SB290157 trifluoroacetate

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

SB290157 trifluacetate 是一种有效的选择性 C3a 受体拮抗剂（IC50 为 200 nM）。 SB 290157 是 125I-C3a 放射性配体的竞争性拮抗剂，与表达人 C3aR（RBL-C3aR，IC50 为 200 nM）的大鼠嗜碱性白血病-2H3 细胞结合。

SB290157 trifluoroacetate is a potent and selective antagonist of C3a receptor(IC50 of 200 nM). 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.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.

SB 290157, functions as a competitive antagonist of 125I-C3a radioligand binding to rat basophilic leukemia-2H3 cells expressing the human C3aR (RBL-C3aR), with an 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 with IC50s f 27.7 and 28 nM, respectively. SB 290157 is selective for the C3aR in that it does not antagonize the C5aR or six other chemotactic G protein-coupled receptors. 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.

SB 290157, inhibits neutrophil recruitment in a guinea pig LPS-induced airway neutrophilia model and decreases paw edema in a rat adjuvant-induced arthritis model. 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.

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Others

Other Targets

C3a

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1140525-25-2

526.51

C24H29F3N4O6

>98% (HPLC)

DMSO:125 mg/mL (237.41 mM; Need ultrasonic)

OC(=O)C(F)(F)F.NC(=N)NCCC[C@H](NC(=O)COCC(c1ccccc1)c1ccccc1)C(O)=O

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(-20℃)

With Ice Pack

≥ 2 years