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Merck
CN

O1385

Ozagrel hydrochloride hydrate

≥98% (HPLC), solid

别名:

(E)-3-[4-(Imidazol-1-ylmethyl)phenyl]propenoic acid hydrochloride hydrate, OKY-046

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经验公式(希尔记法):
C13H12N2O2 · HCl · xH2O
化学文摘社编号:
分子量:
264.71 (anhydrous basis)
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
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InChI

1S/C13H12N2O2.ClH.H2O/c16-13(17)6-5-11-1-3-12(4-2-11)9-15-8-7-14-10-15;;/h1-8,10H,9H2,(H,16,17);1H;1H2/b6-5+;;

SMILES string

O.Cl.OC(=O)\C=C\c1ccc(Cn2ccnc2)cc1

InChI key

OWIZTYOMGVTSDP-TXOOBNKBSA-N

assay

≥98% (HPLC)

form

solid

storage condition

desiccated

color

white to off-white

solubility

H2O: soluble

storage temp.

room temp

Quality Level

Application

Ozagrel hydrochloride hydrate has been used as a thromboxane synthase inhibitor:
  • in high cholesterol-diet rats (HC) to test its effect on arteriolar constriction
  • to pre-treat mice to test its effect on lipopolysaccharide (LPS)-induced behavioral changes
  • to test its effect on arteriolar vasoconstriction in hyperglycemic mice

Biochem/physiol Actions

Ozagrel is a selective thromboxane A2 synthase (TXA2) inhibitor.
Ozagrel is useful in treating lacunar and thrombotic stroke. It blocks vasoconstriction and platelet aggregation. Ozagrel aids in improving the prostacyclin (PGI2)/ thromboxane A2 (TXA2) in the acute phase of cerebral ischemia. It improves endothelial dysfunction in L-methionine-induced hyperhomocysteinemia (HHcy)-induced vascular cognitive impairment and dementia (VCID).

存储类别

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)

法规信息

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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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Akihiro Koumura et al.
The Journal of pharmacology and experimental therapeutics, 338(1), 337-344 (2011-04-16)
Rho kinase (ROCK), one of the serine/threonine kinases, is involved in pathologic conditions, and its activation causes neuronal cell death. Fasudil, a selective ROCK inhibitor, has been reported to cause increased cerebral blood flow (CBF) in the ischemic brain and
Seungjun Lee et al.
Microcirculation (New York, N.Y. : 1994), 15(5), 379-387 (2008-06-25)
Reductions in retinal blood flow are observed early in diabetes. Venules may influence arteriolar constriction and flow; therefore, we hypothesized that diabetes would induce the constriction of arterioles that are in close proximity to venules, with the constriction mediated by
Min-ho Kim et al.
Microvascular research, 73(2), 150-155 (2006-12-13)
This study addresses the role of venule-derived mediators in the arteriolar constriction that accompanies hypercholesterolemia. Constriction was assessed by measuring the tone of small arterioles closely paired with venules in the mesentery of normal cholesterol rats (NC), high cholesterol rats
Yoshio Suzuki et al.
Neurologia medico-chirurgica, 48(6), 241-247 (2008-06-25)
Sub-analysis of the fasudil post-marketing surveillance study compared the safety and efficacy of fasudil plus ozagrel to fasudil only. A total of 3690 patients received fasudil and 1138 received fasudil plus ozagrel between 1995 and 2000. The occurrence of adverse
K Shinagawa et al.
British journal of pharmacology, 131(2), 266-270 (2000-09-19)
1. The purpose of this study was to investigate the involvement of thromboxane A(2) (TXA(2)) in the cough response in a guinea-pig cough model. Here, we describe results obtained using a selective TXA(2) synthetase inhibitor, ozagrel, and a selective TXA(2)

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