284464-77-3 Usage
Biological Activity
bm 567 is acting as an inhibitor of thromboxane a2 (txa2) synthase and an antagonist of the tp receptor.thromboxane a2 (txa2), a potent thrombogenic and vasoconstrictor eicosanoid, is produced in large quantities by activated platelets. txa2 has been reported as a causal factor in the onset of stroke and myocardial infarction.
in vitro
bm 567 was identified as a dual acting antithrombogenic agent, acting as an inhibitor of thromboxane a2 (txa2) synthase and an antagonist of the tp receptor, the g protein-coupled receptor mediating txa2 activity in platelets and vascular smooth muscle. bm 567 antagonized the vascular smooth muscle tp receptor with an ic50 value of 1.1 nm. bm 567 was also able to inhibit platelet tx synthase with an ic50 value of 12 nm. in addition, by comparing crystallographic and electronic properties of bm567 and terbogrel, two compounds with dual action (txra and txsi), two essential anchoring identified: sulfonyl and nitro group for bm567 and carboxylate and pyridine nitrogen for terbogrel [1].
IC 50
1.1 nm for txa2 receptor antagonism
references
[1] michaux, c. ,rolin, s.,dogné, j.m., et al. structure determination and comparison of bm567, a sulfonylurea, with terbogrel, two compounds with dual action, thromboxane receptor antagonism, and thromboxane synthase inhibition. bioorganic & medicinal chemistry letters 11, 1019-1022 (2001).
Check Digit Verification of cas no
The CAS Registry Mumber 284464-77-3 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 2,8,4,4,6 and 4 respectively; the second part has 2 digits, 7 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 284464-77:
(8*2)+(7*8)+(6*4)+(5*4)+(4*6)+(3*4)+(2*7)+(1*7)=173
173 % 10 = 3
So 284464-77-3 is a valid CAS Registry Number.
284464-77-3Relevant articles and documents
Benzene-sulphonamide derivatives and their uses
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Page column 7; 21-22, (2010/02/09)
Benzene-sulphonamide derivatives complying with the general formula (I): in which the different symbols have different meanings, their optical isomers and the salts pharmacologically acceptable of these derivatives, as well as their uses for drug manufacture and as radiolabelled pharmacological tools of the thromboxan A2 receptors.
