TCS 5861528

CAS No. 332117-28-9

TCS 5861528( TCS5861528, TCS-5861528 )

Catalog No. M17484 CAS No. 332117-28-9

TCS5861528 is a TRPA1 channel blocker that antagonizes AITC- and 4-HNE-evoked calcium influx with IC50 values of 14.3 and 18.7 μM, respectively.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    TCS 5861528
  • Note
    Research use only, not for human use.
  • Brief Description
    TCS5861528 is a TRPA1 channel blocker that antagonizes AITC- and 4-HNE-evoked calcium influx with IC50 values of 14.3 and 18.7 μM, respectively.
  • 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.
  • 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.
  • 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.
  • Synonyms
    TCS5861528, TCS-5861528
  • Pathway
    Autophagy
  • Target
    Arginase
  • Recptor
    TRPA1
  • Research Area
    Neurological Disease
  • Indication
    ——

Chemical Information

  • CAS Number
    332117-28-9
  • Formula Weight
    369.42
  • Molecular Formula
    C19H23N5O3
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : 74 mg/mL. 200.31 mM;
  • SMILES
    CCC(C)c1ccc(NC(=O)Cn2cnc3c2c(=O)n(C)c(=O)n3C)cc1
  • Chemical Name
    2-(1,3-Dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)-N-[4-(1-methylpropyl)phenyl]acetamide

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Wei H, et al. Anesthesiology. 2009 Jul;111(1):147-54.
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