Product Name :
VU0810464
Description:
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.
CAS:
2126040-21-7
Molecular Weight:
349.83
Formula:
C18H21ClFN3O
Chemical Name:
2-(3-chloro-4-fluorophenyl)-N-(1-cyclohexyl-3-methyl-1H-pyrazol-5-yl)acetamide
Smiles :
CC1C=C(NC(=O)CC2C=C(Cl)C(F)=CC=2)N(N=1)C1CCCCC1
InChiKey:
HNJJARDABGKWSO-UHFFFAOYSA-N
InChi :
InChI=1S/C18H21ClFN3O/c1-12-9-17(23(22-12)14-5-3-2-4-6-14)21-18(24)11-13-7-8-16(20)15(19)10-13/h7-10,14H,2-6,11H2,1H3,(H,21,24)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
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.|Product information|CAS Number: 2126040-21-7|Molecular Weight: 349.83|Formula: C18H21ClFN3O|Chemical Name: 2-(3-chloro-4-fluorophenyl)-N-(1-cyclohexyl-3-methyl-1H-pyrazol-5-yl)acetamide|Smiles: CC1C=C(NC(=O)CC2C=C(Cl)C(F)=CC=2)N(N=1)C1CCCCC1|InChiKey: HNJJARDABGKWSO-UHFFFAOYSA-N|InChi: InChI=1S/C18H21ClFN3O/c1-12-9-17(23(22-12)14-5-3-2-4-6-14)21-18(24)11-13-7-8-16(20)15(19)10-13/h7-10,14H,2-6,11H2,1H3,(H,21,24)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : ≥ 250 mg/mL (714.{{Eliglustat} site|{Eliglustat} Technical Information|{Eliglustat} Purity|{Eliglustat} manufacturer|{Eliglustat} Autophagy} 63 mM).{{Penicillamine} medchemexpress|{Penicillamine} Apoptosis|{Penicillamine} Biological Activity|{Penicillamine} Data Sheet|{Penicillamine} supplier|{Penicillamine} Epigenetics} |Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.PMID:23671446 |Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|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.|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. 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.|Products are for research use only. Not for human use.|