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
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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 |