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PMX-53

CAS No. : 219639-75-5

MCE 站：PMX-53

产品活性：PMX-53 (3D53) 是一种合成肽，也是一种有效的，具有口服活性的补体 C5a 受体 (CD88) 拮抗剂，IC₅₀ 为 20 nM。PMX-53 还是一种低亲和力的 MrgX2 激动剂，可刺激 MrgX2 介导的肥大细胞脱颗粒。PMX-53 特异性结合 C5aR1，不结合第二个 C5aR (C5L2) 和 C3aR。PMX-53 具有抗炎，抗癌和抗动脉粥样硬化作用。

研究领域：Immunology/Inflammation

作用靶点：Complement System

In Vitro: PMX-53 is a potent CD88 antagonist and inhibits C5a-induced neutrophil myeloperoxidase release and chemotaxis with IC₅₀ values of 22 nM and 75 nM, respectively.
PMX-53 (10 nM) inhibits C5a-induced Ca²⁺ mobilization in HMC-1 cells, but at higher concentrations( ≥30 nM) it causes degranulation in LAD2 mast cells, CD34⁺ cell-derived mast cells, and RBL-2H3 cells stably expressing MrgX2. Replacement of Trp with Ala and Arg with dArg abolishes the ability of PMX-53 to inhibit C5a-induced Ca²⁺ mobilization in HMC-1 cells and to cause degranulation in RBL-2H3 cells expressing MrgX2.

In Vivo: PMX-53 (0.3-3?mg/kg; subcutaneous injection; once; male Wistar rats) treatment inhibits the hypernociception induced by zymosan-activated serum and C5a but not by the direct-acting hypernociceptive mediators, prostaglandin E2 and dopamine.
Local pretreatment of rats with PMX-53 (60-180?μg per paw) inhibits zymosan-, carrageenan-, lipopolysaccharide (LPS)- and antigen-induced hypernociception.
Pharmacokinetic analyses have shown that PMX-53 (3D53) appears in the plasma within 5 min of oral administration (3 mg/kg) to rats, with peak blood levels of approximately 0.3 ?M beingreached within 20 min The plasma elimination half-life wasapproximately 70 min in this case.
The non-acetylated version of PMX-53 (3D53) binds to isolated mouse neutrophils with a K_d value of 30 nM (mouse C5a binds with a K_d value of 0.3 nM) and inhibits mouse C5a-induced chemotaxis with an IC₅₀ value of 0.5 nM.

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