KJM429  (Synonyms: MK-056)

KJM429 (MK-056) is a high-affinity ligand for the rat vanilloid receptor rTRPV1 (K_i=30-63 nM) with a unique dual regulatory function. KJM429 acts as a competitive antagonist to inhibit TRPV1 receptor activation induced by Capsaicin (HY-10448), resiniferatoxin, thermal stimulation and weak acid (pH 6.0), and switches to a TRPV1 agonist under strong acid conditions (pH<5.5). KJM429 effectively blocks calcium influx induced by Capsaicin and partial thermal stimulation, and triggers calcium uptake under low pH conditions, with minimal effects on non-TRPV1-mediated calcium signaling. KJM429 can be used for research on the mechanisms of pain-related diseases such as postherpetic neuralgia, diabetic neuropathy, cluster headache, osteoarthritis and pruritus^[1].

KJM429 inhibits Capsaicin (HY-10448)- and Resiniferatoxin (HY-N2333)-induced calcium uptake in Chinese hamster ovary cells expressing rTRPV1, with a K_i of 53.9 nM and 30.4 nM, respectively^[1].
KJM429 (50-400 nM; 5 min) acts as a competitive antagonist of rTRPV1 in Chinese hamster ovary cells, with a K_i value of 31.2 nM against Capsaicin and 35.2 nM against Resiniferatoxin^[1].
KJM429 (0.3-3000 nM; 5 min) partially inhibits heat-induced calcium uptake in Chinese hamster ovary cells expressing rTRPV1, reducing the uptake by 65.4% at 3000 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

405.58

C₂₀H₂₇N₃O₂S₂

401907-57-1

O=S(=O)(NC1=CC=C(C=C1)CNC(=S)NCC2=CC=C(C=C2)C(C)(C)C)C

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Wang Y, et al. High affinity antagonists of the vanilloid receptor. Mol Pharmacol. 2002;62(4):947-956.  [Content Brief]