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| SB 290157 trifluoroacetate salt Basic information |
| Product Name: | SB 290157 trifluoroacetate salt | | Synonyms: | SB 290157 trifluoroacetate salt;SB290157 (trifluoroacetate);SB 290157 TRIFLUOROACETATE; SB-290157 TRIFLUOROACETATE;SB 290157 - CAS 1140525-25-2 - Calbiochem;(2S)-5-(diaminomethylideneamino)-2-[[2-(2,2-diphenylethoxy)acetyl]amino]pentanoic acid;N2-(2-(2,2-diphenylethoxy)acetyl)-L-arginine, 2,2,2-trifluor;N2-(2-(2,2-diphenylethoxy)acetyl)-L-arginine (trifluoroacetate) | | CAS: | 1140525-25-2 | | MF: | C24H29F3N4O6 | | MW: | 526.51 | | EINECS: | | Product Categories: | | Mol File: | 1140525-25-2.mol |
| SB 290157 trifluoroacetate salt Chemical Properties |
| Melting point | >43°C (dec.) | | storage temp. | -20°C | | solubility | Ethanol (Slightly, Sonicated), Methanol (Slightly), Water (Slightly) | | form | powder | | color | white to beige | | optical activity | [α]/D +1.5 to +5°, c = 1.0 in DMSO | | Stability: | Hygroscopic |
| SB 290157 trifluoroacetate salt Usage And Synthesis |
| Uses | SB 290157 Trifluoroacetate Salt is a selective, high affinity, competitive antagonist of anaphylatoxin C3a receptor. | | General Description | A non-peptide with anti-inflammatory properties that acts as a selective, high affinity, competitive antagonist of the anaphylatoxin C3a receptor (C3aR; IC50 = 200 nM). Does not antagonize C5aR or other chemotactic G-protein coupled receptors. Blocks C3a-induced internalization of C3aR in human neutrophils and C3a-induced Ca2+ mobilization in basophilic leukemia RBL-2H3 cells expressing murine, guinea pig, or human C3aR (IC50 = 7, 12.5, and 27.7 nM, respectively). Also blocks C3a-mediated ATP release from guinea pig platelets (IC50 = 30 nM). | | Biological Activity | sb 290157 is a c3ar antagonist.the anaphylatoxin c3a, a potent chemotactic peptide and inflammatory mediator, binds to and activates a g-protein-coupled receptor. molecular cloning of the c3ar has facilitated the identification of the non-peptide c3ar antagonists. | | Biochem/physiol Actions | Target IC50: 200 nM against the anaphylatoxin C3a receptor; 7, 12.5, and 27.7 nM, in blocking C3a-induced internalization of C3aR in human neutrophils and C3a-induced Ca2+ mobilization in basophilic leukemia RBL-2H3 cells expressing murine, guinea pig, or human C3aR | | in vitro | sb 290157 was a competitive antagonist of 125i-c3a and binding to rat basophilic leukemia (rbl)-2h3 cells expressing the human c3ar , with an ic50 of 200 nm. sb 290157 could also block the c3a-induced c3ar internalization concentration-dependently and c3a-induced ca21 mobilization in rbl-c3ar cells and human neutrophils. sb 290157 was founf to be selective for the c3ar in that it did not antagonize the c5ar or six other chemotactic g protein-coupled receptors. in addition, sb 290157 could also inhibit c3a induced ca21 mobilization of rbl-2h3 cells expressing the mouse and guinea pig c3ars [1]. | | in vivo | in animal models, sb 290157 was able to inhibit neutrophil recruitment in a guinea pig lps-induced airway neutrophilia model and decrease paw edema in a rat adjuvant-induced arthritis model [1]. | | IC 50 | 200 nm | | references | [1] r. s. ames, d. lee, j. j. foley, et al. identification of a selective nonpeptide antagonist of the anaphylatoxin c3a receptor that demonstrates antiinflammatory activity in animal models. journal of immunology 166(10), 6341-6348 (2001). |
| SB 290157 trifluoroacetate salt Preparation Products And Raw materials |
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