化合物SB290157 trifluoroacetate T12851

Product Introduction
Bioactivity


英文名: SB290157 trifluoroacetate

描述: SB290157 trifluoroacetate 是一种选择性 C3a 受体拮抗剂，IC50值为200 nM。

体外活性: SB 290157 is a competitive antagonist of 125I-C3a radioligand binding to rat basophilic leukemia-2H3 cells expressing the human C3aR (RBL-C3aR, IC50 of 200 nM). SB 290157 blocks C3a-induced C3aR internalization in a concentration-dependent manner and C3a-induced Ca2+ mobilization in RBL-C3aR cells and human neutrophils (IC50s of 27.7 and 28 nM, respectively). SB 290157 is selective for the C3aR in that. SB 290157 also inhibits C3a-induced Ca2+ mobilization of RBL-2H3 cells expressing the mouse and guinea pig C3aRs. It potently inhibits C3a-mediated ATP release from guinea pig platelets and inhibits C3a-induced potentiation of the contractile response to field stimulation of perfused rat caudal artery[1].

体内活性: Neutrophil recruitment in a guinea pig LPS-induced airway neutrophilia model inhibited by SB 290157 ,SB 290157 decreases paw edema in a rat adjuvant-induced arthritis model[1]. The antagonist is able to reduce joint swelling only at 3 h, and about 50% inhibition of joint swelling is observed with the concentration of 30 mg/kg. The C3 level is significantly decreased at 3 h compared with naive mice showing complement consumption. Furthermore, the C3 activation is observed and increased corresponding to the graded concentration of anti-OVA pAb[2].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 125 mg/mL (237.41 mM)


关键字: SB290157 Trifluoroacetate | SB290157 | SB-290157 trifluoroacetate | Inhibitor | SB 290157 Trifluoroacetate | inhibit | SB 290157 | Complement System | SB-290157 | SB290157 trifluoroacetate | SB-290157 Trifluoroacetate

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相关库: Bioactive Compounds Library Max | Inhibitor Library | NO PAINS Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途