BI-671800

SKU: orb1219114

Description

BI-671800 is a highly specific and potent antagonist of chemoattractant receptor-homologous molecule on Th2 cells (DP2/CRTH2). With IC50 values of 4.5 nM and 3.7 nM for PGD2 binding to CRTH2 in hCRTH2 and mCRTH2 transfected cells, respectively. BI-671800 has potential for the treatment of poorly controlled asthma.

Key Properties

• CAS Number: 1093108-50-9
• MW: 501.5
• Purity: >98% (HPLC)
• Formula: C₂₅H₂₆F₃N₅O₃
• SMILES: CN(C)c1nc(Cc(cc2)ccc2NC(c2ccc(C(F)(F)F)cc2)=O)nc(N(C)C)c1CC(O)=O
• Target: GPR
• Solubility: DMSO:130 mg/mL (259.22 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  BI-671800 (compound A, 0.1-10 mg/kg, i. g.) shows significant inhibition of AHR in mice. BI-671800 (compound A), effectively blocks edema formation and greatly reduces the inflammatory infiltrate and skin pathology observed in drug vehicle-treated animals. Animal model: 6-8-week-old age-and sex-matched BALB/c mice (mice were sensitized for 14 days, challenged intranasally). Dosage: 10-0.1 mg/kg. Administration: Oral gavage for 4 weeks. Result: Shows significant inhibition of AHR in mice.
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• In Vitro:
  BI-671800 (compound A) exhibits low nM potency as an antagonist of human or mouse CRTH2 in transfected cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AP-761 | Cmpd A

Quick Database Links

Gene Symbol

GPR