TCS 5861528

Research use only, not for human use.

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.

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.

Chembridge-5861528 (TCS 5861528) shows no TRPA1 or TRPV1 channel agonism and no TRPV1 channel antagonism up to a dose of 100 μM.

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.

TCS5861528, TCS-5861528

Autophagy

Arginase

TRPA1

Neurological Disease

——

332117-28-9

369.42

C19H23N5O3

>98% (HPLC)

DMSO : 74 mg/mL. 200.31 mM;

CCC(C)c1ccc(NC(=O)Cn2cnc3c2c(=O)n(C)c(=O)n3C)cc1

2-(1,3-Dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)-N-[4-(1-methylpropyl)phenyl]acetamide

(-20℃)

With Ice Pack

≥ 2 years