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SR 8278 Sale

目录号 : GC15275

An antagonist of REV-ERBα

SR 8278 Chemical Structure

Cas No.:1254944-66-5

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,485.00
现货
1mg
¥628.00
现货
5mg
¥1,350.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

REV-ERBα is a nuclear receptor and transcription repressor that coordinates circadian rhythm and metabolic pathways in a heme-dependent manner.[1],[2] SR8278 is an antagonist of REV-ERBα (EC50 = 0.47 µM), blocking activation of the receptor by the synthetic agonist GSK 4112.[2] Moreover, SR8278 stimulates the expression of two REV-ERBα target genes involved in the regulation of glucose production, glucose 6-phosphatase and phosphoenolpyruvate carboxykinase, in liver cells.2 SR8278 has been used, with GSK 4112, to elucidate the role of REV-ERBα in regulating glucagon secretion in pancreatic alpha cells.[3]

Reference:
[1]. Duez, H., and Staels, B. Rev-erb-α: An integrator of circadian rhythms and metabolism. Journal of Applied Physiology 107(6), 1972-1980 (2009).
[2]. Kojetin, D., Wang, Y., Kameneck, T.M., et al. Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB. ACS Chemical Biology 6(2), 131-134 (2011).
[3]. Vieira, E., Marroquí, L., Figueroa, A.L., et al. Involvement of the clock gene Rev-erb alpha in the regulation of glucagon secretion in pancreatic alpha-cells. PLoS One 8(7), 1-15 (2013).

Chemical Properties

Cas No. 1254944-66-5 SDF
化学名 (S)-ethyl 2-(5-(methylthio)thiophene-2-carbonyl)-1,2,3,4-tetrahydroisoquinoline-3-carboxylate
Canonical SMILES O=C([C@H]1N(C(C2=CC=C(SC)S2)=O)CC3=CC=CC=C3C1)OCC
分子式 C18H19NO3S2 分子量 361.48
溶解度 ≤15mg/ml in ethanol;≤10mg/ml in DMSO 储存条件 Store at -20°C
General tips 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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.7664 mL 13.832 mL 27.664 mL
5 mM 0.5533 mL 2.7664 mL 5.5328 mL
10 mM 0.2766 mL 1.3832 mL 2.7664 mL
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