Aglafoline inhibits in a selective and concentration-dependent manner the aggregation and ATP release reaction induced in washed rabbit platelets by PAF (platelet-activating factor). The IC50 values of Aglafoline on PAF (3.6 nM)-induced platelet aggregation were about 50 μM.ic50 value: 50 μMTarget: PAFin vitro: Aglafoline also inhibits [3H]PAF (3.6 nM) binding to washed rabbit platelets with an IC50 value of 17.8 ± 2.6 μM. The concentration-response curve of PAF-induced platelet aggregation was shifted to the right by Aglafoline with pA2 and pA10 values of 5.97 and 5.04, respectively. Although thromboxane B2 formation caused by collagen and thrombin was partially suppressed by Aglafoline, thromboxane B2 formation caused by ionophore A23187 and arachidonic acid was not affected. Aglafoline inhibited the [3H]inositol monophosphate formation caused by PAF but not that caused by collagen or thrombin in the presence of indomethacin (20 μM). in vivo: The cAMP content of washed rabbit platelets was not affected by Aglafoline. Rat femoral intravenous administration of Aglafoline (10 mg/kg) did not affect blood pressure. However, Aglafoline (10 mg/kg) both prophylactically and therapeutically antagonized PAF (2.5 μg/kg)-induced hypotensive shock in rats. Intravenous PAF (30 ng/kg) caused severe bronchoconstriction in guinea pigs. This effect was completely blocked by Aglafoline. This implies Aglafoline is an effective PAF antagonist not only in vitro, but also in vivo.

Product information

CAS Number: 143901-35-3

Molecular Weight: 492.52

Formula: C28H28O8

Chemical Name: methyl (2S,3R,4R,5S,6R)-2,3-dihydroxy-10,12-dimethoxy-6-(4-methoxyphenyl)-5-phenyl-7-oxatricyclo[6.4.0.0²,⁶]dodeca-1(12),8,10-triene-4-carboxylate

Smiles: COC1C=C(C=C2O[C@]3([C@@H]([C@H]([C@@H](O)[C@@]3(O)C=12)C(=O)OC)C1C=CC=CC=1)C1C=CC(=CC=1)OC)OC

InChiKey: VFTGDXPPYSWBSO-GWNOIRNCSA-N

InChi: InChI=1S/C28H28O8/c1-32-18-12-10-17(11-13-18)28-23(16-8-6-5-7-9-16)22(26(30)35-4)25(29)27(28,31)24-20(34-3)14-19(33-2)15-21(24)36-28/h5-15,22-23,25,29,31H,1-4H3/t22-,23-,25-,27+,28+/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 21.43 mg/mL (43.51 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

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