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559410

Sigma-Aldrich

SB 290157

A non-peptide that acts as a selective, high affinity, competitive antagonist of the anaphylatoxin C3a receptor (IC₅₀ = 200 nM).

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Synonym(s):
SB 290157, N²-[(2,2-Diphenylethoxy)acetyl]-L-arginine, TFA
Empirical Formula (Hill Notation):
C22H28N4O4 · xC2HF3O2
CAS Number:
Molecular Weight:
412.48 (free base basis)
UNSPSC Code:
12352202
NACRES:
NA.25

Quality Level

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

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
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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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