78712-43-3 Usage
Description
Ozagrel hydrochloride, with the chemical formula C18H22ClNO4, is a potent and selective inhibitor of thromboxane (TXA2) synthetase, a key enzyme involved in platelet aggregation and blood clot formation. It exhibits a high inhibitory potency with an IC50 value of 4 nM and does not inhibit prostacyclin (PGI2) synthase, cyclooxygenase, or PGE2 isomerase, as indicated by an IC50 greater than 1 mM. Ozagrel hydrochloride has been shown to inhibit platelet aggregation in vitro and arachidonate-induced arterial contraction in vivo. It also provides protection against arachidonate-induced sudden death in rabbits and alleviates liver injury induced by acetaminophen overdose in mice.
Uses
Used in Antithrombotic Applications:
Ozagrel hydrochloride is used as an antithrombotic agent for preventing blood clot formation. Its selective inhibition of thromboxane synthetase helps reduce platelet aggregation and arterial contraction, thereby decreasing the risk of thrombotic events.
Used in Thromboxane Synthase Inhibition:
Ozagrel hydrochloride is used as a thromboxane synthase inhibitor for managing conditions associated with excessive platelet aggregation and blood clot formation. By inhibiting the synthesis of thromboxane A2, a potent vasoconstrictor and platelet aggregator, ozagrel hydrochloride helps maintain blood flow and prevent thrombotic complications.
References
1) Hiraku?et al. (1986),?Pharmacological studies on the TXA2?synthetase inhibitor (E)-3-[p-(1H-imidazol-1-ylmethyl)phenyl]-2-propenoic acid (OKY-046); Jpn. J. Pharmacol.,?41?393
2) Naito?et al. (1983), Effects of thromboxane synthetase inhibitors on aggregation of rabbit platelets; Eur. J. Pharmacol.,?91?41
3) Edmonds and Leffer (1984),?Protective actions of a new thromboxane synthetase inhibitor in arachidonate induced sudden death; Life Sci.,?35?1763
4) Tomishima?et al. (2013),?Ozagrel hydrochloride, a selective thromboxane A2?synthase inhibitor, alleviates liver injury induced by acetaminophen overdose in mice; BMC Gastroenterol.,?30?13
Check Digit Verification of cas no
The CAS Registry Mumber 78712-43-3 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 7,8,7,1 and 2 respectively; the second part has 2 digits, 4 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 78712-43:
(7*7)+(6*8)+(5*7)+(4*1)+(3*2)+(2*4)+(1*3)=153
153 % 10 = 3
So 78712-43-3 is a valid CAS Registry Number.
InChI:InChI=1/C12H12N2O.ClH/c15-8-5-11-1-3-12(4-2-11)9-14-7-6-13-10-14;/h1-8,10,15H,9H2;1H/b8-5+;
78712-43-3Relevant articles and documents
Photoisomerization of Sulindac and Ozagrel Hydrochloride by Vitamin B2 Catalyst Under Visible Light Irradiation
Makino, Kosho,Natsugari, Hideaki,Oshitari, Tetsuta,Suga, Mayuko,Tabata, Hidetsugu,Takahashi, Hideyo
, (2022/03/07)
Purpose: Photoisomerization of the E/Z-alkene structures of drugs is a matter of concern as it could result in potency loss and adverse side effects. This study focused on light-induced isomerization of sulindac and ozagrel hydrochloride catalyzed by concomitant vitamin B2 under light-emitting diode (LED) or fluorescent light. Methods: In the presence of 0.05/0.03 equivalents of vitamin B2/flavin adenine dinucleotide (FAD), sulindac or ozagrel hydrochloride was irradiated with LED light (405?nm) or fluorescent light. The photoisomerization in CD3OD and D2O was monitored by 1H NMR spectroscopy. Results: Sulindac and ozagrel hydrochloride isomerized in the presence of a catalytic amount of vitamin B2 or FAD under irradiation of 405?nm LED light and fluorescent light. Irradiation with LED light was found to be more effective than fluorescent light irradiation. The rate of photoisomerization was affected by the solvent, and the reaction in CD3OD proceeded faster than in D2O. Furthermore, ozagrel hydrochloride was more prone to isomerization than sulindac. Conclusion: The catalytic activity of vitamin B2 or FAD was demonstrated in the photoisomerization reaction of sulindac and ozagrel hydrochloride. Considering that the rate of photoisomerization in D2O is very slow, the possibility of the occurrence of photoisomerization during clinical use is low. However, this study suggests that the interfusion of vitamin B2 or FAD under excessive light exposure should be avoided as a caution during intravenous administration of sulindac or ozagrel hydrochloride.
A new route for the synthesis of ozagrel hydrochloride
Yu, Chenglong,Zhao, Baohai,Zhao, Yihong,Lin, Jimao
experimental part, p. 183 - 185 (2010/09/05)
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