TCS 5861528

SKU: orb1223147

Description

TCS-5861528, also known as Chembridge-5861528, is a TRPA1 receptor antagonist. TCS-5861528 antagonizes AITC- and 4-HNE-evoked calcium influx (IC50 values are 14.3 and 18.7μM respectively). TRPA1 was found to mediate acute inflammation and the development of degenerative cartilage changes and joint pain in MIA-induced experimental OA in the mouse. TRPA1 may be a potential mediator and drug target in OA.

Key Properties

• CAS Number: 332117-28-9
• MW: 369.42
• Purity: >98% (HPLC)
• Formula: C₁₉H₂₃N₅O₃
• SMILES: CCC(C)c1ccc(NC(=O)Cn2cnc3c2c(=O)n(C)c(=O)n3C)cc1
• Target: Arginase
• Solubility: DMSO : 74 mg/mL. 200.31 mM

Bioactivity

• In Vivo:
  Chembridge-5861528 (TCS 5861528) (30 mg/kg; i.p.; twice daily for a week) significantly attenuates development of mechanical hypersensitivity in Streptozocin (HY-13753)-induced diabetes mellitus rat model. Chembridge-5861528 (3 and 10 μg/rat; i. t. ; once) attenuates Capsaicin (HY-10448)-induced blood flow increase in a dose-related fashion. Animal model: Male Hannover-Wistar rats, Streptozocin-induced diabetes mellitus model. Dosage: 30 mg/kg. Administration: Intraperitoneal injection, twice daily for a week. Result: Significantly attenuated development of mechanical hypersensitivity as revealed by the paw pressure test (F1, 80 = 31.4, P < 0.0001). Animal model: Male Hannover–Wistar rats (220-260 g), Capsaicin-induced neurogenic inflammation model. Dosage: 0, 3, and 10 μg/rat. Administration: Intrathecal injection, 20 min before Capsaicin injection. Result: Significantly decreased the blood flow at 10 μg.
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• In Vitro:
  Chembridge-5861528 (TCS 5861528) shows no TRPA1 or TRPV1 channel agonism and no TRPV1 channel antagonism up to a dose of 100 μM.

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

TCS5861528, TCS-5861528

Quick Database Links

Gene Symbol

Arginase