| Identification | Back Directory | [Name]
VU 0463271 | [CAS]
1391737-01-1 | [Synonyms]
VU 0463271
N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide
Acetamide, N-cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]-
VU0463271 (N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide)
VU0463271 (Synonyms: N-Cyclopropyl-N-(4-methyl-2-thiazolyl)-2-[(6-phenyl-3-pyridazinyl)thio]acetamide) | [Molecular Formula]
C19H18N4OS2 | [MDL Number]
MFCD30182240 | [MOL File]
1391737-01-1.mol | [Molecular Weight]
382.5 |
| Chemical Properties | Back Directory | [storage temp. ]
2-8°C | [solubility ]
Soluble in DMSO | [form ]
powder | [color ]
off-white to blue-gray | [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 | [InChIKey]
DPONSKCACOZTGN-UHFFFAOYSA-N | [SMILES]
[s]1c(nc(c1)C)N(C4CC4)C(=O)CSc2nnc(cc2)c3ccccc3 |
| Hazard Information | Back Directory | [Uses]
VU 0463271 is a novel antagonist of the neuronal-specific potassium-chloride cotransporter 2 (KCC2). | [Biological Activity]
VU0463271 is a potent and selective potassium-chloride cotransporter 2 (KCC2) inhibitor th at displays greatly enhanced potency than its structural analogs VU0255011 (ML077) & VU0240511 (IC50 = 61537and 568 nMrespectively). VU0463271 exhibits much reduced efficacy against the related Na-K-2Cl cotransporter 1 (NKCC1 inhibition max ~37% at 100 μM) and little affinity toward a panel of 68 GPCRsion channelsand transporters. Although VU0463271 is reported to exhibit affinity toward mitochondrial translocator protein TSPO (IC50 of 204 nM against PK11195 binding; r at heart) and inhibitory potency against α1B adrenergic receptor (IC50 of 364.7 nM; human α1B CHO transfectants)these proteins are not known to affect chloride homeostasis. | [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[1]. | [storage]
Store at +4°C |
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| Company Name: |
cjbscvictory
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| Tel: |
13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
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