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Chemical Structure : SB 290157
Catalog No.: PC-60789Not For Human Use, Lab Use Only.
SB-290157 (SB 290157) potent, selective nonpeptide antagonist of anaphylatoxin C3a receptor (C3aR) with IC50 of 200 nM.
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SB-290157 (SB 290157) potent, selective nonpeptide antagonist of anaphylatoxin C3a receptor (C3aR) with IC50 of 200 nM.
SB 290157 does not antagonize the C5aR or 5 other chemotactic GPCRs on human neutrophils.
SB 290157 blocks C3a-induced C3aR internalization and C3a-induced Ca(2+) mobilization in RBL-C3aR cells and human neutrophils with IC50 of 27.7 and 28 nM, respectively.
SB 290157 also inhibits C3a-induced Ca2+ mobilization of mouse and guinea pig C3aRS with IC50 of 7 and 12.5 nM, respectively.
SB 290157 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, demonstrates antiinflammatory activity in animal models.
| M.Wt | 412.49 | |
| Formula | C22H28N4O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Ames RS, et al. J Immunol. 2001 May 15;166(10):6341-8.
2. Therien AG. J Immunol. 2005 Jun 15;174(12):7479; author reply 7479-80.
3. Ratajczak J, et al. Blood. 2004 Mar 15;103(6):2071-8.
4. Proctor LM, et al. Br J Pharmacol. 2004 Jun;142(4):756-64.
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