
NDT 9513727
CAS No. 439571-48-9
NDT 9513727 ( NDT9513727 )
产品货号. M14495 CAS No. 439571-48-9
NDT 9513727 是一种有效的、选择性的、口服生物可利用的 C5a 受体反向激动剂,在放射性配体结合测定中 IC50 为 11.6 nM。
纯度: >98% (HPLC)






规格 | 价格/人民币 | 库存 | 数量 |
5MG | ¥2730 | 有现货 |
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50MG | ¥11259 | 有现货 |
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100MG | ¥16929 | 有现货 |
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200MG | 获取报价 | 有现货 |
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500MG | 获取报价 | 有现货 |
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1G | 获取报价 | 有现货 |
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生物学信息
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产品名称NDT 9513727
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注意事项本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
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产品简述NDT 9513727 是一种有效的、选择性的、口服生物可利用的 C5a 受体反向激动剂,在放射性配体结合测定中 IC50 为 11.6 nM。
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产品描述NDT 9513727 is a potent, selective and orally bioavailable C5a receptor inverse agonist with IC50 of 11.6 nM in radioligand binding assay; exhibits potent activity in both gerbil and monkey lung membrane preparations (6.4 and 7.3 nM), but has minimal activity in rat, mouse, and dog lung preparations (>10 uM); blocks hC5a-stimulated chemotaxis activity in human polymorphonuclear neutrophils and U937 cells with IC50 of 4.7 and 4.3 nM, respectively, inhibits C5a-stimulated responses, including guanosine 5'-3-O-(thio)triphosphate binding, Ca(2+) mobilization, oxidative burst, degranulation, cell surface CD11b expression and chemotaxis in various cell types with IC50 of 1.1-9.2 nM; effectively inhibits C5a-induced neutropenia in gerbil and cynomolgus macaque in vivo.
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体外实验——
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体内实验Animal Model:Six-week-old Mongolian gerbils Dosage:1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg Administration:Oral administration Result:Significantly inhibited hC5a-induced neutropenia at 3 mg/kg, 10 mg/kg, 30 mg/kg.Animal Model:Rat Dosage:50 mg/kg (Pharmacokinetic Analysis) Administration:Oral administrationResult:Oral bioavailability (73%), Cmax (5.98 μM), T1/2 (4.8 h).Animal Model:Monkey Dosage:25.2 mg/kg (Pharmacokinetic Analysis) Administration:Oral administrationResult:Oral bioavailability (26%), Cmax (830 nM), T1/2 (7.9 h).
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同义词NDT9513727
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通路Immunology/Inflammation
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靶点Complement System
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受体Complement System
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研究领域——
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适应症——
化学信息
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CAS Number439571-48-9
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分子量573.693
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分子式C36H35N3O4
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纯度>98% (HPLC)
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溶解度In Vitro:?DMSO : 100 mg/mL (174.31 mM)
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SMILESCCCCN1C(CN(CC2=CC=C(OCO3)C3=C2)CC4=CC=C(OCO5)C5=C4)=C(C6=CC=CC=C6)N=C1C7=CC=CC=C7
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化学全称N,N-Bis(1,3-benzodioxol-5-ylmethyl)-1-butyl-2,4-diphenyl-1H-imidazole-5-methanamine
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1. Brodbeck RM, et al. J Pharmacol Exp Ther. 2008 Dec;327(3):898-909.
2. Robertson N, et al. Nature. 2018 Jan 3;553(7686):111-114.
产品手册




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