926661-54-3
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
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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. |
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| 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 |
| Molecular Formula | C21H21FN2O4S |
|---|---|
| Molecular Weight | 416.47 |