XPC-6444
目录号: PL11371 纯度: ≥99%
CAS No. :2230144-21-3
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中文名称
XPC-6444
中文别名
化合物 T13359
英文名称
XPC-6444
英文别名
XPC-6444;https://pubmed.ncbi.nlm.nih.gov/34355886/;SCHEMBL20238093;BDBM50530537;MS-29253;CHEMBL4471825;2230144-21-3;HY-128772;AKOS040740584;CS-0105108;4-[[2-[[tert-butyl(methyl)amino]methyl]-6-fluorophenyl]methylamino]-2,6-difluoro-N-(1,3-thiazol-4-yl)benzenesulfonamide;XPC 6444,XPC6444;Benzenesulfonamide, 4-[[[2-[[(1,1-dimethylethyl)methylamino]methyl]-6-fluorophenyl]methyl]amino]-2,6-difluoro-N-4-thiazolyl-
Cas No.
2230144-21-3
分子式
C22H25F3N4O2S2
分子量
498.58
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
XPC-6444 是一种高效的,亚型选择性的,CNS-渗透性的 NaV1.6 抑制剂 (对 hNaV1.6 的IC50=41 nM)。XPC-6444 也有效阻断了 NaV1.2 (IC50=125 nM)。XPC-6444 具有抗惊厥活性。
生物活性
XPC-6444 is a highly potent, isoform-selective, and CNS-penetrant Na V 1.6 inhibitor (IC 50 =41 nM for hNa V 1.6). XPC-6444 also displays potent block of Na V 1.2 (IC 50 =125 nM). XPC-6444 shows anticonvulsant activity.
性状
Solid
IC50 & Target[1][2]
IC50: 41 nM (hNaV1.6), 125 nM (hNaV1.2)
体外研究(In Vitro)
XPC-6444 shows high selectivity over NaV1.1 and NaV1.5. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
XPC-6444 exhibits good metabolic stability in human liver microsomes and hepatocytes, and low potential for MDR1 mediated efflux. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Focken T, et al. Identification of CNS-Penetrant Aryl Sulfonamides as Isoform-Selective NaV1.6 Inhibitors with Efficacy in Mouse Models of Epilepsy. J Med Chem. 2019 Oct 3.
溶解度数据
In Vitro: DMSO : 125 mg/mL (250.71 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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