Enpatoran hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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 (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.

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.

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. Enpatoran hydrochloride exhibits high oral bioavailability (mouse 100%, rat 87%, dog 84%) following oral administration (mouse, rat and dog 1.0 mg/kg). 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).Animal Model:Female C57BL/6 mice Dosage:0.1 mg/kg and 1 mg/kg Administration:Oral gavage; administered 1 hour prior to R848 challenge Result:The TLR7/8 agonist R848 stimulated both IFN-α and IL-6 production in mice.Enpatoran hydrochloridedecreased IFN-α and IL-6 production stimulated by R848.

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Others

Other Targets

Others

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2101945-93-9

356.78

C16H16ClF3N4

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 16.67 mg/mL (46.72 mM; 超声助溶 (<60°C)

Cl.N[C@@H]1C[C@@H](CN(C1)c1ccc(C#N)c2ncccc12)C(F)(F)F

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(-20℃)

With Ice Pack

≥ 2 years