PMX53

• 常用名: PMX53
• 英文名: PMX 53
• CAS号: 219639-75-5
• 分子量: 896.089
• 密度: 1.4±0.1 g/cm3
• 沸点: N/A
• 分子式: C₄₇H₆₅N₁₁O₇
• 熔点: N/A
• 闪点: N/A

PMX53用途

PMX53(Ac-Phe-cyclo(Orn-Pro-D-Cha-Trp-Arg))是一种有效的C5a受体(CD88)拮抗剂,IC50为20 nM,也是人类Mas相关基因2(MrgX2)的激动剂。肥大细胞；PMX-53(10 nM)抑制HMC-1细胞中C5a诱导的Ca(2+)动员,但在较高浓度(>30 nM)时,它导致LAD2肥大细胞脱粒,CD34(+)细胞衍生的肥大细胞和稳定表达MrgX2的RBL-2H3细胞；抑制酵母聚糖,角叉菜胶,LPS和抗原诱导的大鼠过度伤害感受。

PMX53名称

• 英文名: Nα-Acetyl-N-[3-(cyclohexylmethyl)-9-{3-[(diaminomethylene)amino]propyl}-6-(1H-indol-3-ylmethyl)-1,4,7,10,16-pentaoxoicosahydropyrrolo[1,2-a][1,4,7,10,13]pentaazacyclooctadecin-15-yl]phenylalaninamidato

PMX53生物活性

• 描述: PMX53(Ac-Phe-cyclo(Orn-Pro-D-Cha-Trp-Arg))是一种有效的C5a受体(CD88)拮抗剂,IC50为20 nM,也是人类Mas相关基因2(MrgX2)的激动剂。肥大细胞；PMX-53(10 nM)抑制HMC-1细胞中C5a诱导的Ca(2+)动员,但在较高浓度(>30 nM)时,它导致LAD2肥大细胞脱粒,CD34(+)细胞衍生的肥大细胞和稳定表达MrgX2的RBL-2H3细胞；抑制酵母聚糖,角叉菜胶,LPS和抗原诱导的大鼠过度伤害感受。
• 参考文献: References 1. Ting E, et al. Br J Pharmacol. 2008 Mar;153(5):1043-53. 2. Subramanian H, et al. Mol Pharmacol. 2011 Jun;79(6):1005-13. 3. Liu H, et al. Nat Struct Mol Biol. 2018 Jun;25(6):472-481. 4. Finch AM, et al. J Med Chem. 1999 Jun 3;42(11):1965-74. View Related Products by Target Complement System

PMX53物理化学性质

• 密度: 1.4±0.1 g/cm3
• 分子式: C₄₇H₆₅N₁₁O₇
• 分子量: 896.089
• 精确质量: 895.506836
• LogP: 0.81
• InChIKey: YOKBGCTZYPOSQM-UNHORJANSA-N
• SMILES: CC(=O)NC(Cc1ccccc1)C(=O)NC1CCCNC(=O)C(CCCN=C(N)N)NC(=O)C(Cc2c[nH]c3ccccc23)NC(=O)C(CC2CCCCC2)NC(=O)C2CCCN2C1=O
• 折射率: 1.684
• 储存条件: -20°C

PMX53靶点实验

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实验名称：Oral bioavailability in Wistar rat at 10 mg/kg 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL4229739

实验名称：Antagonist activity at of C5aR in in human macrophages assessed as half life of resid... 来源：ChEMBL 靶标：C5a anaphylatoxin chemotactic receptor 1 External Id：CHEMBL4138670

实验名称：Half life in Wistar rat at 10 mg/kg, po or 1 mg/kg, iv 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL4229740

实验名称：Displacement of [125I-C5a] from C5a receptor in human PBMC by scintillation counting 来源：ChEMBL 靶标：C5a anaphylatoxin chemotactic receptor 1 External Id：CHEMBL1176067

实验名称：Human C5a1 receptor (Complement peptide receptors) 来源：IUPHAR-DB 靶标：C5a1 receptor (Complement peptide receptors) [Homo sapiens] External Id：32_Human

实验名称：Displacement of [125I-C3a] from C3a receptor in human PBMC at 1 mM by scintillation c... 来源：ChEMBL 靶标：C3a anaphylatoxin chemotactic receptor External Id：CHEMBL1176064

实验名称：Agonist activity at human C3a receptor in human U937 cells assessed as induction of i... 来源：ChEMBL 靶标：C3a anaphylatoxin chemotactic receptor External Id：CHEMBL1176063

实验名称：ASTRAZENECA: % bound to plasma by equilibrium dialysis. Compound is incubated with wh... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3301366

实验名称：Stability in human plasma after 1 hr at 37 degC 来源：ChEMBL 靶标：Plasma External Id：CHEMBL910271

实验名称：Inhibition of CYP3A4 at 10 uM 来源：ChEMBL 靶标：Cytochrome P450 3A4 External Id：CHEMBL910275

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PMX53英文别名

• Nα-Acetyl-N-[3-(cyclohexylmethyl)-9-{3-[(diaminomethylene)amino]propyl}-6-(1H-indol-3-ylmethyl)-1,4,7,10,16-pentaoxoicosahydropyrrolo[1,2-a][1,4,7,10,13]pentaazacyclooctadecin-15-yl]phenylalaninam idato