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GSK1702934A

目录号: PL12472 纯度: ≥98%

GSK1702934A是一种选择性的 TRPC3 激动剂。GSK1702934A 通过激活 TRPC3 调节心脏收缩力和心律失常。

CAS No. :924377-85-5

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中文名称	GSK1702934A
中文别名	化合物 T15425
英文名称	GSK1702934A
英文别名	GSK1702934A;GTPL10278;GSK 1702934A;J3.648.055F;Z126939448;1-(1-(5,6,7,8-Tetrahydro-4H-cyclohepta[b]thiophene-2-ylcarbonyl)-4-piperidinyl)-1H-benzoimidazole-2(3H)-one;1,3-Dihydro-1-[1-[(5,6,7,8-tetrahydro-4H-cyclohepta[b]thien-2-yl)carbonyl]-4-piperidinyl]-2H-benzimidazol-2-one;1-(1-{4H,5H,6H,7H,8H-cyclohepta[b]thiophene-2-carbonyl}piperidin-4-yl)-2,3-dihydro-1H-1,3-benzodiazol-2-one;CID 16376051;GSK-1702934A,GSK1702934A;2H-Benzimidazol-2-one, 1,3-dihydro-1-[1-[(5,6,7,8-tetrahydro-4H-cyclohepta[b]thien-2-yl)carbonyl]-4-piperidinyl]-
Cas No.	924377-85-5
分子式	C₂₂H₂₅N₃O₂S
分子量	396.00
包装储存	Powder -20°C 3 years；In solvent -80°C 6 months
详情描述	GSK1702934A是一种选择性的 TRPC3 激动剂。GSK1702934A 通过激活 TRPC3 调节心脏收缩力和心律失常。

产品详情	GSK1702934A是一种选择性的 TRPC3 激动剂。GSK1702934A 通过激活 TRPC3 调节心脏收缩力和心律失常。
生物活性	GSK1702934A is a selective TRPC3 agonist. GSK1702934A modulates cardiac contractility and f arrhythmogenesis by activation of TRPC3.
性状	Solid
IC50 & Target[1][2]	TRPC3
体外研究(In Vitro)	GSK1702934A is able to induce TRPC3/6-currents in HEK293 cells transduced with recombinant human TRPC3/6 with an EC50 of 0.08 mM and 0.44 mM, respectively. GSK1702934A induces a transient, non-selective conductance and prolonged action potentials in TRPC3-overexpressing myocytes but not in wild-type myocytes. GSK1702934A substantially promotes NCX currents in TRPC3-overexpressing myocytes. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	GSK1702934A (0.3-3 mg/kg; i.v.) transiently increases blood pressure by 15 ~ 35 mmHg in conscious Sprague Dawley rats. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；In solvent -80°C 6 months
参考文献	[1]. de la Cruz GG, et al. Intensified Microwave-Assisted N-Acylation Procedure - Synthesis and Activity Evaluation of TRPC3 Channel Agonists with a 1,3-Dihydro-2H-benzo[d]imidazol-2-one Core. Synlett. 2017 Apr;28(6):695-700. [2]. Doleschal B, et al. TRPC3 contributes to regulation of cardiac contractility and arrhythmogenesis by dynamic interaction with NCX1. Cardiovasc Res. 2015 Apr 1;106(1):163-73.

溶解度数据	In Vitro: DMSO : 100 mg/mL (252.83 mM; Need ultrasonic)配制储备液

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[1]. de la Cruz GG, et al. Intensified Microwave-Assisted N-Acylation Procedure - Synthesis and Activity Evaluation of TRPC3 Channel Agonists with a 1,3-Dihydro-2H-benzo[d]imidazol-2-one Core. Synlett. 2017 Apr;28(6):695-700.
[2]. Doleschal B, et al. TRPC3 contributes to regulation of cardiac contractility and arrhythmogenesis by dynamic interaction with NCX1. Cardiovasc Res. 2015 Apr 1;106(1):163-73.

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

GSK1702934A

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