GSK2798745
目录号: PL12473 纯度: ≥99%
CAS No. :1419609-94-1
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中文名称
GSK2798745
中文别名
1-(((5S,7S)-3-(5-(2-hydroxypropan-2-yl)pyrazin-2-yl)-7-methyl-2-oxo-1-oxa-3-azaspiro[4.5]decan-7-yl)methyl)-1H-benzo[d]imidazole-6-carbonitrile
英文名称
GSK2798745
英文别名
1-(((5S,7S)-3-(5-(2-hydroxypropan-2-yl)pyrazin-2-yl)-7-methyl-2-oxo-1-oxa-3-azaspiro[4.5]decan-7-yl)methyl)-1H-benzo[d]imidazole-6-carbonitrile;GSK2798745;63FJ7LF55O;URCMKDJBULWNAI-DQEYMECFSA-N;3-[[(5S,7S)-3-[5-(2-Hydroxypropan-2-yl)pyrazin-2-yl]-7-methyl-2-oxo-1-oxa-3-azaspiro[4.5]decan-7-yl];3-[[(5S,7S)-3-[5-(2-hydroxypropan-2-yl)pyrazin-2-yl]-7-methyl-2-oxo-1-oxa-3-azaspiro[4.5]decan-7-yl]methyl]benzimidazole-5-carbonitrile;BDBM50502640;AT16701;1-(((5S,7S)-3-(5-(2-Hydroxypropan-2-yl)pyrazin-2-yl)-7-methyl-2-oxo-1-oxa-3-azaspiro(4.5)decan-7-yl)methyl)-1hbenzo(d)imidazole-6-carbonitrile;1-(((5S,7S)-3-(5-(2-hydroxypropan-2-yl)pyrazin-2-yl)-7-methyl-2-oxo-1-oxa-3-az;Unii-63FJ7LF55O
Cas No.
1419609-94-1
分子式
C25H28N6O3
分子量
460.53
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
GSK2798745 是一种强效的、选择性的且具有口服活性的瞬时受体电位香草酸 4 (TRPV4) 离子通道阻断剂,对 hTRPV4 和 rTRPV4 的 IC50 值分别为 1.8 和 1.6 nM。GSK2798745 可用于心脏和呼吸系统疾病研究。
生物活性
GSK2798745 is a potent, selective, and orally active transient receptor potential vanilloid 4 (TRPV4) ion channel blocker with IC 50 s of 1.8 and 1.6 nM for hTRPV4 and rTRPV4, respectively. GSK2798745 can be used in cardiac and respiratory diseases research.
性状
Solid
IC50 & Target[1][2]
IC50: 1.8 nM (hTRPV4) and 1.6 nM (rTRPV4)
体外研究(In Vitro)
GSK2798745 inhibits TRPV4 agonist-induced impedance reduction in human umbilical vein endothelial cells (HUVECs). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
GSK2798745 inhibits TRPV4 agonist-mediated lung edema in rats in a dose-dependent manner. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: TRPV4-mediated lung edema in male Sprague-Daw
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Goyal N, et al. Clinical Pharmacokinetics, Safety, and Tolerability of a Novel, First-in-Class TRPV4 Ion Channel Inhibitor, GSK2798745, in Healthy and Heart Failure Subjects. Am J Cardiovasc Drugs. 2019 Jun;19(3):335-342.
[2]. Brooks CA, et al. Discovery of GSK2798745: A Clinical Candidate for Inhibition of Transient Receptor Potential Vanilloid 4 (TRPV4). ACS Med Chem Lett. 2019 Jul 15;10(8):1228-1233.
溶解度数据
In Vitro: DMSO : 250 mg/mL (542.85 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

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。

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