Chemical Structure : SB 290157
CAS No.:
259218-28-5
SB 290157
(SB-290157;SB290157)
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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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412.49
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Formula
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C22H28N4O4
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20 °C 12 Months; 4°C 6 Months
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- In Solvent
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-80 °C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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N(2)-[(2,2-diphenylethoxy)acetyl]-L-arginine
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References
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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