A-205804

SKU: orb1223174

Description

A-205804 is a specific and effective inhibitor of E-selectin( IC50=20 nM ) and ICAM-1(IC50=25 nM) expression.

Key Properties

• CAS Number: 251992-66-2
• MW: 300.41
• Purity: >98% (HPLC)
• Formula: C₁₅H₁₂N₂OS₂
• SMILES: Cc1ccc(cc1)Sc1c2cc(sc2cnc1)C(=O)N
• Target: Sigma receptor
• Solubility: In Vitro: DMSO : 100 mg/mL (332.89 mM)

Bioactivity

• In Vivo:
  A-205804 (5 mg/kg; p.o.) shows a half-life of 1 hour for rat. A-205804 (10 mg/kg; p.o. ; 3 times per week; for 2 weeks) attenuates the E-selectin expression on the endothelial vascular niche cells in mice. Animal model: C57BL/6 mice. Dosage: 10 mg/kg. Administration: Oral administration, 3 times per week, for 2 weeks. Result: Efficiently decreased the expression of E-selectin on the endothelial vascular niche cells. Animal model: Rat. Dosage: 5 mg/kg (Pharmacokinetic Analysis). Administration: Oral administration. Result: t1/2 = 1 hour.
• In Vitro:
  A-205804 exhibits Cellular Toxicities for HUVEC with an IC50 of152 μM. A-205804 is an effective inhibitor of cell-cell adhesion in an in vitro flow experiment, demonstrating relevance in a model physiological system.

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

Sigma receptor