Ligustrazine Hydrochloride - CAS 76494-51-4
Catalog number: 76494-51-4
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C8H13N2Cl
Molecular Weight:
172.66
COA:
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Targets:
Others
Description:
Ligustrazine Hydrochloride is a natural product extracted from the rhizomes of Ligusticum chuanxiong Hort. It displayed a protection effect on injured ECV304 cells in vitro. It also has certain protection effect on the vascular endothelium undergoing CPB, and lower excessive activation of coagulation reaction and inflammation reaction in patients undergoing CPB.
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Purity:
98%
Appearance:
Solid powder
Synonyms:
2,3,5,6-Tetramethylpyrazine hydrochloride;Chuanxiongzine Hydrochlorid;Tetramethylpyrazine hydrochloride;Ligustrazine HCl
Solubility:
10 mM in DMSO
Storage:
-20°C Freezer
MSDS:
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Application:
Ligustrazine Hydrochloride displayed a protection effect on injured ECV304 cells in vitro. It also has certain protection effect on the vascular endothelium undergoing CPB, and lower excessive activation of coagulation reaction and inflammation reaction in patients undergoing CPB.
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Grams to Kilograms
Boiling Point:
192.7°Cat760mmHg
InChIKey:
RQKFOGXUTRDQPB-UHFFFAOYSA-N
InChI:
InChI=1S/C8H12N2.ClH/c1-5-6(2)10-8(4)7(3)9-5;/h1-4H3;1H
Canonical SMILES:
CC1=C(N=C(C(=N1)C)C)C.Cl
1.[Preparation and in vitro permeation of tetramethylpyrazine hydrochloride transdermal gel].
Tang Z1, Xu HY, Wang Q. Zhongguo Zhong Yao Za Zhi. 2013 Jul;38(13):2101-4.
The purpose of this study was to prepare tetramethylpyrazine hydrochloride transdermal gel and to study its permeation ability in vitro. The skin permeation ability was evaluated by Valian-Chien permeation cells with isolated rat skin. The concentration of tetramethylpyrazine in samples was determined by HPLC. The optimal formulation was composed with 5% azone, 5% peppermint oil, 8% sodium carboxymethylcellulose and 8% tetramethylpyrazine hydrochloride. The accumulative permeation amount of the gel was (6 731.87 +/- 102.31) microg x cm(-2) in 12 h,and the permeation rate was (535.02 +/- 33.89) microg x cm(-2) x h(-1). The release profile in vitro was in line with zero-order formulation. Tetramethylpyrazine hydrochloride gel prepared in the study would be developed as a novel transdermal preparation.
2.Tetramethylpyrazine-mediated suppression of C6 gliomas involves inhibition of chemokine receptor CXCR4 expression.
Yu K1, Chen Z, Pan X, Yang Y, Tian S, Zhang J, Ge J, Ambati B, Zhuang J. Oncol Rep. 2012 Sep;28(3):955-60. doi: 10.3892/or.2012.1866. Epub 2012 Jun 14.
Tetramethylpyrazine (TMP) is the major component extracted from the Chinese herb Chuanxiong. Increasing numbers of studies have indicated that tetramethylpyrazine hydrochloride (TMPH) has anticancer effects. However, the molecular mechanisms underlying the actions of TMPH have not been fully elucidated. In this study, using real-time RT-PCR and western blot techniques, we demonstrate that TMPH significantly downregulates the expression of the chemokine receptor CXCR4 in C6 glioma cells. Consistent with a role for CXCR4 in cancer development, TMPH inhibits the migration, proliferation and colony formation of C6 glioma cells in vitro more effectively than the CXCR4 antagonist AMD3100. Interestingly, TMPH does not affect the cell cycle when the cells are grown to 50-80% confluency but induces S-phase arrest at 100% confluency, as indicated by a significant reduction in the G1 and G2 populations.
3.Brain microdialysate, CSF and plasma pharmacokinetics of ligustrazine hydrochloride in rats after intranasal and intravenous administration.
Wang Q1, Tang Z, Zhang W. Biopharm Drug Dispos. 2013 Oct;34(7):417-22. doi: 10.1002/bdd.1854. Epub 2013 Aug 14.
The aim of this work was to investigate the pharmacokinetics of ligustrazine hydrochloride (LZH) in plasma, cerebrospinal fluid (CSF) and cerebral cortex after intranasal (10 mg/kg) or intravenous administration (10 mg/kg) in male Sprague-Dawley rats. Plasma, CSF and cerebral cortex microdialysates were collected at timed intervals for the measurement of LZH by a quick and sensitive HPLC-UV method. LZH entered the brain quickly following both routes of administration. No significant difference was observed between the AUCCSF or cortex /AUCplasma ratio of LZH after intranasal administration (38.4%, 17.4%) and that after intravenous injection (45.9%, 19.9%). The drug targeting index (DTI) was 0.85 and 0.91 in the CSF and cortex, respectively. In conclusion, LZH is rapidly absorbed into the systemic circulation following intranasal administration. There is no direct pathway for LZH transport from the nasal cavity to the brain. The rapidity and magnitude of LZH penetration into the brain indicate that intranasal administration of this agent is a promising alternative to intravenous administration.
4.[Protective effect of ligustrazine hydrochloride on homocysteine-injured ECV304 cells].
Xu D1, Wu D. Zhongguo Zhong Yao Za Zhi. 2012 Jun;37(12):1836-9.
OBJECTIVE: To detect the protective effect of ligustrazine hydrochloride on homocysteine-injured ECV304 cells.
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CAS 76494-51-4 Ligustrazine Hydrochloride

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