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Enpatoran hydrochloride

Catalog No. T37287 CAS 2101945-93-9

Enpatoran (M5049) hydrochloride is a potent and orally active dual inhibitor of TLR7/8 with IC50 values of 11.1 nM and 24.1 nM in HEK293 cells, respectively. This compound specifically inhibits TLR7 and TLR8, while showing no activity against TLR3, TLR4, and TLR9. Enpatoran hydrochloride has the ability to block both synthetic molecule ligands and natural endogenous RNA ligands. Additionally, it demonstrates excellent pharmacokinetic properties in vivo. Enpatoran hydrochloride can be a valuable tool for studying and modulating both innate and adaptive autoimmunity. [1]

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Enpatoran hydrochloride Chemical Structure

Enpatoran hydrochloride, CAS 2101945-93-9

Pack Size	Availability	Price/USD
2 mg	5 days	$ 177.00
5 mg	5 days	$ 297.00
1 mL * 10 mM (in DMSO)	5 days	$ 296.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	Enpatoran (M5049) hydrochloride is a potent and orally active dual inhibitor of TLR7/8 with IC50 values of 11.1 nM and 24.1 nM in HEK293 cells, respectively. This compound specifically inhibits TLR7 and TLR8, while showing no activity against TLR3, TLR4, and TLR9. Enpatoran hydrochloride has the ability to block both synthetic molecule ligands and natural endogenous RNA ligands. Additionally, it demonstrates excellent pharmacokinetic properties in vivo. Enpatoran hydrochloride can be a valuable tool for studying and modulating both innate and adaptive autoimmunity. [1]
Targets&IC50	TLR8:24.1 nM (IC50), TLR7:11.1 nM (IC50)
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 IC50 values ranging from 35 to 45 nM[1].
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[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].

Molecular Weight	356.78
Formula	C16H16ClF3N4
CAS No.	2101945-93-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 16.67 mg/mL (46.72 mM), Sonication and heating to 60℃ are recommended.

References and Literature

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.

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Keywords

Enpatoran hydrochloride 2101945-93-9 Enpatoran Hydrochloride inhibitor inhibit

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