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SB290157 trifluoroacetate
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SB290157 trifluoroacetate
CAS No. : 1140525-25-2
MCE 站:SB290157 trifluoroacetate
产品活性:SB290157 trifluoroacetate是有效,选择性的C3a受体的拮抗剂,IC50值为200 nM。
作用靶点:Complement System
In Vitro: 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.
In Vivo: 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.
相关产品:Bioactive Compound Library Plus | Immunology/Inflammation Compound Library | Peptidomimetic Library | Anti-Blood Cancer Compound Library | Dexamethasone | Cyclosporin A | EG00229 | PMX-53 | PMX 205 Trifluoroacetate | Leukadherin-1 | EG01377 dihydrochloride | BCX 1470 methanesulfonate | W-54011 | Compstatin | TLQP-21 TFA | C3a (70-77) TFA | FD-IN-1 | NDT 9513727 | Compstatin control peptide | POT-4
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