TY-52156

SKU: orb1219719

Description

TY-52156 is an effective and selective S1P3 receptor antagonist (Ki: 110 nM). TY-52156 displays submicromolar potency and a high degree of selectivity for the S1P3 receptor. TY-52156 inhibits the S1P3 receptor-dependent increase in [Ca2+]i. TY-52156 (10 μM; 10 min) inhibits S1P-induced p44/p42 MAPK phosphorylation.After oral administration in vivo, TY-52156 (10 mg/kg, 30 mg/kg; p.o.) inhibits S1P3 receptor-induced bradycardia.

Key Properties

• CAS Number: 934369-14-9
• MW: 364.27
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₉Cl₂N₃O
• SMILES: CC(C)(C)C(=O)C(\NNc1ccc(Cl)cc1)=N\c1ccc(Cl)cc1
• Target: S1P Receptor
• Solubility: DMSO:100 mg/mL (274.52 mM)

Bioactivity

• In Vivo:
  Animal model: Male SD rats (290–340 g). Dosage: 10 mg/kg, 30 mg/kg. Administration: Oral administration. Result: Inhibited S1P3 receptor-induced bradycardia after oral administration In vivo.
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• In Vitro:
  Western blot analysis. Cell line: Chinese hamster ovary K1 cells. Concentration: 10 μM. Incubation time: 10 min. Result: Inhibited S1P-induced p44/p42 MAPK phosphorylation.
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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

S1P Receptor