| Name | Enpatoran hydrochloride |
| Description | Enpatoran hydrochloride (M5049 hydrochloride) is an orally active, selective, and potent TLR7/8 inhibitor with antiviral activity for the study of autoimmune diseases and COVID-19 pneumonia. |
| In vitro | 0.01 nM-10 μM Enpatoran hydrochloride, was able to inhibit IL-6 production induced by all ligands (e.g., miR-122, Let7c RNA, Alu RNA, and R848) with IC50 values ranging from 35 to 45 nM. [1] |
| In vivo | Injection of R848 (25 μg intraperitoneally) into mice was able to dose-dependently inhibit IL-6 and IFN-α production after pretreatment with 1 mg/kg Enpatoran hydrochloride by oral gavage.
Enpatoran hydrochloride exhibited good bioavailability after oral administration of 1.0 mg/kg (100% in mice, 87% in rats, and 84% in dogs). Following intravenous administration, Enpatoran hydrochloride has a moderate half-life (1.4 hours in mice, 5.0 hours in rats, and 13 hours in dogs), which is associated with its high plasma clearance (1.4 L/h/kg in mice, 1.2 L/h/kg in rats, and 0.59 L/h/kg in dogs, respectively) and large volume of distribution (2.7 L/kg in mice, 8.7 L/kg in rats, and 8.7 L/kg in dogs, respectively). /in mice, 8.7 L/kg in rats, and 5.7 L/kg in dogs, respectively). [1] |
| Storage | keep away from moisture,keep away from direct sunlight,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 10.00 mg/mL (28.03 mM), Sonication is recommended.
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| Keywords | TLR8 | TLR7 | Antiviral |
| Inhibitors Related | BTA-188 | Hydroxychloroquine | Chloroquine phosphate | Oxytetracycline Hydrochloride | Chloranil | Chloroquine | CU-115 | Valganciclovir hydrochloride | Imiquimod | TLR3-IN-1 | Resiquimod | Stevioside |
| Related Compound Libraries | Bioactive Compound Library | Anti-Alzheimer's Disease Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max |
United States
