926661-54-3

926661-54-3 structure
926661-54-3 structure
  • Name: CRTH2-IN-1
  • Chemical Name: CRTH2-IN-1
  • CAS Number: 926661-54-3
  • Molecular Formula: C21H21FN2O4S
  • Molecular Weight: 416.47
  • Catalog: Signaling Pathways GPCR/G Protein Prostaglandin Receptor
  • Create Date: 2018-02-17 03:59:48
  • Modify Date: 2024-01-22 18:18:09
  • CRTH2-IN-1 (Ramatroban analog) is a selective prostaglandin D2 receptor DP2 (CRTH2) antagonist with an IC50 of 6 nM in a human DP2 binding assay.

Name CRTH2-IN-1
Description CRTH2-IN-1 (Ramatroban analog) is a selective prostaglandin D2 receptor DP2 (CRTH2) antagonist with an IC50 of 6 nM in a human DP2 binding assay.
Related Catalog
Target

CYP 2C9:5 μM (IC50)

CYP3A4:7 μM (IC50)

In Vitro CRTH2-IN-1 (Ramatroban analog, Compound 5) is a novel prostaglandin D2 receptor DP2 (CRTH2) antagonist with an IC50 of 7 nM in a human whole blood eosinophil shape change assay (hESC). CRTH2-IN-1 (Ramatroban analog) is a novel tricyclic antagonist of the prostaglandin D2 receptor DP2 (CRTH2) with efficacy in a murine model of allergic rhinitis. Human prostaglandin D1 receptor (hDP1) binding is performed using 3H-PGD2 and human platelet membranes. Human thromboxane receptor (hTP) binding performed using human platelet membranes and 3H-SQ-29,548. Human prostacyclin receptor (hIP) binding perfomed using hIP/293 membranes and 3Hiloprost. CRTH2-IN-1 inhibits hDP1 binding with an IC50 of 1μM. CRTH2-IN-1 inhibits hTP and hIP binding with IC50s of >100 μM. CRTH2-IN-1 inhibits human CYP isoforms CYP3A4, CYP 2C9 and CYP2D6 with IC50s of 7, 5 and >30 μM, respectively[1].
References

[1]. Stearns BA, et al. Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine modelof allergic rhinitis. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4647-51.

Molecular Formula C21H21FN2O4S
Molecular Weight 416.47