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Enpatoran hydrochloride Sale

(Synonyms: M5049 hydrochloride) 目录号 : GC62471

Enpatoran (M5049) hydrochloride 是一种有效的、具有口服活性的 TLR7/8 抑制剂,在HEK293 细胞中,其IC50s 分别为 11.1 nM 和 24.1 nM。Enpatoran hydrochloride 对 TLR3, TLR4 和 TLR9 无活性。Enpatoran hydrochloride 可以阻断分子合成配体和天然内源性 RNA 配体。Enpatoran hydrochloride 在体内的表现出良好的药代动力学特性。Enpatoran hydrochloride 可用于先天性和适应性自身免疫阻断的相关研究。

Enpatoran hydrochloride Chemical Structure

Cas No.:2101945-93-9

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥3,960.00
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5 mg
¥3,600.00
现货
10 mg
¥6,120.00
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25 mg
¥12,150.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

Enpatoran (M5049) hydrochloride is a potent, orally active and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran hydrochloride is inactive against TLR3, TLR4 and TLR9. Enpatoran hydrochloride can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran hydrochloride exhibits excellent pharmacokinetic properties in vivo. Enpatoran hydrochloride can be used for both innate and adaptive autoimmunity blocking research[1].

Enpatoran hydrochloride (0.01 nM-10 μM) inhibits production of IL-6 stimulated by all the ligands (miR-122, Let7c RNA, Alu RNA, and R848) with IC50 values ranging from 35 to 45 nM[1].

Pre-treatment with Enpatoran hydrochloride (oral gavage; 1 mg/kg) before R848 (intraperitoneal injection of 25 µg) dose-dependently inhibits the production of IL-6 and IFN-α in mice[1]. Enpatoran hydrochloride exhibits high oral bioavailability (mouse 100%, rat 87%, dog 84%) following oral administration (mouse, rat and dog 1.0 mg/kg)[1]. Enpatoran hydrochloride exhibits moderate half-lives (mouse 1.4, rat 5.0 and dog 13 h) due to high plasma clearance (1.4, 1.2 and 0.59 L/h/kg, respectively) combined with large volumes of distribution (2.7, 8.7 and 5.7 L/kg, respectively) following intravenous administration (mouse, rat and dog 1.0 mg/kg)[1].

[1]. Jaromir Vlach, et al. Discovery of M5049: A Novel Selective TLR7/8 Inhibitor for Treatment of Autoimmunity. J Pharmacol Exp Ther. 2020 Dec 16;JPET-AR-2020-000275.

Chemical Properties

Cas No. 2101945-93-9 SDF
别名 M5049 hydrochloride
分子式 C16H16ClF3N4 分子量 356.77
溶解度 DMSO : 16.67 mg/mL (46.72 mM; ultrasonic and warming and heat to 60°C) 储存条件 Store at -20°C, sealed storage, away from moisture and light
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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1 mg 5 mg 10 mg
1 mM 2.8029 mL 14.0146 mL 28.0293 mL
5 mM 0.5606 mL 2.8029 mL 5.6059 mL
10 mM 0.2803 mL 1.4015 mL 2.8029 mL
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