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.
Product information
CAS Number: 926661-54-3
Molecular Weight: 416.47
Formula: C21H21FN2O4S
Chemical Name: 2-[7-(N-methyl4-fluorobenzenesulfonamido)-6H,7H,8H,9H-pyrido[1,2-a]indol-10-yl]acetic acid
Smiles: CN(C1CN2C3C=CC=CC=3C(CC(O)=O)=C2CC1)S(=O)(=O)C1C=CC(F)=CC=1
InChiKey: JTCAGRAKUAAYDY-UHFFFAOYSA-N
InChi: InChI=1S/C21H21FN2O4S/c1-23(29(27,28)16-9-6-14(22)7-10-16)15-8-11-20-18(12-21(25)26)17-4-2-3-5-19(17)24(20)13-15/h2-7,9-10,15H,8,11-13H2,1H3,(H,25,26)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
Products are for research use only. Not for human use.
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