1809863-68-0
1809863-68-0
Chemical Structure
ACT-774312
- CAS. Nr.: 1809863-68-0
- Formula:C18H17ClFN5O2
- Molecular Weight:389.81
InChIKey: IKOFSSXNZQZRTE-NSHDSACASA-N
SMILES: OC(CN1C2=C(C[C@H](CC2)N(C3=NC=C(Cl)C=N3)C)C4=NC(F)=CC=C41)=O
Biological Activity: ACT-774312 is a potent and selective CRTH2 antagonist with an IC50 of 4 nM. ACT-774312 blocks the activity and internalization of the CRTH2 receptor, and inhibits PGD2-induced morphological changes in eosinophils. ACT-774312 can be used in the research of nasal polyps and type 2 inflammatory diseases.[1][2]
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ACT-774312 | ACT-774312 is a potent and selective CRTH2 antagonist with an IC50 of 4 nM. ACT-774312 blocks the activity and internalization of the CRTH2 receptor, and inhibits PGD2-induced morphological changes in eosinophils. ACT-774312 can be used in the research of nasal polyps and type 2 inflammatory diseases. | |||||||||||||||||||||
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References
- [1]. Aissaoui H, et al. Design, Synthesis, and Optimization of Indole Acetic Acid Derivatives as Potent and Selective CRTH2 Receptor Antagonists: Discovery of ACT-774312. ChemMedChem. 2023;18(10):e202300007. [Content Brief]
- [2]. Géhin M, et al. Pharmacokinetics, pharmacodynamics, tolerability and prediction of clinically effective dose of ACT-774312: A novel CRTH2 antagonist. Basic Clin Pharmacol Toxicol. 2019;124(6):711-721. [Content Brief]
Keywords
