GSK2945 hydrochloride|西域试剂

GSK2945 hydrochloride,99.79%

产品编号：Bellancom-117147A| 分子式：C₂₀H₁₉Cl₃N₂O₂S| 分子量：457.80

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货号	价格	库存与货期
Bellancom-117147A	￥3500.00	杭州北京（现货）
Bellancom-117147A	￥5500.00	杭州北京（现货）
Bellancom-117147A	￥16500.00	杭州北京（现货）
Bellancom-117147A	￥22500.00	杭州北京（现货）

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GSK2945 hydrochloride

产品介绍

GSK2945 hydrochloride 是一类叔胺，是一种高度特异性的 Rev-erbα/REV-ERBα (小鼠/人反向成红细胞病病毒α) 拮抗剂，其 EC₅₀ 值分别为 21.5 μM 和 20.8 μM。GSK2945 hydrochloride 可增强胆固醇 7α-羟化酶 (CYP7A1) 水平和胆固醇代谢。

生物活性

GSK2945 hydrochloride is a class of tertiary amine, and is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist with EC₅₀s of 21.5 μM and 20.8 μM, respectively. GSK2945 hydrochloride enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism.

体外研究

GSK2945 dose-dependently enhances the transcriptional activity of Rev-erbα and a Bmal1 (a target gene of REV-ERBs) luciferase reporter (EC₅₀ of 2.05 μM).
GSK2945 (20 μM; 12 hours and 24 hours; mouse and human primary hepatocytes) treatment increases levels of Cyp7a1/CYP7A1 in mouse and human primary hepatocytes. GSK2945 (20 μM) treatment also increases Lrh-1/LRH-1 (a known hepatic activator of Cyp7a1/CYP7A1) mRNA and protein.

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

RT-PCR

Cell Line:	Mouse (male, CD1) and human (male, Caucasian) primary hepatocytes
Concentration:	20 μM
Incubation Time:	12 hours and 24 hours
Result:	Led to significant increases in mRNA and protein (at 24-h) expression of Cyp7a1. mRNA and protein (at 24-h) levels of CYP7A1 were increased in human primary hepatocyte. Lrh-1/LRH-1 was upregulated.

体内研究
(In Vivo)

GSK2945 (0-10 mg/kg; intraperitoneal injection; twice every day; for 7 days; male C57BL/6 mice) treatment increases hepatic mouse cholesterol 7α-hydroxylase (Cyp7a1) level and lowers plasma cholesterol in wild-type mice.

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

Animal Model:	Male C57BL/6 mice (8-10 weeks of age)
Dosage:	0 mg/kg or 10 mg/kg
Administration:	Intraperitoneal injection; twice every day; for 7 days
Result:	Increased hepatic mouse cholesterol 7α-hydroxylase (Cyp7a1) level and lowered plasma cholesterol in wild-type mice.

体内研究

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

Animal Model:	Male C57BL/6 mice (8-10 weeks of age)
Dosage:	0 mg/kg or 10 mg/kg
Administration:	Intraperitoneal injection; twice every day; for 7 days
Result:	Increased hepatic mouse cholesterol 7α-hydroxylase (Cyp7a1) level and lowered plasma cholesterol in wild-type mice.

体内研究

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

Animal Model:	Male C57BL/6 mice (8-10 weeks of age)
Dosage:	0 mg/kg or 10 mg/kg
Administration:	Intraperitoneal injection; twice every day; for 7 days
Result:	Increased hepatic mouse cholesterol 7α-hydroxylase (Cyp7a1) level and lowered plasma cholesterol in wild-type mice.

性状

Solid

溶解性数据

In Vitro:

DMSO : 20.83 mg/mL (45.50 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1844 mL	10.9218 mL	21.8436 mL
5 mM	0.4369 mL	2.1844 mL	4.3687 mL
10 mM	0.2184 mL	1.0922 mL	2.1844 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 (stored 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。

In Vivo:

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

1.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.08 mg/mL (4.54 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (4.54 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.8 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。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.54 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.54 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。