货号	规格	价格	上海	北京	珠海	重庆	武汉
T87724-1mg买3赠1	97.20%	￥140.00 T87724-1mg ￥140.00 现货（买3赠1）	4 4	-	-	-	-
T87724-5mg买3赠1	97.20%	￥340.00 T87724-5mg ￥340.00 现货（买3赠1）	4 4	-	-	-	-
T87724-10mg买3赠1	97.20%	￥590.00 T87724-10mg ￥590.00 现货（买3赠1）	1 1	-	-	-	-
T87724-50mg买3赠1	97.20%	￥1930.00 T87724-50mg ￥1930.00 现货（买3赠1）	2 2	-	-	-	-
T87724-100mg	97.20%	￥2830.00 T87724-100mg ￥2830.00 现货	1 1	-	-	-	-

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产品描述：

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。

靶点：

KCC2

体外研究：

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[.
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.

体内研究：

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.

参考文献：

[1]. Delpire E, et al. Further optimization of the K-Cl cotransporter KCC2 antagonist ML077: development of a highly selective and more potent in vitro probe. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4532-5.
[2]. Rui Chen, et al. Functional Coupling of K +-Cl - Cotransporter (KCC) to GABA-Gated Cl - Channels in the Central Nervous System of Drosophila melanogaster Leads to Altered Drug Sensitivities. ACS Chem Neurosci. 2019 Jun 19;10(6):2765-2776.

溶解性：

Soluble in DMSO

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.614 ml	13.072 ml	26.144 ml
5 mM	0.523 ml	2.614 ml	5.229 ml
10 mM	0.261 ml	1.307 ml	2.614 ml
50 mM	0.052 ml	0.261 ml	0.523 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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VU 0463271