SB 290157 trifluoroacetate salt
- Product Name
- SB 290157 trifluoroacetate salt
- CAS No.
- 1140525-25-2
- Chemical Name
- SB 290157 trifluoroacetate salt
- Synonyms
- SB290157 (trifluoroacetate);SB 290157 trifluoroacetate salt;SB290157 trifluoroacetate, 10 mM in DMSO;SB 290157 - CAS 1140525-25-2 - Calbiochem;SB 290157 TRIFLUOROACETATE; SB-290157 TRIFLUOROACETATE;N2-(2-(2,2-diphenylethoxy)acetyl)-L-arginine, 2,2,2-trifluor;N2-(2-(2,2-diphenylethoxy)acetyl)-L-arginine (trifluoroacetate);(2-(2,2-Diphenylethoxy)acetyl)-L-arginine 2,2,2-trifluoroacetate;(2S)-5-(diaminomethylideneamino)-2-[[2-(2,2-diphenylethoxy)acetyl]amino]pentanoic acid;(2S)-5-(Diaminomethylideneamino)-2-[[2-(2,2-diphenylethoxy)acetyl]amino]pentanoicacid,2,2,2-trifluoroaceticacid
- CBNumber
- CB82537362
- Molecular Formula
- C24H29F3N4O6
- Formula Weight
- 526.51
- MOL File
- 1140525-25-2.mol
SB 290157 trifluoroacetate salt Property
- 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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- SML1192
- Product name
- SB290157 trifluoroacetate salt
- Purity
- ≥97% (HPLC)
- Packaging
- 5mg
- Price
- $103
- Updated
- 2024/03/01
- Product number
- 559410
- Product name
- SB 290157 - CAS 1140525-25-2 - Calbiochem
- Packaging
- 10mg
- Price
- $166
- Updated
- 2024/03/01
- Product number
- 15783
- Product name
- SB 290157 (trifluoroacetate salt)
- Purity
- ≥95%
- Packaging
- 1mg
- Price
- $44
- Updated
- 2024/03/01
- Product number
- 15783
- Product name
- SB 290157 (trifluoroacetate salt)
- Purity
- ≥95%
- Packaging
- 5mg
- Price
- $87
- Updated
- 2024/03/01
- Product number
- SML1192
- Product name
- SB290157 trifluoroacetate salt
- Purity
- ≥97% (HPLC)
- Packaging
- 25mg
- Price
- $403
- Updated
- 2024/03/01
SB 290157 trifluoroacetate salt Chemical Properties,Usage,Production
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
storage
Desiccate at RT
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
Raw materials
Preparation Products
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