SW480
Concentration: 88, 176, 352 and 704 μM
Incubation Time: 24 h
Result: Induced G2/M phase arrest in a dose-dependent manner.

Apoptosis Analysis[5]

Cell Line: HCT-116, SW480
Concentration: 88, 176, 352 and 704 μM
Incubation Time: 24 h
Result: Induced apoptosis in a dose-dependent manner.
体内研究
(In Vivo)

Palmatine (50 or 100 mg/kg; p.o.; daily for 7 days) ameliorates DSS (dextran sulfate sodium)-induced colitis and prevents infiltration of inflammatory cells[1].
? Palmatine (0-200 mg/kg; i.p.; once) attenuates D-galactosamine/Lipopolysaccharides (HY-D1056)-induced fulminant hepatic failure in mice[2].
? Palmatine (0-1 mg/kg; i.p.; 10 days) shows memory-enhancing activity in mice[4].
? Palmatine (33.75-135 mg/kg; p.o.; daily for 26 days) can effectively inhibit the growth of HCT-116 xenografts in mice[5].

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

Animal Model: DSS- induced Colitis BALB/c mice model (8-week-old)[1]
Dosage: 50 or 100 mg/kg
Administration: Orally, daily, for 7 days
Result: Ameliorated DSS-induced colitis and prevented infiltration of inflammatory cells; remarkably extended the colon length; significantly suppressed the colonic MPO activity. Decreased the levels of colonic inflammatory cytokines (TNF-α, IFN-γ, IL-1β, IL-6, IL-4 and IL-10); Protected mucosal integrity by modulating TJs protein and apoptosis proteins; Restored DSS-induced decreases of TJ protein ZO-1, ZO-2 and claudin-1; Reduced Bax expression and enhanced Bcl-2 expression at the dose of 100 mg/kg, prevented epithelial apoptosis and improved intestinal integrity. Prevented DSS-induced changes of gut microbiota in colitis mice.
Animal Model: Male ICR mice (20–22 g), D-galactosamine/lipopolysaccharide (GalN/LPS)-induced fulminant hepatic failure model[2]
Dosage: 25, 50, 100, or 200 mg/kg
Administration: Intraperitoneal injection, 1 h before the GalN/LPS treatment
Result: Attenuated the mortality and serum aminotransferase activities increased by GalN/LPS. Prevented the increase of serum TNF-α and augmented that of serum IL-10. Decreased the TNF-a mRNA expression and increased the IL-10 mRNA expression. Attenuated the apoptosis of hepatocytes.
Animal Model: Swiss young male albino mice, with Scopolamine (HY-N0296)- and diazepam-induced amnesia model[4]
Dosage: 0.1, 0.5, 1 mg/kg
Administration: Intraperitoneal injection, 10 days
Result: Significantly improved learning and memory of mice at 0.5 and 1 mg/kg and did not show any significant effect on locomotor activity of the mice. Significantly reversed scopolamine- and diazepam-induced amnesia in mice. Significantly reduced brain acetylcholinesterase activity of mice.
Animal Model: BALB/c-nude mice, HCT-116 xenograft model[5]
Dosage: 33.75, 67.5 and 135 mg/kg
Administration: Oral administration, once a day for 26 days
Result: The tumor volume and weight of the treatment group were significantly reduced.
分子量

387.86

Formula

C21H22ClNO4

CAS 号
性状

固体

颜色

Light yellow to yellow

中文名称

盐酸巴马汀;盐酸巴马亭;盐酸掌叶防己碱;氯化巴马亭;棕榈碱

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

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

溶解性数据
细胞实验: 

DMSO 中的溶解度 : ≥ 32 mg/mL (82.50 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)

H2O 中的溶解度 : 5 mg/mL (12.89 mM; 超声助溶)

* "≥" 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 2.5782 mL 12.8912 mL 25.7825 mL
5 mM 0.5156 mL 2.5782 mL 5.1565 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, 1 year; -20°C, 6 months (sealed storage, away from moisture and light)。-80°C储存时,请在1年内使用, -20°C储存时,请在6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 (6.45 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 (6.45 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 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。

以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 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: PBS

    Solubility: 2.5 mg/mL (6.45 mM); 澄清溶液; 超声助溶 (<60°C)

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)。

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

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: 99.81%

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, 1 year; -20°C, 6 months (sealed storage, away from moisture and light)。-80°C储存时,请在1年内使用, -20°C储存时,请在6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 2.5782 mL 12.8912 mL 25.7825 mL 64.4562 mL
5 mM 0.5156 mL 2.5782 mL 5.1565 mL 12.8912 mL
10 mM 0.2578 mL 1.2891 mL 2.5782 mL 6.4456 mL
DMSO 15 mM 0.1719 mL 0.8594 mL 1.7188 mL 4.2971 mL
20 mM 0.1289 mL 0.6446 mL 1.2891 mL 3.2228 mL
25 mM 0.1031 mL 0.5156 mL 1.0313 mL 2.5782 mL
30 mM 0.0859 mL 0.4297 mL 0.8594 mL 2.1485 mL
40 mM 0.0645 mL 0.3223 mL 0.6446 mL 1.6114 mL
50 mM 0.0516 mL 0.2578 mL 0.5156 mL 1.2891 mL
60 mM 0.0430 mL 0.2149 mL 0.4297 mL 1.0743 mL
80 mM 0.0322 mL 0.1611 mL 0.3223 mL 0.8057 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。

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产品名称:
Palmatine chloride
目录号:
HY-N0110
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