3075832-16-2
Chemical Structure
INCB187175
- CAS No.: 3075832-16-2
- Formula:C23H21F7N6O2
- Molecular Weight:546.44
InChIKey: HSXGQRNXTOKOHH-SHTZXODSSA-N
SMILES: FC(C=C1)=CC=C1C2(CN(C(N[C@@H]3C[C@@H](O)C3)=O)C2)CNC4=CC(C(F)(F)F)=NC5=CC(C(F)(F)F)=NN54
Biological Activity: INCB187175 is an orally active MRGPRX2 antagonist that blocks Gq signaling and β-arrestin recruitment. INCB187175 inhibits MRGPRX2-mediated mast cell degranulation and suppresses agonist-evoked vascular leakage in human MRGPRX2 knock-in mouse models without broadly inhibiting IgE-mediated mast cell activation. INCB187175 shows minimal inhibition of major cytochrome P450 (Cytochrome P450) isoforms and has a low hERG risk[1]. INCB187175 can be used for research on mast cell-mediated diseases[1].
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INCB187175 | INCB187175 is an orally active MRGPRX2 antagonist that blocks Gq signaling and β-arrestin recruitment. INCB187175 inhibits MRGPRX2-mediated mast cell degranulation and suppresses agonist-evoked vascular leakage in human MRGPRX2 knock-in mouse models without broadly inhibiting IgE-mediated mast cell activation. INCB187175 shows minimal inhibition of major cytochrome P450 (Cytochrome P450) isoforms and has a low hERG risk. INCB187175 can be used for research on mast cell-mediated diseases. | |||||||||||||||||||||
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