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CRTH2-IN-1

Catalog No. T10891   CAS 926661-54-3
Synonyms: Ramatroban analog

CRTH2-IN-1 is a selective prostaglandin D2 receptor DP2 (CRTH2) antagonist, a Ramatroban analog, with an IC50 of 6 nM in the human DP2 binding assay.

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CRTH2-IN-1 Chemical Structure
CRTH2-IN-1, CAS 926661-54-3
Pack Size Availability Price/USD Quantity
25 mg 8-10 weeks $ 1,820.00
50 mg 8-10 weeks $ 2,380.00
100 mg 8-10 weeks $ 3,100.00
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Biological Description
Chemical Properties
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Description CRTH2-IN-1 is a selective prostaglandin D2 receptor DP2 (CRTH2) antagonist, a Ramatroban analog, with an IC50 of 6 nM in the human DP2 binding assay.
Targets&IC50 DP2 (human):6 nM, CYP2C9:5 μM, CYP3A4:7 μM, DP1 (human):1 μM
In vitro CRTH2-IN-1 (Ramatroban analog) is a new type of prostaglandin D2 receptor DP2 (CRTH2) antagonist with IC50 of 7 nM in human whole blood eosinophil deformation assay (hESC). It has efficacy in a mouse model of allergic rhinitis. Using 3H-PGD2 and human platelet membrane for human prostaglandin D1 receptor (hDP1) binding. Human thromboxane receptor (hTP) binding was performed using human platelet membrane and 3H-SQ-29,548. HIP / 293 membrane and 3Hiloprost were used for human prostacyclin receptor (hIP) binding. CRTH2-IN-1 inhibits hDP1 binding with IC50 of 1 μM. CRTH2-IN-1 inhibits the combination of hTP and hIP with IC50 greater than 100 μM. CRTH2-IN-1 inhibits human CYP subtypes CYP3A4, CYP 2C9 and CYP2D6 with IC50 of 7, 5 and> 30 μM, respectively.
Synonyms Ramatroban analog
Molecular Weight 416.47
Formula C21H21FN2O4S
CAS No. 926661-54-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

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.

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Keywords

CRTH2-IN-1 926661-54-3 Metabolism P450 Ramatroban analog CRTH-2-IN-1 CRTH2 IN 1 CRTH2IN1 inhibitor inhibit

 

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