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。

PMX-53 (3D53) is a synthetic peptidic and a potent and orally active complement C5a receptor (CD88) antagonist with an IC 50 of 20 nM. PMX-53 is also a low-affinity MrgX2 agonist that stimulates MrgX2-mediated mast cell degranulation. PMX-53 specifically binds to C5aR1 and does not bind to the second C5aR (C5L2) and C3aR. PMX-53 has anti-inflammatory, anticancer and antiatherosclerotic effects.

Solid

IC50: 20 nM (Complement C5a receptor)
MrgX2

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 Ca 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 Ca mobilization in HMC-1 cells and to cause degranulation in RBL-2H3 cells expressing MrgX2. has not independently confirmed the accuracy of these methods. They are for reference only.

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 μM 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 ch

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture and light, under nitrogenPowder -80°C 2 years；-20°C 1 ye

F-{Orn}-P-{d-Cha}-WR (Lactam bridge: Orn2- Arg6)

[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.

In Vitro: DMSO : 125 mg/mL (139.49 mM; Need ultrasonic)H₂O : 4 mg/mL (4.46 mM; ultrasonic and warming and heat to 60°C)配制储备液