ZINC-3573 is a potent and highly selective MRGPRX2 probe. The MRGPRX2-activating opioids and ZINC-3573 induced intracellular Ca2+ release and degranulation in a human mast cell line. ZINC-3573 activates endogenous MRGPRX2 in a human mast cell line, inducing degranulation and calcium release. MRGPRX2 is a unique atypical opioid-like receptor important for modulating mast cell degranulation, which can now be specifically modulated with ZINC-3573. References: Lansu K, Karpiak J, Liu J, Huang XP, McCorvy JD, Kroeze WK, Che T, Nagase H, Carroll FI, Jin J, Shoichet BK, Roth BL. In silico design of novel probes for the atypical opioid receptor MRGPRX2. Nat Chem Biol. 2017 May;13(5):529-536. doi: 10.1038/nchembio.2334. Epub 2017 Mar 13. PubMed PMID: 28288109; PubMed Central PMCID: PMC5391270.
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CAS:2089389-15-9