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Submit ReviewPMX 53
说明： Potent C5a receptor antagonist
纯度： ≥95% (HPLC)
生物活性 for PMX 53
PMX 53 is a 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.
技术数据 for PMX 53
| 分子量 | 896.1 |
| 公式 | C47H65N11O7 |
| 序列 |
FXPXWR (Modifications: Phe-1 = N-terminal Ac, X-2 = Orn, X-4 = D-Cha, Lactam bridge: Orn-2 to Arg-6) |
| 储存 | Store at -20°C |
| 纯度 | ≥95% (HPLC) |
| CAS Number | 219639-75-5 |
| PubChem ID | 23526550 |
| InChI Key | YOKBGCTZYPOSQM-UHFFFAOYSA-N |
| Smiles | NC(=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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for PMX 53
| 溶解性 | Soluble to 2 mg/ml in water |
产品说明书 for PMX 53
参考文献 for PMX 53
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for PMX 53, please let us know.
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关键词: PMX 53, PMX 53 supplier, PMX53, potent, c5a, complement, system, receptors, antagonists, mrgx2, mas-related, agonists, hypernociception, MRGPRX2, Complement, Mas-related, G, Protein-Coupled, Receptors, 5473, Tocris Bioscience
4 篇 PMX 53 的引用文献
引用文献是使用了 Tocris 产品的出版物。 PMX 53 的部分引用包括：
Sharma et al (2021) Epithelial phenotype restoring drugs suppress macular degeneration phenotypes in an iPSC model. Nat Commun 12 7293 PMID: 34911940
Heping et al (2022) Complement activation contributes to subretinal fibrosis through the induction of epithelial-to-mesenchymal transition (EMT) in retinal pigment epithelial cells. J Neuroinflammation 19 182 PMID: 35831910
Liu (2018) Orthosteric and allosteric action of the C5a receptor antagonists. Nat Struct Mol Biol 25 472 PMID: 29867214
Sarah Y et al (2020) Gut Ischemia Reperfusion Injury Induces Lung Inflammation via Mesenteric Lymph-Mediated Neutrophil Activation. Front Immunol 11 586685 PMID: 33042165
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PMX 53 的评论
平均评分: 5 (Based on 1 Review.)
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test.
By
Xiaogang Wang on 06/22/2021
分析类型： In Vitro
种属： Human
细胞系/组织： neutrophils
We used this inhibitor to study the biological activity of staphylococcal leukocidin PVL, which uses C5aR as a receptor to target host immune cells. We treated neutrophils with different concentrations (2.5, 5, and 10 uM) of pmx-53 for 1 h before incubated with 1 ug/ml PVL, and the cytotoxicity of treated cells was measured by LDH assay kit. As expected, pmx-53 treatment resulted in a dose-dependent reduction of PVL cytotoxicity to neutrophils.
