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SB290157 trifluoroacetate

Chemical Structure : SB290157 trifluoroacetate

CAS No.: 1140525-25-2

SB290157 trifluoroacetate (SB 290157)

Catalog No.: PC-21966Not For Human Use, Lab Use Only.

SB290157 (SB 290157) trifluoroacetate is a potent, selective nonpeptide antagonist of anaphylatoxin C3a receptor (C3aR) with IC50 of 200 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

SB290157 (SB 290157) trifluoroacetate is a 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

M.Wt 526.51
Formula C24H29F3N4O6
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(2S)-5-(diaminomethylideneamino)-2-[[2-(2,2-diphenylethoxy)acetyl]amino]pentanoic acid;2,2,2-trifluoroacetic acid

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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