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Enpatoran (M5049) hydrochloride 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 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 In Vitro 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 IC 50 values ranging from 35 to 45 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 hydrochloride decreased IFN-α and IL-6 production stimulated by R848. Form:Solid IC50& Target:TLR7 11.1 nM (IC 50 ) TLR8 24.1 nM (IC 50 )
中文名称
Enpatoran hydrochloride
英文名称
Enpatoran hydrochloride
中文别名
盐酸恩帕托兰
英文别名
-
CAS号
2101945-93-9
分子式
C16H16ClF3N4
分子量
356.77 g/mol
精确质量
≥98%
PSA
-
Logp
-
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Enpatoran hydrochloride 10mM in DMSO 1ml

源叶 Enpatoran hydrochloride 10mM in DMSO 1ml,2101945-93-9,规格齐全,生产科研实验检测,科学材料数智化一站式易购平台。

品牌:源叶
货号:T96948-1ml
级别: -
货期:30天
已售 579 件
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