219639-75-5
219639-75-5 結(jié)構(gòu)式
基本信息
拮抗劑多肽PMX-53
N-乙?；?L-苯丙氨酰基-L-鳥?；?L-脯氨?；?3-環(huán)己基-D-丙氨?；?L-色氨酸-L-精氨酸-(6→2)-內(nèi)酰胺
L-Arginine, N-acetyl-L-phenylalanyl-L-ornithyl-L-prolyl-3-cyclohexyl-D-alanyl-L-tryptophyl-, (6→2)-lactam
物理化學(xué)性質(zhì)
| 報價日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
| 2026/06/05 | HY-106178 | PMX 53 PMX-53 | 219639-75-5 | 5 mg | 2000元 |
| 2026/06/05 | HY-106178 | PMX 53 PMX-53 | 219639-75-5 | 10 mg | 2950元 |
| 2026/06/05 | HY-106178 | PMX 53 PMX-53 | 219639-75-5 | 10 mM * 1 mL in DMSO | 3943元 |
常見問題列表
IC50: 20 nM (Complement C5a receptor)
MrgX2
PMX-53 is a potent CD88 antagonist and inhibits C5a-induced neutrophil myeloperoxidase release and chemotaxis with IC
50
values of 22 nM and 75 nM, respectively.
PMX-53 (10 nM) inhibits C5a-induced Ca
2+
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
2+
mobilization in HMC-1 cells and to cause degranulation in RBL-2H3 cells expressing MrgX2.
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 chemotaxis with an IC
50
value of 0.5 nM.
| Animal Model: | Adult male Wistar rats (weighing 180-200?g) injected with zymosan |
| Dosage: | 0.3 mg/kg, 1 mg/kg or 3?mg/kg |
| Administration: | Subcutaneous injection; once |
| Result: | Inhibited the hypernociception induced by zymosan-activated serum and C5a. |