PMX 53 acetate(219639-75-5 free base) Bioactivity,Chemical Properties,Storage & Solubility Information Pathways-PeptideDB

Description	PMX-53 is a potent and orally active CD88 (C5aR) antagonist (IC50: 20 nM) and inhibits C5a-induced neutrophil myeloperoxidase release and chemotaxis with IC50 values of 22 nM and 75 nM, respectively. PMX-53 is also an agonist of Mas-related gene 2 (MrgX2).
In vitro	在HMC-1细胞中，PMX-53（10 nM）可抑制C5a诱导的Ca2+动员，但在更高浓度（≥30 nM）时，可导致LAD2肥大细胞、CD34+细胞衍生的肥大细胞以及稳定表达MrgX2的RBL-2H3细胞发生脱颗粒作用。将Trp替换为Ala和Arg替换为dArg可以消除PMX-53在HMC-1细胞中抑制C5a诱导的Ca2+动员以及在表达MrgX2的RBL-2H3细胞中引发脱颗粒的能力[1]。
In vivo	大鼠爪部局部预处理PMX-53（60-180μg/爪），可抑制由酵母多糖、卡拉胶、脂多糖(LPS)和抗原引起的过度痛觉敏感[2]。药代动力学分析表明，口服PMX-53（3 mg/kg）给大鼠后，5分钟内可在血浆中检测到该药物，约20分钟达到峰值血药浓度，大约0.3 μM。此情况下，血浆清除半衰期约为70分钟[3]。
molecular weight	956.16
Molecular formula	C49H69N11O9
CAS	852629-88-0
Storage	keep away from moisture　\|　Powder: -20°C for 3 years \| In solvent: -80°C for 1 year
Solubility	DMSO: 125 mg/mL (139.49 mM), Sonication is recommended.
References	1. Subramanian H, et al. PMX-53 as a dual CD88 antagonist and an agonist for Mas-related gene 2 (MrgX2) in human mast cells. Mol Pharmacol. 2011 Jun;79(6):1005-13. 2. Ting E, et al. Role of complement C5a in mechanical inflammatory hypernociception: potential use of C5a receptor antagonists to control inflammatory pain. Br J Pharmacol. 2008 Mar;153(5):1043-53. 3. Holland MC, et al. Synthetic small-molecule complement inhibitors. Curr Opin Investig Drugs. 2004 Nov;5(11):1164-73. 4. Finch AM, et al. Low-molecular-weight peptidic and cyclic antagonists of the receptor for the complement factor C5a. J Med Chem. 1999 Jun 3;42(11):1965-74.

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PMX 53 acetate(219639-75-5 free base)

CAS No.: 852629-88-0