1. GPCR/G Protein
  2. Prostaglandin Receptor

CRTH2-IN-1 (Synonyms: Ramatroban analog)

Cat. No.: HY-U00423
Handling Instructions

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.

For research use only. We do not sell to patients.

CRTH2-IN-1 Chemical Structure

CRTH2-IN-1 Chemical Structure

CAS No. : 926661-54-3

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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

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.

IC50 & Target[1]

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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4011 mL 12.0057 mL 24.0113 mL
5 mM 0.4802 mL 2.4011 mL 4.8023 mL
10 mM 0.2401 mL 1.2006 mL 2.4011 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

416.47

Formula

C₂₁H₂₁FN₂O₄S

CAS No.

926661-54-3

SMILES

O=C(O)CC1=C(CCC(N(S(=O)(C2=CC=C(F)C=C2)=O)C)C3)N3C4=C1C=CC=C4

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
CRTH2-IN-1
Cat. No.:
HY-U00423
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CRTH2-IN-1

Cat. No.: HY-U00423