A selective TRPA1 blocker that antagonizes TRPA1-mediated calcium influx induced by allyl isothiocyanate and 4-hydroxy nonenal (IC50s = 14.3 and 18.7 μM

TCS 5861528 – 50 mg

Brand:
Cayman
CAS:
332117-28-9
Storage:
-20
UN-No:
Non-Hazardous - /

The transient receptor potential ankyrin 1 (TRPA1) ion channel integrates the nociception and transmission of diverse, potentially damaging and noxious stimuli, including cold, electrophilic compounds, divalent cations, and mechanical stimulation. TCS 5861528 is a selective TRPA1 blocker that antagonizes TRPA1-mediated calcium influx induced by allyl isothiocyanate and 4-hydroxy nonenal (Item No. 32100) with IC50 values of 14.3 and 18.7 μM, respectively.{29617,22996} At 30 mg/kg twice daily in rats, TCS 5861528 has been used to attenuate pain-related behavior in models of diabetic hypersensitivity and postoperative pain.{29617,24757}  

 

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Description

A selective TRPA1 blocker that antagonizes TRPA1-mediated calcium influx induced by allyl isothiocyanate and 4-hydroxy nonenal (IC50s = 14.3 and 18.7 μM, respectively); 30 mg/kg twice daily in rats attenuates pain-related behavior in models of diabetic hypersensitivity and postoperative pain

Formal name: 1,2,3,6-tetrahydro-1,3-dimethyl-N-[4-(1-methylpropyl)phenyl]-2,6-dioxo-7H-purine-7-acetamide

Synonyms: 

Molecular weight: 369.4

CAS: 332117-28-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Neuroscience|Pain Research

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