259218-28-5

259218-28-5 structure

Name: SB 290157
Chemical Name: SB 290157
CAS Number: 259218-28-5
Molecular Formula: C₂₂H₂₈N₄O₄
Molecular Weight: 412.49
Create Date: 2020-01-12 10:59:49
Modify Date: 2024-01-03 20:05:39
A potent, selective nonpeptide antagonist of anaphylatoxin C3a receptor (C3aR) with IC50 of 200 nM; does not antagonize the C5aR or 5 other chemotactic GPCRs on human neutrophils; 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; also inhibits C3a-induced Ca2+ mobilization of mouse and guinea pig C3aRS with IC50 of 7 and 12.5 nM, respectively; 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.

Name	SB 290157

Description	A potent, selective nonpeptide antagonist of anaphylatoxin C3a receptor (C3aR) with IC50 of 200 nM; does not antagonize the C5aR or 5 other chemotactic GPCRs on human neutrophils; 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; also inhibits C3a-induced Ca2+ mobilization of mouse and guinea pig C3aRS with IC50 of 7 and 12.5 nM, respectively; 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.
References	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. View Related Products by Target Complement System

Molecular Formula	C₂₂H₂₈N₄O₄
Molecular Weight	412.49