S1p-receptor-agonist-1

SKU: orb1223276

Description

S1p receptor agonist 1 is an S1P receptor agonist extracted from patent WO 2015039587 A1, compound example 2. Sphingosine 1-phosphate (S1P) suppresses the collagen-induced activation of human platelets via S1P4 receptor. S1P inhibits the collagen-induced human platelet activation through S1PR4 but not S1PR1.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1514888-56-2
• MW: 409.45
• Purity: >98% (HPLC)
• Formula: C₂₃H₂₄FN₃O₃
• SMILES: c1c(ccc(c1)CC(C)C)c1nc(no1)c1ccc(c(c1)F)CN1CC(C1)C(=O)O
• Target: S1P
• Solubility: DMSO : 6.8 mg/mL. 16.61 mM

Bioactivity

• In Vivo:
  Icanbelimod (oral administration; 0.01 mg/kg-1 mg/kg) at all dose is active, and only a dose of 0.01 mg/kg is required to observe a decrease in the number of peripheral blood lymphocytes by more than 50% and a decrease in the 1 mg/kg dose. Besides, this compound islymphocyte-specific, which dose not significantly alter the number of peripheral monocytes and other white blood cells in SD rats. Icanbelimod (oral administration; 3 mg/kg; 12 days)is has been proved to block lymphocyte efflux. In the development of type II collagen-induced arthritis in rat model, compound 2 is effective in inhibiting the development of joint swelling in arthritis andjoint structure destruction. Icanbelimod (oral administration; 0.3-1 mg/kg; 30 days; once daily) inhibits the development of experimental autoimmune encephalitis (EAE) as a dose-dependent manner in mice model. Animal model: Lewis rats. Dosage: 3 mg/kg. Administration: Oral administration. Result: Decreased the severity score of arthritis in the four-legged rats. Animal model: Female C57BL/6 mice. Dosage: 0.03, 0.1, and 1 mg/kg. Administration: Oral administration. Result: Decreased the severity score of EAE in MOG 35-55 induced mice.

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

S1P-agonist-1 | DC10392 | S1p receptor agonist 1

Quick Database Links

Gene Symbol

S1P