Product Name :
VU0463271
Description:
VU0463271 is a selective KCC2 antagonist, with an IC50 of 61 nM.
CAS:
1391737-01-1
Molecular Weight:
382.50
Formula:
C19H18N4OS2
Chemical Name:
N-cyclopropyl-N-(4-methyl-1,3-thiazol-2-yl)-2-[(6-phenylpyridazin-3-yl)sulfanyl]acetamide
Smiles :
CC1=CSC(=N1)N(C1CC1)C(=O)CSC1C=CC(=NN=1)C1C=CC=CC=1
InChiKey:
DPONSKCACOZTGN-UHFFFAOYSA-N
InChi :
InChI=1S/C19H18N4OS2/c1-13-11-26-19(20-13)23(15-7-8-15)18(24)12-25-17-10-9-16(21-22-17)14-5-3-2-4-6-14/h2-6,9-11,15H,7-8,12H2,1H3
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:
VU0463271 is a selective KCC2 antagonist, with an IC50 of 61 nM.|Product information|CAS Number: 1391737-01-1|Molecular Weight: 382.50|Formula: C19H18N4OS2|Chemical Name: N-cyclopropyl-N-(4-methyl-1,3-thiazol-2-yl)-2-[(6-phenylpyridazin-3-yl)sulfanyl]acetamide|Smiles: CC1=CSC(=N1)N(C1CC1)C(=O)CSC1C=CC(=NN=1)C1C=CC=CC=1|InChiKey: DPONSKCACOZTGN-UHFFFAOYSA-N|InChi: InChI=1S/C19H18N4OS2/c1-13-11-26-19(20-13)23(15-7-8-15)18(24)12-25-17-10-9-16(21-22-17)14-5-3-2-4-6-14/h2-6,9-11,15H,7-8,12H2,1H3|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 25 mg/mL (65.Gap 26 Inhibitor 36 mM; Need ultrasonic).|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.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|VU0463271 is a potent antagonist of the neuronal-specific potassium-chloride cotransporter 2 (KCC2), with an IC50 of 61 nM and >100-fold selectivity versus the closely related Na-K-2Cl cotransporter 1 (NKCC1) and no activity in a larger panel of GPCRs, ion channels and transporters. It is also found rapidly cleared in vitro.Ziritaxestat References VU0463271 is applied to the transected CNS preparation and resulted in a significant increase in firing rates of the Drosophila CNS with 1 μM VU0463271 resulting in a peak firing rate that was a 2.PMID:32644525 7- and 2.5-fold increase over baseline firing rate for OR and rdl strains, respectively. VU0463271 (10-100 nM) results in approximately 20% reduction of CNS firing frequency within asmall percentage of preparations.|In Vivo:|VU0463271 is found to be a moderate-to-high clearance compound in rat (CL=57 mL/min/kg) following intravenous administration (1 mg/kg); the low volume of distribution at steady state (Vss 0.4 L/kg), coupled with moderate-to-high clearance produce a relatively short t1/2 (9 min) in vivo.|Products are for research use only. Not for human use.|
