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2126040-21-7

中文名稱 VU0810464
英文名稱 VU0810464
CAS 2126040-21-7
分子式 C18H21ClFN3O
分子量 349.83
MOL 文件 2126040-21-7.mol
更新日期 2026/05/25 13:08:19
2126040-21-7 結(jié)構(gòu)式 2126040-21-7 結(jié)構(gòu)式

基本信息

中文別名
化合物VU0810464
2-(3-氯-4-氟苯基)-N-(1-環(huán)己基-3-甲基-1H-吡唑-5-基)乙酰胺
英文別名
VU0810464
Benzeneacetamide, 3-chloro-N-(1-cyclohexyl-3-methyl-1H-pyrazol-5-yl)-4-fluoro-

物理化學(xué)性質(zhì)

沸點549.1±50.0 °C(Predicted)
密度1.31±0.1 g/cm3(Predicted)
儲存條件Sealed in dry,2-8°C
溶解度DMSO: ≥ 250 mg/mL (714.63 mM)
酸度系數(shù)(pKa)13.35±0.70(Predicted)
形態(tài)Solid
顏色White to off-white

安全數(shù)據(jù)

危險性符號(GHS)有害 (GHS07)
GHS07
警示詞警告
危險性描述H302-H315-H319-H335
VU0810464價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2025/12/22HY-127106VU08104642126040-21-71 mg696元
2025/12/22HY-127106VU0810464
VU0810464
2126040-21-710mM * 1mLin DMSO1338元
2025/12/22HY-127106VU0810464
VU0810464
2126040-21-75mg1738元

常見問題列表

生物活性
VU0810464 是有效的,選擇性的非尿素蛋白門控的內(nèi)向整流鉀通道 (GIRK, Kir3) 激活劑。 VU0810464 對神經(jīng)元 GIRK1/2 (EC50=165 nM) 和 GIRK1/4 (EC50=720 nM) 神經(jīng)通道具有納摩爾效價,并且具有腦部滲透性。
靶點

EC50: 165 nM (GIRK 1/2); 720 nM (GIRK1/4 )

體外研究

VU0810464 (0, 0.1, 0.3, 1, 3, 10, 30 μM) produces a concentration‐dependent response curves of currents in SAN and HPC cells, in addition, VU0810464 is 9‐fold higher potency for Kir3 channel activation in neurons as compared to SAN cells.

體內(nèi)研究

VU0810464 (intraperitoneal?injection; 30 mg/kg, 10 mg/kg; 30mg/kg; pre-treated 30 mins) produces a dose-dependent reduction of SIH response in Male C57BL/6J mice. To test if VU0810464 plays it role through Kir3 channel activation, VU0810464 (10 mg/kg) suppresses the SIH response in wild‐ type mice, but has no impact on Kcnj3 ?/? mice. VU0810464 (intraperitoneal?injection?; 30 mg/kg; 15, 30, 45, or 60 min post‐injection) displays a favourable distribution to the brain (K p,uu = 0.83), has a improvement over ML297 (K p,uu = 0.32). Clearance of VU0810464 is rapid,brain and plasma half-lives is 20 min in a PK study.

Animal Model: Male C57BL/6J mice, Kcnj3 ?/? siblings female and male C57BL/6J mice
Dosage: 10 mg/kg; 30mg/kg
Administration: Intraperitoneal?injection
Result: Reduced stress‐induced hyperthermia (SIH), a physiological test of anxiolytic efficacy in wild mice, but had no impact in and Kcnj3 (Girk1) ?/? mice.
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