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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.1,2 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.1,3
WARNING This product is not for human or veterinary use.
1. Attenuation of the mechanical hypersensitivity by an antagonist of the TRPA1 ion channel in diabetic animals. Anesthesiology 111, 147-154 (2009).
2. TRPA1 as an analgesic target. Open Drug Discov.J. 2, 64-70 (2010).
3. Transient receptor potential ankyrin 1 ion channel contributes to guarding pain and mechanical hypersensitivity in a rat model of postoperative pain. Anesthesiology 117(1), 137-148 (2012).