Vimirogant hydrochloride||(VTP-43742 hydrochloride)-陌孚医药/Medlife

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Vimirogant hydrochloride (Synonyms: VTP-43742 hydrochloride)

目录号: PL11083 纯度: ≥98%

商品编号	规格	价格	会员价
PL11083-1mg	1mg	¥12777.00	请登录
PL11083-5mg	5mg	¥28127.00	请登录
PL11083-10mg	10mg	¥45003.00	请登录
PL11083-50mg	50mg	询价	询价
PL11083-100mg	100mg	询价	询价

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中文名称	Vimirogant hydrochloride
英文名称	Vimirogant hydrochloride
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Vimirogant (VTP-43742) hydrochloride 是一种选择性、具有口服活性的的 RORγt 抑制剂 (K_i=3.5 nM; IC₅₀=17 nM)。Vimirogant hydrochloride 与 RORα 和 RORβ 比，高出 >1000 倍的选择性。Vimirogant hydrochloride 抑制小鼠脾细胞的 Th17 分化和 IL-17A 分泌 (IC₅₀=57 nM)，而不会影响 Th1，Th2 或 Treg 细胞的分化。Vimirogant hydrochloride可用于研究自身免疫性疾病研究。

生物活性

Vimirogant (VTP-43742) hydrochloride is a potent, selective, and orally active RORγt inhibitor (K i =3.5 nM; IC 50 =17 nM). Vimirogant hydrochloride exhibits >1000-fold selectivity versus the RORα and RORβ isotypes. Vimirogant hydrochloride inhibits Th17 differentiation and IL-17A secretion from mouse splenocytes (IC 50 =57 nM) without affecting Th1, Th2, or Treg cell differentiation. Vimirogant hydrochloride has the potential for autoimmune disorders research.

性状

Solid

IC50 & Target[1][2]

RORγt 3.5 nM (Ki) RORγt 17 nM (IC50)

体外研究(In Vitro)

Vimirogant hydrochloride inhibits the secretion of IL-17A from activated hPBMCs (IC50=18 nM) and human whole blood (IC50=192 nM). has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

In the MOG35-55/CFA immunized mouse EAE model, Vimirogant hydrochloride (p.o.) significantly suppresses clinical symptoms, demyelination and mRNA expression of multiple inflammatory markers in the spinal cord. 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

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Gege C. RORγt inhibitors as potential back-ups for the phase II candidate VTP-43742 from Vitae Pharmaceuticals: patent evaluation of WO2016061160 and US20160122345. Expert Opin Ther Pat. 2017;27(1):1-8.
[2]. Gerard McGeehan, et al. VTP-43742 is a potent and selective RORγt blocker that demonstrates oral efficacy in a mouse model of autoimmunity through suppression of IL-17A production (THER7P.945). J Immunol May 1, 2015, 194 (1 Supplement) 208.5-208.5.

溶解度数据	In Vitro: DMSO : 125 mg/mL (Need ultrasonic)Ethanol : 50 mg/mL (Need ultrasonic)In Vivo:

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产品使用指南

Data Sheet

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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