Enpatoran|2101938-42-3|(M5049)-陌孚医药/Medlife

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Enpatoran (Synonyms: M5049)

目录号: PL12322 纯度: ≥99%

CAS No. :2101938-42-3

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中文名称	Enpatoran
英文名称	Enpatoran
英文别名	7CZ390V26X;5-[(3~{R},5~{S})-3-azanyl-5-(trifluoromethyl)piperidin-1-yl]quinoline-8-carbonitrile;Enpatoran;Enpatoran [INN];enpatoran (proposed INN);GTPL11307;compound 73 [WO2017106607A1];5-((3R,5S)-3-Amino-5-trifluoromethylpiperidin-1-yl)quinoline-8-carbonitrile;5-[(3R,5S)-3-amino-5-(trifluoromethyl)piperidin-1-yl]quinoline-8-carbonitrile;8-Quinolinecarbonitrile, 5-((3R,5S)-3-amino-5-(trifluoromethyl)-1-piperidinyl)-;QLH;Unii-7CZ390V26X
Cas No.	2101938-42-3
分子式	C₁₆H₁₅F₃N₄
分子量	320.31
包装储存	-20°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

产品详情

Enpatoran (M5049) 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 对 TLR3, TLR4 和 TLR9 无活性。Enpatoran 可以阻断分子合成配体和天然内源性 RNA 配体。Enpatoran 在体内的表现出良好的药代动力学特性。Enpatoran 可用于先天性和适应性自身免疫阻断的相关研究。

生物活性

Enpatoran (M5049) is a potent, orally active and dual TLR7/8 inhibitor with IC 50 s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran is inactive against TLR3, TLR4 and TLR9. Enpatoran can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran exhibits excellent pharmacokinetic properties in vivo. Enpatoran can be used for both innate and adaptive autoimmunity blocking research .

性状

Solid

IC50 & Target[1][2]

TLR7 11.1 nM (IC50, in HEK293 cells) TLR8an

体外研究(In Vitro)

Enpatoran (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. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Pre-treatment with Enpatoran (M5049; 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 (M5049) exhibits high oral bioavailability (mouse 100%, rat 87%, dog 84%) following oral administration (mouse, rat and dog 1.0 mg/kg).
Enpatoran 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). 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

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

ClinicalTrial

参考文献

[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.

溶解度数据	In Vitro: DMSO : 24.44 mg/mL (76.30 mM; Need ultrasonic)配制储备液

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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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