GSK4112 SR6452|cas:1216744-19-2|西域试剂

GSK4112 SR6452,98.0%

产品编号：Bellancom-14414| CAS NO：1216744-19-2| 分子式：C₁₈H₂₁ClN₂O₄S| 分子量：396.89

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货号	价格	库存与货期
Bellancom-14414	￥500.00	杭州北京（现货）
Bellancom-14414	￥900.00	杭州北京（现货）
Bellancom-14414	￥3600.00	杭州北京（现货）
Bellancom-14414	￥6500.00	杭州北京（现货）

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GSK4112 SR6452

产品介绍

GSK4112 (SR6452) 是 Rev-erbα 的激动剂，EC₅₀ 值为 0.4 μM。GSK4112 可作为一种化学工具来探究 Rev-erbα 在转录抑制、昼夜节律生物学调节和代谢途径中的功能。

生物活性

GSK4112 (SR6452) is a Rev-erbα agonist with an EC₅₀ value of 0.4 μM. GSK4112 can be used as a chemical tool to probe the function of Rev-erbα in transcriptional repression, regulation of circadian biology, and metabolic pathways.

体外研究

GSK4112 (0-100 μM; 1 h) interacts with Rev-erbα with an EC₅₀ value of 0.4 μM.
GSK4112 (10 μM; 6 h) represses expression of bmal1 and the target genes associated with the pathway of gluconeogenesis, recruits HDAC3 and modulates the effect of Rev-erbα on oscillation of hepatic gene expression.
GSK4112 (10 μM; 16 h) reduces glucose output in murine hepatocytes.

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

RT-PCR

Cell Line:	HepG2 cell line
Concentration:	10 μM
Incubation Time:	6 hours
Result:	Repressed mRNA levels of bmal1, G6 Pase, PEPCK and PGC1α.

体内研究
(In Vivo)

GSK4112 (25 mg/kg; i.p. 0.5 h before Jo2 exposure) attenuates Fas-induced hepatic damage.

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

Animal Model:	Male C57BL/6 mice with Fas-induced acute hepatic damage
Dosage:	25 mg/kg
Administration:	Intraperitoneal injection; 25 mg/kg; 0.5 h before Jo2 exposure
Result:	Obviously ameliorated the degree of liver damage, suppressed Jo2-induced ALT and AST increasing, improved the survival rate of mice and suppressed Fas-induced hepatocyte apoptosis.

体内研究

GSK4112 (25 mg/kg; i.p. 0.5 h before Jo2 exposure) attenuates Fas-induced hepatic damage.

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

Animal Model:	Male C57BL/6 mice with Fas-induced acute hepatic damage
Dosage:	25 mg/kg
Administration:	Intraperitoneal injection; 25 mg/kg; 0.5 h before Jo2 exposure
Result:	Obviously ameliorated the degree of liver damage, suppressed Jo2-induced ALT and AST increasing, improved the survival rate of mice and suppressed Fas-induced hepatocyte apoptosis.

体内研究

GSK4112 (25 mg/kg; i.p. 0.5 h before Jo2 exposure) attenuates Fas-induced hepatic damage.

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

Animal Model:	Male C57BL/6 mice with Fas-induced acute hepatic damage
Dosage:	25 mg/kg
Administration:	Intraperitoneal injection; 25 mg/kg; 0.5 h before Jo2 exposure
Result:	Obviously ameliorated the degree of liver damage, suppressed Jo2-induced ALT and AST increasing, improved the survival rate of mice and suppressed Fas-induced hepatocyte apoptosis.

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (62.99 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5196 mL	12.5979 mL	25.1959 mL
5 mM	0.5039 mL	2.5196 mL	5.0392 mL
10 mM	0.2520 mL	1.2598 mL	2.5196 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。-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 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (6.30 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.30 mM，饱和度未知) 的澄清溶液。
以 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；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (6.30 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (6.30 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 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。
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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.30 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.30 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。