PMX 53
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- CAS号:
- 219639-75-5
- 英文名:
- PMX 53
- 英文别名:
- PMX-53 (3D53);Ac-Phe-cyclo(Orn-Pro-D-Cha-Trp-Arg);L-Arginine, N-acetyl-L-phenylalanyl-L-ornithyl-L-prolyl-3-cyclohexyl-D-alanyl-L-tryptophyl-, (6→2)-lactam;(S)-N-((3R,6S,9S,15S,20aS)-6-((1H-indol-3-yl)methyl)-3-(cyclohexylmethyl)-9-(3-guanidinopropyl)-1,4,7,10,16-pentaoxoicosahydropyrrolo[1,2-a][1,4,7,10,13]pentaazacyclooctadecin-15-yl)-2-acetamido-3-phenylpropanamide
- 中文名:
- PMX 53
- 中文别名:
- 化合物 T28429;拮抗剂多肽PMX-53;PMX53|||PMX 53;PMX 53,C5A受体拮抗剂;N-乙酰基-L-苯丙氨酰基-L-鸟酰基-L-脯氨酰基-3-环己基-D-丙氨酰基-L-色氨酸-L-精氨酸-(6→2)-内酰胺
- CBNumber:
- CB64796594
- 分子式:
- C47H65N11O7
- 分子量:
- 896.11
- MOL File:
- 219639-75-5.mol
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PMX 53化学性质
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密度:
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1.40±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C, protect from light, stored under nitrogen
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溶解度:
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Soluble in DMSO
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形态:
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Solid
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酸度系数(pKa):
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13.23±0.70(Predicted)
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颜色:
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White to off-white
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水溶解性:
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Soluble to 2 mg/ml in water
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PMX 53性质、用途与生产工艺
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。
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:
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Adult male Wistar rats (weighing 180-200 g) injected with zymosan
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Dosage:
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0.3 mg/kg, 1 mg/kg or 3 mg/kg
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Administration:
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Subcutaneous injection; once
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Result:
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Inhibited the hypernociception induced by zymosan-activated serum and C5a.
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PMX 53
上下游产品信息
上游原料
下游产品
219639-75-5, PMX 53 相关搜索:
- 药靶配体
- 目录多肽
- 目录肽
- 药物多肽
- PMX53|||PMX 53
- PMX 53,C5A受体拮抗剂
- 拮抗剂多肽PMX-53
- 化合物 T28429
- N-乙酰基-L-苯丙氨酰基-L-鸟酰基-L-脯氨酰基-3-环己基-D-丙氨酰基-L-色氨酸-L-精氨酸-(6→2)-内酰胺
- 219639-75-5
- PMX-53 (3D53)
- (S)-N-((3R,6S,9S,15S,20aS)-6-((1H-indol-3-yl)methyl)-3-(cyclohexylmethyl)-9-(3-guanidinopropyl)-1,4,7,10,16-pentaoxoicosahydropyrrolo[1,2-a][1,4,7,10,13]pentaazacyclooctadecin-15-yl)-2-acetamido-3-phenylpropanamide
- L-Arginine, N-acetyl-L-phenylalanyl-L-ornithyl-L-prolyl-3-cyclohexyl-D-alanyl-L-tryptophyl-, (6→2)-lactam
- Ac-Phe-cyclo(Orn-Pro-D-Cha-Trp-Arg)