目錄:MedChemExpress LLC>>信號通路>> Enpatoran | MCE
CAS | 2101938-42-3 | 純度 | 99.77% |
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分子量 | 320.31 | 分子式 | C??H??F?N? |
供貨周期 | 現(xiàn)貨 | 規(guī)格 | 5 mg |
貨號 | HY-134581 | 應用領域 | 醫(yī)療衛(wèi)生,化工,生物產業(yè),制藥 |
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產品活性:Enpatoran (M5049) 是一種有效的、具有口服活性的 TLR7/8 抑制劑,在HEK293 細胞中,其IC50s 分別為 11.1 nM 和 24.1 nM。Enpatoran 對 TLR3, TLR4 和 TLR9 無活性。Enpatoran 可以阻斷分子合成配體和天然內源性 RNA 配體。Enpatoran 在體內的表現(xiàn)出良好的藥代動力學特性。Enpatoran 可用于先天性和適應性自身免疫阻斷的相關研究。
研究領域:Immunology/Inflammation
作用靶點:Toll-like Receptor (TLR)
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.
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).
相關產品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Immunology/Inflammation Compound Library | Clinical Compound Library | Antiviral Compound Library | Small Molecule Immuno-Oncology Compound Library | Drug Repurposing Compound Library | Antioxidant Compound Library | Differentiation Inducing Compound Library | Oxygen Sensing Compound Library | Pyroptosis Compound Library | Orally Active Compound Library | Heterocyclic Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | C29 | ODN 1018 | TLR7 agonist 5 | AN-3485 | ODN 2088 | TLR4/NF-κB/MAPK-IN-1 | TLR9-IN-1 | ODN 105871 | MC-Val-Cit-PAB-Amide-TLR7 agonist 4 | Monophosphoryl lipid A | β-D-Glucan | Poly (I:C):Kanamycin (1:1) (sodium) | ODN TTAGGG | Bropirimine | Polygalasaponin F | Chloroquine-d5 (diphosphate) | DB-3-291 | ODN 24888 | ODN 2216 | Agatolimod | Enpatoran hydrochloride | BBIQ | UC-1V150 | AZD8848 | ODN 105870 | CU-T12-9 | TLR7/8 agonist 7 | ODN 21158 | TH1020 | Lefitolimod
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