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CV-3988 (CAS 85703-73-7)

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Synonym:rac-3-(N-Octadecylcarbamoyl)-2-Methoxy) propyl-(2- thiazolioethyl) phosphate
Application:A specific antagonist of PAF binding to PAF-R
CAS Number:85703-73-7
Purity:98%
Molecular Weight:592.77
Molecular Formula:C28H53N2O7PS
Refer to Certificate of Analysis for lot specific data (including water content).
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Product NameCatalog #UnitPriceQtyAddFavorites
CV-3988 sc-201015 5 mg $147
CV-3988 sc-201015A 25 mg $599
Description
CV-3988 is a specific antagonist of PAF-R (platelet-activating factor receptor), blocking signaling events correlated to the expression and binding of PAF to the PAF-R (Ki = 0.872 μM). CV-3988 has close structural similarity to PAF allowing recognition by the receptor, where it then associates strongly to the binding site and blocks the activating interaction with PAF. Inhibition of this binding has been used to investigate the numerous cellular consequences of PAF association to the PAF-R. PAF-induced platelet aggregation is inhibited by CV-3988. Mediation of the severity of endotoxin shock was demonstrated upon administration of CV-3988, indicating that PAF serves a pivotal role in the pathogenesis of endotoxin shock. The lethality of anaphylactic shock in mice was also subdued in the presence of CV-3988, suggesting a lethal role of PAF in the anaphylaxis. As a specific antagonist of PAF binding, CV-3988 has seen wide utility as a benchmark PAF-binding antagonist for binding studies with other compounds.
Technical Information
Appearance:Powder
Physical State:Solid
Solubility:Soluble in ethanol (15 mg/ml), and DMSO (≥10 mg/ml).
Storage:Store at -20° C
IC50:Platelet activating factor receptor: IC50 = 600 nM (human); Oryctolagus cuniculus: EC5050 = 30.5 µM
pK Values:pKa: 1.27
Safety and Reference Information
WGK Germany:3
PubChem CID:107681
MDL Number:MFCD00133274
SMILES:CCCCCCCCCCCCCCCCCCNC(=O)OCC(COP(=O)([O-])OCC[N+]1=CSC=C1)OC
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
References
1. Terashita, Z., et al. 1983. Life Sci. 32: 1975-1982. PMID: 6403793
2. Terashita, Z., et al. 1985. Biochem. Pharmacol. 34: 1491-1495. PMID: 2986648
3. Terashita, Z., et al. 1985. Eur. J. Pharmacol. 109: 257-261. PMID: 3996473
4. Hwang, S.B. and Lam, M.H. 1986. Biochem. Pharmacol. 35: 4511-4518. PMID: 3024653
5. Terashita, Z., et al. 1987. J. Pharmacol. Exp. Ther. 243: 378-383. PMID: 3118009
6. Hayashi, M., et al. 1987. Jpn. J. Pharmacol. 44: 127-134. PMID: 2888915
7. Robertson, D.A., et al. 1988. J. Pharmacol. Exp. Ther. 245: 124-128. PMID: 3361438
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