559410
SB 290157
≥95% (HPLC), C3a receptor antagonist, lyophilized
別名:
SB 290157, N²-[(2,2-Diphenylethoxy)acetyl]-L-arginine, TFA
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この商品について
実験式（ヒル表記法）:
C22H28N4O4 · xC2HF3O2
CAS番号:
分子量:
412.48 (free base basis)
MDL number:
UNSPSC Code:
12352202
NACRES:
NA.25
Assay:
≥95% (HPLC)
Form:
lyophilized
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light
製品名
SB 290157, A non-peptide that acts as a selective, high affinity, competitive antagonist of the anaphylatoxin C3a receptor (IC50 = 200 nM).
Quality Segment
assay
≥95% (HPLC)
form
lyophilized
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, desiccated (hygroscopic), protect from light
solubility
DMSO: 5 mg/mL
shipped in
ambient
storage temp.
−20°C
SMILES string
FC(F)(F)C(=O)O.N([C@@H](CCCN\C(=N/[H])\N)C(=O)O)C(=O)COCC(c2ccccc2)c1ccccc1
InChI
1S/C22H28N4O4.C2HF3O2/c23-22(24)25-13-7-12-19(21(28)29)26-20(27)15-30-14-18(16-8-3-1-4-9-16)17-10-5-2-6-11-17;3-2(4,5)1(6)7/h1-6,8-11,18-19H,7,12-15H2,(H,26,27)(H,28,29)(H4,23,24,25);(H,6,7)/t19-;/m0./s1
InChI key
ZJRMPPVJAQWGEG-FYZYNONXSA-N
General description
A non-peptide that acts as a selective, high affinity, competitive antagonist of the anaphylatoxin C3a receptor (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). Exhibits anti-inflammatory properties. Supplied as a trifluoroacetate salt.
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).
Biochem/physiol Actions
Cell permeable: no
Primary Target
C3a receptor
C3a receptor
Product does not compete with ATP.
Reversible: no
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
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. Do not reuse solutions diluted in physiological buffers.
Other Notes
Ames, R.S., et al. 2001. J. Immunol. 166, 6341.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
保管分類
11 - Combustible Solids
一体何が起きているの？
WGK 3
引火点 (F)
Not applicable
引火点（°C）
Not applicable