Basic information Safety Supplier Related

VU0810464

Basic information Safety Supplier Related

VU0810464 Basic information

Product Name:
VU0810464
Synonyms:
  • VU0810464
  • Benzeneacetamide, 3-chloro-N-(1-cyclohexyl-3-methyl-1H-pyrazol-5-yl)-4-fluoro-
  • 2-(3-Chloro-4-fluorophenyl)-N-(1-cyclohexyl-3-methyl-1H-pyrazol-5-yl)acetamide
  • cells,KcsA,VU-0810464,Potassium Channel,neuronal GIRK,HPC,VU0810464,VU 0810464,SAN,inhibit,Inhibitor
  • VU0810464, 10 mM in DMSO
  • 3-?Chloro-?N-?(1-?cyclohexyl-?3-?methyl-?1H-?pyrazol-?5-?yl)?-?4-?fluoro-benzeneacetamide
CAS:
2126040-21-7
MF:
C18H21ClFN3O
MW:
349.83
Mol File:
2126040-21-7.mol
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VU0810464 Chemical Properties

Boiling point:
549.1±50.0 °C(Predicted)
Density 
1.31±0.1 g/cm3(Predicted)
storage temp. 
2-8°C
solubility 
DMSO: ≥ 250 mg/mL (714.63 mM)
pka
13.35±0.70(Predicted)
form 
Solid
color 
White to off-white
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VU0810464 Usage And Synthesis

Uses

VU0810464 is a potent and selective non-ureaG protein-gated inwardly-rectifying potassium channels (GIRK, Kir3) activator. VU0810464 displays nanomolar potency for neuronal (EC50=165 nM) and GIRK1/4 (EC50=720 nM) channels with improved brain penetration[1][2].

in vivo

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[2]. VU0810464 (intraperitoneal?injection?; 30 mg/kg; 15, 30, 45, or 60 min post‐injection) displays a favourable distribution to the brain (Kp,uu = 0.83), has a improvement over ML297 (Kp,uu= 0.32). Clearance of VU0810464 is rapid,brain and plasma half-lives is 20 min in a PK study[2].

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.

References

[1] Vo BN, et al. VU0810464, a non-urea G protein-gated inwardly rectifying K+?(Kir?3/GIRK) channel activator, exhibits enhanced selectivity for neuronal Kir?3 channels and reduces stress-induced hyperthermia in mice.Br J Pharmacol.?2019 Jul;176(13):2238-2249. DOI:10.1111/bph.14671
[2] Wieting JM,et al. Discovery and Characterization of 1H-Pyrazol-5-yl-2-phenylacetamides as Novel, Non-Urea-Containing GIRK1/2 Potassium Channel Activators.ACS Chem Neurosci.?2017?Sep 20;8(9):1873-1879. DOI:10.1021/acschemneuro.7b00217

VU0810464Supplier

Shanghai Beckham Medical Technology Co., Ltd
Tel
13816613772
Email
huahero21@sina.com
Shanghai YuanYe Biotechnology Co., Ltd.
Tel
021-61312847; 18021002903
Email
3008007409@qq.com
Tianjin Kailiqi Biotechnology Co., Ltd.
Tel
15076683720
Email
klq@cw-bio.com
Beijing Solarbio Science & Tecnology Co., Ltd.
Tel
010-50973130 18101056239
Email
3193328036@qq.com
TargetMol Chemicals Inc.
Tel
+1-781-999-5354; +17819995354
Email
marketing@targetmol.com
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VU0810464(2126040-21-7)Related Product Information