Description
KF 13218 is a potent, selective and long lasting thromboxane B2 (TXB2) synthase inhibitor with an IC50 value of 5.3±1.3 nM.
Product information
CAS Number: 127654-03-9
Molecular Weight: 336.38
Formula: C20H20N2O3
Chemical Name: 6-[(2Z)-10-methyl-9-oxo-5,10-diazatricyclo[9.4.0.0³,⁸]pentadeca-1(15),3,5,7,11,13-hexaen-2-ylidene]hexanoic acid
Smiles: CN1C2=CC=CC=C2/C(=C/CCCCC(O)=O)/C2=CN=CC=C2C1=O
InChiKey: QFZVHDITZGTVJH-AUWJEWJLSA-N
InChi: InChI=1S/C20H20N2O3/c1-22-18-9-6-5-8-15(18)14(7-3-2-4-10-19(23)24)17-13-21-12-11-16(17)20(22)25/h5-9,11-13H,2-4,10H2,1H3,(H,23,24)/b14-7-
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
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
How to use
In Vitro:
KF 13218 inhibits human and bovine platelet thromboxane synthase with IC50 values of 27±5.8 nM (mean±S.E.M.) and 36±6.9 nM, respectively. KF 13218 does not inhibit cyclooxygenase or 5-lipoxygenase up to a dose of 100 μM and does not antagonize thromboxane A2/prostaglandin H2 receptors. KF 13218 inhibits arachidonic acid-induced thromboxane B2 production by human intact platelets with an IC50 value of 5.3±1.3 nM. The IC50 value of KF 13218 for the intact platelets is about 5 times lower than that for the microsomal enzyme. The inhibition of thromboxane synthase in platelets by KF 13218 is sustained after removal of the extracellular compound.
In Vivo:
After oral dosing in rat from 0.03 mg/kg to 3 mg/kg, KF 13218 dose-dependently inhibits the thromboxane B2 production in serum, and the inhibition is retained for 72 h. KF 13218, at a dose of 0.1 mg/kg p.o. prevents mortality induced by sodium arachidonate in rabbit.
Products are for research use only. Not for human use.
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