VU 0463271
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- CAS号:
- 1391737-01-1
- 英文名:
- VU 0463271
- 英文别名:
- VU 0463271;Inhibitor,KcsA,VU0463271,Potassium Channel,VU 0463271,VU-0463271,inhibit;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)
- 中文名:
- VU 0463271
- 中文别名:
- 化合物 T17243;化合物VU0463271;N-环丙基-N-(4-甲基-2-噻唑基)-2-[(6-苯基-3-哒嗪基)硫基]乙酰胺
- CBNumber:
- CB74668658
- 分子式:
- C19H18N4OS2
- 分子量:
- 382.5
- MOL File:
- 1391737-01-1.mol
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VU 0463271化学性质
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储存条件:
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2-8°C
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溶解度:
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Soluble in DMSO
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形态:
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powder
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颜色:
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off-white to blue-gray
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VU 0463271性质、用途与生产工艺
VU0463271 是选择性的神经特异性氯钾协同转运蛋白 2 (KCC2) 的有效抑制剂，其 IC50 值为 61 nM。
VU0463271 is a potent antagonist of the neuronal-specific potassium-chloride cotransporter 2 (KCC2), with an IC
50
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.
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 2.7- 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 a
small percentage of preparations.
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.
VU 0463271
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| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-110110 | VU 0463271
VU0463271 | 1391737-01-1 | 5mg | 900元 |
| 2024/04/30 | HY-110110 | VU0463271 | | 10 mM * 1 mLin DMSO | 990元 |
1391737-01-1, VU 0463271 相关搜索:
- N-环丙基-N-(4-甲基-2-噻唑基)-2-[(6-苯基-3-哒嗪基)硫基]乙酰胺
- 化合物VU0463271
- 化合物 T17243
- 1391737-01-1
- Inhibitor,KcsA,VU0463271,Potassium Channel,VU 0463271,VU-0463271,inhibit
- 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)
- 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)
- VU 0463271