Palmatine 黄藤素|cas:3486-67-7|西域试剂

Palmatine 黄藤素

产品编号：Bellancom-N0110A| CAS NO：3486-67-7| 分子式：C₂₁H₂₂NO₄⁺| 分子量：352.40

Palmatine 是一种口服活性的不可逆 IDO-1 抑制剂。Palmatine 可以减轻结肠损伤，预防肠道菌群失调和调节色氨酸分解代谢，从而改善DSS诱发的结肠炎。Palmatine 有潜力用于结肠炎的研究。

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	包装	价格	库存与货期	购买量	操作
Bellancom-N0110A		￥500.00	杭州北京（现货）
Bellancom-N0110A		￥750.00	杭州北京（现货）

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Palmatine 黄藤素

产品介绍

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

生物活性

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

体外研究

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.
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].

西域 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.
Palmatine (0-200 mg/kg; i.p.; once) attenuates D-galactosamine/Lipopolysaccharides (HY-D1056)-induced fulminant hepatic failure in mice.
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].

西域 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)
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
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.

体内研究

西域 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)
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
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.

体内研究

西域 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)
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
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (283.77 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8377 mL	14.1884 mL	28.3768 mL
5 mM	0.5675 mL	2.8377 mL	5.6754 mL
10 mM	0.2838 mL	1.4188 mL	2.8377 mL

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 (protect from light)。-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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

参考文献

. Zhang XJ, et al. Palmatine ameliorated murine colitis by suppressing tryptophan metabolism and regulating gut microbiota.Pharmacol Res. 2018 Nov;137:34-46. [Content Brief]

. Lee WC, et al. Palmatine attenuates D-galactosamine/lipopolysaccharide-induced fulminant hepatic failure in mice. Food Chem Toxicol. 2010 Jan;48(1):222-8. [Content Brief]

. Jia F, et al. Identification of palmatine as an inhibitor of West Nile virus. Arch Virol. 2010 Aug;155(8):1325-9. [Content Brief]

[4]. Dhingra D, et al. Memory-enhancing activity of palmatine in mice using elevated plus maze and morris water maze. Adv Pharmacol Sci. 2012;2012:357368. [Content Brief]

[5]. Liu X, et al. Palmatine induces G2/M phase arrest and mitochondrial-associated pathway apoptosis in colon cancer cells by targeting AURKA. Biochem Pharmacol. 2020 May;175:113933. [Content Brief]

[6]. Long J, et al. Palmatine: A review of its pharmacology, toxicity and pharmacokinetics. Biochimie. 2019 Jul;162:176-184. [Content Brief]

化学品安全说明书(MSDS)

下载MSDS

质检证书(COA)

产品编号(Item Number)

批号(Lot Number)

海关编码	2933990090

1. 物质的识别

产品名：	Palmatine
CAS号：	3486-67-7
制造商/供应商：	西域试剂网站：www.hzbp.cn 邮件：13911702513@139.com

2. 合成/成分数据

产品名：	Palmatine
分子式：	C21H22NO4+
分子量：	352.40

3. 急救措施

吸入后：	如果吸入，移至空气新鲜处，如果呼吸困难，给输氧，如呼吸停止，给予人工呼吸。
皮肤接触后：	用大量的水冲洗，移除污染的衣服和鞋子。
眼睛接触后：	检查并取下隐形眼镜，并用大量的水冲洗；呼叫医生。
吞食后：	如果吞食，用大量纯净水漱口；呼叫医生。

4. 消防措施

适当的灭火剂：	雾状水，二氧化碳，干粉或泡沫。
防护设备：	穿戴自给式呼吸器和防护服，以防止与皮肤和眼睛接触。

5. 泄漏应急处理

安全防范措施：	封锁泄漏区域；穿戴自给式呼吸器，防护服和厚橡胶手套。
清洁/收集措施：	使用液体粘合原料（硅藻土，通用粘合剂）吸取精细粉末；使用酒精擦洗表面和设备除去污渍；根据第11条处理被污染的材料。

6. 处理和储存

安全处理说明：	避免吸入和接触皮肤，眼睛及衣物；材料可能略微具有刺激性。
储存：	粉末型式 -20°C 3年；4°C 2年溶于溶剂 -80°C 6个月；-20°C 1个月

7. 接触控制和个人防护

呼吸设备：	NIOSH / MSHA认可的呼吸器。
双手保护：	耐化学腐蚀的橡胶手套。
眼睛防护：	化学安全护目镜。

8. 稳定性和反应活性

稳定性：	按照说明存储是稳定的；避免强氧化剂。
热分解/其他要避免的情况：	避免光和热。

9. 毒性资料

急性毒性：	无可用资料。
主要刺激性影响：	无可用资料。
在皮肤上：	无可用资料。
对眼睛：	无可用资料；可能具有刺激性。