2101938-42-3
2101938-42-3
Chemical Structure
Enpatoran
Synonym(s): M5049
- CAS No.: 2101938-42-3
- Formula:C16H15F3N4
- Molecular Weight:320.31
IUPAC Name: 5-((3R,5S)-3-amino-5-(trifluoromethyl)piperidin-1-yl)quinoline-8-carbonitrile
InChIKey: BJXYHBKEQFQVES-NWDGAFQWSA-N
SMILES: N#CC(C=C1)=C(N=CC=C2)C2=C1N3C[C@@H](C(F)(F)F)C[C@@H](N)C3
Biological Activity: Enpatoran (M5049) is an orally active and selective TLR7/8 antagonist. Enpatoran inhibits the activation of the downstream type I interferon pathway. Enpatoran is used in studies of cutaneous lupus erythematosus, systemic lupus erythematosus with cutaneous manifestations, and psoriasis[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Enpatoran | 99.87% | Enpatoran (M5049) is an orally active and selective TLR7/8 antagonist. Enpatoran inhibits the activation of the downstream type I interferon pathway. Enpatoran is used in studies of cutaneous lupus erythematosus, systemic lupus erythematosus with cutaneous manifestations, and psoriasis. | ||||||||||||||||||||
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Enpatoran (Standard) | ≥98% | Enpatoran (Standard) is the analytical standard of Enpatoran (HY-134581). This product is intended for research and analytical applications. Enpatoran (M5049) 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 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 . | ||||||||||||||||||||
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References
- [1]. Morand EF, et al. Efficacy and safety of enpatoran, a Toll-like receptor 7/8 inhibitor, in patients with skin manifestations of cutaneous lupus erythematosus or systemic lupus erythematosus: findings from Cohort A of a multicentre, international, double-blind, placebo-controlled, dose-finding phase 2 trial. The Lancet. Rheumatology. 2026 Jul;8(7):e513-e527.
- [2]. Gaudenzi C, et al. Psoriatic microRNAs induce NK cell activation via an innate immune crosstalk abrogated by the Toll-like receptor 7/8 antagonist Enpatoran. Journal of translational medicine. 2026 Mar 02;24(1):478.
- [3]. Vlach J, et al. Discovery of M5049: A Novel Selective Toll-Like Receptor 7/8 Inhibitor for Treatment of Autoimmunity. The Journal of pharmacology and experimental therapeutics. 2021 Mar;376(3):397-409. [Content Brief]
