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 |
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英文别名 |
Benzenepropanamide, α-(acetylamino)-N-[3-(cyclohexylmethyl)-9-[3-[(diaminomethylene)amino]propyl]eicosahydro-6-(1H-indol-3-ylmethyl)-1,4,7,10,16-pentaoxopyrrolo[1,2-a][1,4,7,10,13]pentaazacyclooct adecin-15-yl]-
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 |
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。 |
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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 |
密度 | 1.4±0.1 g/cm3 |
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分子式 | C47H65N11O7 |
分子量 | 896.089 |
精确质量 | 895.506836 |
LogP | 0.81 |
折射率 | 1.684 |
储存条件 | -20°C |