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PMX 53
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CAS NO:219639-75-5
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
1mg电议
5mg电议
10mg电议

产品介绍
PMX 53 (3D53) 是一种合成肽类,是一种有效且具有口服活性的补体 C5a 受体 (CD88) 拮抗剂,IC50 为 20 nM。
Cas No.219639-75-5
别名3D53
Canonical SMILESNC(=NCCCC1NC(=O)C(NC(=O)C(CC2CCCCC2)NC(=O)C2N(C(=O)C(CCCNC1=O)NC(=O)C(Cc1ccccc1)NC(=O)C)CCC2)Cc1c[nH]c2c1cccc2)N
分子式C47H65N11O7
分子量896.1
溶解度Soluble in DMSO
储存条件Store at -20°C, protect from light, stored under nitrogen
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Potent C5a receptor antagonist (IC50 = 20 nM). Also MrgX2 agonist. Stimulates MrgX2-mediated mast cell degranulation. Also inhibits C5a-induced hypernociception in rats, inhibits lung metastasis in a mouse breast cancer model and reduces atherosclerotic lesions in a mouse model of atherosclerosis. Negative Control also available.

Ting et al (2008) Role of complement C5a in mechanical inflammatory hypernociception: potential use of C5a receptor antagonists to control inflammatory pain. Br.J.Pharmacol. 153 1043 PMID:18084313 |Subramanian et al (2011) PMX-53 as a dual CD88 antagonist and an agonist for Mas-related gene 2 (MrgX2) in human mast cells. Mol.Pharmacol. 79 1005 PMID:21441599 |Finch et al (1999) Low-molecular-weight peptidic and cyclic antagonists of the receptor for the complement factor C5a. J.Med.Chem. 42 1965 PMID:10354404 |Vadrevu et al (2014) Complement c5a receptor facilitates cancer metastasis by altering T-cell responses in the metastatic niche. Cancer Res. 74 3454 PMID:24786787 |Manthey et al (2011) Complement C5a inhibition reduces atherosclerosis in ApoE-/- mice. FASEB J 25 2447 PMID:21490292 |Kumar et al (2018) Development and validation of a LC-MS/MS assay for pharmacokinetic studies of complement C5a receptor antagonists PMX53 and PMX205 in mice. Sci.Rep. 8 8101 PMID:29802264