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  3. Palmatine hydroxide

Palmatine hydroxide 

目录号: HY-N0110B 纯度: 99.64%
COA 产品使用指南

Palmatine hydroxide 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 hydroxide 也能非竞争性抑制西尼罗病毒 (WNV) NS2B-NS3 蛋白酶,IC50 为 96 μM。Palmatine hydroxide 具有抗癌、抗炎、神经保护、抗细菌、抗病毒活性。

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Palmatine hydroxide Chemical Structure

Palmatine hydroxide Chemical Structure

CAS No. : 131-04-4

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10 mM * 1 mL in DMSO ¥220
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Other Forms of Palmatine hydroxide:

查看 mAChR 亚型特异性产品:

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

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Palmatine hydroxide 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 hydroxide can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC50 of 96 μM. Palmatine hydroxide shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities[1][2][3][4][5].

IC50 & Target

IDO-1

3 μM (IC50, HEK 293-hIDO-1)

IDO-1

157 μM (IC50, rhIDO-1)

WNV NS2B-NS3

96 μM (IC50)

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, 48 and 72 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, 48 and 72 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, 48 and 72 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

369.41

Formula

C21H23NO5

CAS 号
性状

固体

颜色

Light yellow to yellow

结构分类
初始来源
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 : 15.62 mg/mL (42.28 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7070 mL 13.5351 mL 27.0702 mL
5 mM 0.5414 mL 2.7070 mL 5.4140 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: 99.64%

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 2.7070 mL 13.5351 mL 27.0702 mL 67.6755 mL
5 mM 0.5414 mL 2.7070 mL 5.4140 mL 13.5351 mL
10 mM 0.2707 mL 1.3535 mL 2.7070 mL 6.7675 mL
15 mM 0.1805 mL 0.9023 mL 1.8047 mL 4.5117 mL
20 mM 0.1354 mL 0.6768 mL 1.3535 mL 3.3838 mL
25 mM 0.1083 mL 0.5414 mL 1.0828 mL 2.7070 mL
30 mM 0.0902 mL 0.4512 mL 0.9023 mL 2.2558 mL
40 mM 0.0677 mL 0.3384 mL 0.6768 mL 1.6919 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:
Palmatine hydroxide
目录号:
HY-N0110B
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