| SB 290157 (trifluoroacetate salt)C3aR antagonist |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity ≥95.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
SB 290157 (trifluoroacetate salt) Dilution Calculator
calculate
SB 290157 (trifluoroacetate salt) Molarity Calculator
calculate
| Cas No. | 1140525-25-2 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | N2-[2-(2,2-diphenylethoxy)acetyl]-L-arginine, 2,2,2-trifluoroacetate | ||
| Canonical SMILES | O=C(N[C@H](C(O)=O)CCCNC(N)=N)COCC(C1=CC=CC=C1)C2=CC=CC=C2.FC(F)(C(O)=O)F | ||
| Formula | C22H28N4O4 • CF3COOH | M.Wt | 526.5 |
| Solubility | ≤30mg/ml in ethanol;20mg/ml in DMSO;25mg/ml in dimethyl formamide | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
IC50: 200 nM
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.
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].
Clinical trial: So far, no clinical study has been conducted.
Reference:[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).
