| Bioactivity | MS47134 is a potent and selective MRGPRX4 agonist with an EC50 value of 149 nM. MS47134 can be used for research of pain, itch and mast cell-mediated hypersensitivity[1]. | ||||||||||||
| Target | EC50: 149 nM (MRGPRX4) | ||||||||||||
| Invitro | MS47134 exhibits increased potency as a MRGPRX4 agonist in the FLIPR Ca2+ assay compared with Nateglinide (HY-B0422)[1].MS47134 (0.001 nM-0.1 mM) shows 47-fold improved selectivity for MRGPRX4 over the Kir6.2/SUR1 potassium channel[1].The MRGPRX family of receptors (MRGPRX1-4) is a family of mas-related G-protein-coupled receptors that have evolved relatively recently. MRGPRX2 and MRGPRX4 are key physiological and pathological mediators of itch and related mast cell-mediated hypersensitivity reactions[1]. | ||||||||||||
| Name | MS47134 | ||||||||||||
| Formula | C22H29NO3 | ||||||||||||
| Molar Mass | 355.47 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Cao C, et al. Structure, function and pharmacology of human itch GPCRs. Nature. 2021 Dec;600(7887):170-175. |