CID 2745687

SKU: orb1218250

Description

CID 2745687 is a GPR35 antagonist that inhibited the effects at human GPR35 of cromolyn disodium and zaprinast, two agonists that share an overlapping binding site.

Key Properties

• CAS Number: 264233-05-8
• MW: 395.43
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₉F₂N₅O₂S
• SMILES: O=C(C1=C(C=NNC(NC(C)(C)C)=S)N(C2=CC=C(F)C=C2F)N=C1)OC
• Target: GPR
• Solubility: In Vitro: DMSO : 125 mg/mL (316.11 mM)

Bioactivity

• In Vivo:
  CID 2745687 (CID2745687; 1 mg/kg; administrated orally every day for the last 4 weeks), a specific GPR35 antagonist, reverses Lodoxamide-mediated anti-fibrotic effects. Animal model: Six-week-old male C57BL/6 mice. Dosage: 1 mg/kg. Administration: Oral administration, every day for 4 weeks. Result: Inhibited Lodoxamide-mediated protective effects.
• In Vitro:
  For ERK1/2 phosphorylation with 1 μM Pamoic acid as the agonist, the CID 2745687 (CID2745687) Ki is 18 nM. CID 2745687 (CID-2745687) is a potent antagonist in β-arrestin-2 interaction assays only at human GPR35.Using the BRET-based GPR35-β-arrestin-2 interaction assay and an EC80 concentration of Zaprinast (20 μM) as agonist, CID 2745687 behaved as a moderately potent, concentration-dependent antagonist at human GPR35 with pIC50=6.70±0.09.CID 2745687 (pIC50=6.27±0.08) fully reverses the agonist action of Cromolyn disodium.

Storage & Handling

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

Quick Database Links

Gene Symbol

GPR