A potent, selective PAF receptor antagonist
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Apafant

Item No. 14532

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[4-(2-chlorophenyl)-9-methyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-2-yl]-1-(4-morpholinyl)-1-propanone
CAS Number
105219-56-5
Synonyms
  • WEB 2086
Molecular Formula
C22H22ClN5O2S
Formula Weight
456.0
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlEthanol: 5 mg/mlPBS (pH 7.2): 0.25 mg/ml
λmax
204, 242 nm
SMILES
CC1=NN=C(N21)CN=C(C3=C(Cl)C=CC=C3)C4=C2SC(CCC(N5CCOCC5)=O)=C4
InChi Code
InChI=1S/C22H22ClN5O2S/c1-14-25-26-19-13-24-21(16-4-2-3-5-18(16)23)17-12-15(31-22(17)28(14)19)6-7-20(29)27-8-10-30-11-9-27/h2-5,12H,6-11,13H2,1H3
InChi Key
JGPJQFOROWSRRS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Platelet-activating factor (PAF) is a biologically active phospholipid that activates platelets, polymorphonuclear leukocytes, monocytes, and macrophages.1 PAF also increases vascular permeability, decreases cardiac output, induces hypotension, stimulates uterine contraction, and has been implicated in pathological processes, such as inflammation and allergy.2 Apafant is a water soluble, selective PAF receptor antagonist that inhibits PAF binding to human PAF receptors with a Ki value of 9.9 nM.3 Apafant displays anti-inflammatory, antiangiogenic, and anticancer activity.3,4,5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Prescott, S.M., Zimmerman, G.A., and McIntyre, T.M. Platelet-activating factor. The Journal of Biological Chemisty 265(29), 17381-17384 (1990).

    2. Snyder, F. Platelet-activating factor and related acetylated lipids as potent biologically active cellular mediators. Am. J. Physiol. Cell Physiol. 259(5 Pt 1), C697-C708 (1990).

    3. Kato, M., Imoto, K., Miyake, H., et al. Apafant, a potent platelet-activating factor antagonist, blocks eosinophil activation and is effective in the chronic phase of experimental allergic conjunctivitis in guinea pigs. J. Pharmacol. Sci. 95(4), 435-442 (2004).

    4. Bielenberg, G.W., Wagener, G., and Beck, T. Infarct reduction by the platelet activating factor antagonist apafant in rats. Stroke 23(1), 98-103 (1992).

    5. Cellai, C., Laurenzana, A., Vannucchi, A.M., et al. Growth inhibition and differentiation of human breast cancer cells by the PAFR antagonist WEB-2086. Br. J. Cancer 94(11), 1637-1642 (2006).