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Apafant

Chemical Structure : Apafant

CAS No.: 105219-56-5

Apafant (WEB2086, WEB-2086)

Catalog No.: PC-70045Not For Human Use, Lab Use Only.

Apafant (WEB2086) is a potent and specific antagonist of platelet activating factor (PAF) receptor that inhibits PAF-induced human platelet and neutrophil aggregation in vitro with IC50 of 0.17 and 0.36 uM, respectively.

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Biological Activity

Apafant (WEB2086) is a potent and specific antagonist of platelet activating factor (PAF) receptor that inhibits PAF-induced human platelet and neutrophil aggregation in vitro with IC50 of 0.17 and 0.36 uM, respectively.
Apafant (WEB2086) reverses or abolishes the bronchoconstriction, hypotension, thrombocytopenia and leukopenia induced by PAF-acether at 0.1-1 mg/kg in guinea-pigs.
Apafant (WEB2086) also markedly decreases the bronchoconstriction and leukopenia induced by 100 ug/kg antigen in mepyramine.

Physicochemical Properties

M.Wt 455.961
Formula C22H22N5O2SCl
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-(4-(2-chlorophenyl)-9-methyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-2-yl)-1-morpholinopropan-1-one

References

1. Casals-Stenzel J, et al. J Pharmacol Exp Ther. 1987 Jun;241(3):974-81.

2. Casals-Stenzel J, et al. Br J Pharmacol. 1987 Aug;91(4):799-802.

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