Cat. No.: HY-N0935

Ligustrazine hydrochloride

(Synonyms: Chuanxiongzine hydrochloride; Tetramethylpyrazine hydrochloride)

11 Cited Publications

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Based on 11 publication(s) in Google Scholar

Ligustrazine hydrochloride is an orally active, blood-brain barrier-permeable alkaloid. It can be isolated from Ligusticum striatum DC. Ligustrazine hydrochloride reduces ROS, upregulates the levels of p-Akt/Akt and p-eNOS/eNOS, and decreases ALT and AST. It inhibits glutamate excitotoxicity, calcium overload, oxidative stress, ischemia-reperfusion injury and atherosclerotic plaque progression, enhances synaptic plasticity, and improves neurological function, cerebral infarct volume and brain water content. Ligustrazine hydrochloride possesses anti-inflammatory, antioxidant, lipid-lowering, endothelial protective and hepatoprotective activities. It can be used in studies related to ischemic stroke, cerebral ischemia-reperfusion injury and atherosclerosis.

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Pureté: 99.93%
CAS No.: 76494-51-4
Formule: C₈H₁₂N₂.xHCl

Stockage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Ligustrazine hydrochloride Chemical Structure

CAS No.: 76494-51-4

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (11)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Calculators
Help & FAQs
Bioz

Activité biologique

Description

IC₅₀ & Target^[2]

eNOS

Voir tous les produits spécifiques à Isoform Akt :

Voir tous les produits spécifiques à Isoform NO Synthase :

Voir tous les produits spécifiques à Isoform Aminotransferases (Transaminases) :

In Vitro

Ligustrazine (1-100 μM) hydrochloride dose-dependently increases NO production in OGD-treated human amniotic epithelial cells by activating the PI3K/Akt pathway, with no significant effect on NO production in normal HAECs^[2].
Ligustrazine (0.1-10 μM) hydrochloride dose-dependently increases p-Akt/Akt and p-eNOS/eNOS in OGD-treated human amniotic epithelial cells by activating the PI3K/Akt pathway, with no significant effect on these factors in normal HAECs^[2].
Ligustrazine hydrochloride protects endothelial cells against LDL-induced damage in an in vitro cell-based system^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Ligustrazine (10-120 mg/kg; intraperitoneal injection; intravenous injection; oral administration) hydrochloride exerts protective effects on rat models of ischemic stroke, significantly improves neurological function, reduces the levels of brain injury markers, regulates inflammatory and oxidative stress pathways, inhibits cell apoptosis, and repairs blood-brain barrier permeability^[1].
Ligustrazine (20 mg/kg; i.p.; 15 min after model establishment) hydrochloride improves neurological function in male C57BL/6 mouse models of ischemic stroke^[1].
Ligustrazine (1-10 mg/kg; i.p.; administered once at 2 h and 12 h post-operation) hydrochloride protects Wistar rats against cerebral ischemia-reperfusion injury in a dose-dependent manner by activating the PI3K/Akt pathway, which increases the levels of p-Akt and p-eNOS, improves neurological function, and alleviates brain tissue damage^[2].
Ligustrazine (20-80 mg/kg; p.o.; 6 weeks) hydrochloride dose-dependently inhibits the progression of atherosclerosis and hepatic lipid accumulation in Sprague-Dawley rats, with the daily oral dose of 80 mg/kg reducing the aortic lesion area by 49.0% compared with the untreated atherosclerotic control group^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Wistar rats^[2]
Dosage:

1 mg/kg; 3 mg/kg; 10 mg/kg
Administration:

i.p.; twice (at 2 hours and 12 hours after operation)
Result:

Increased brain tissue levels of p-Akt (normalized to Akt) in a dose-dependent manner.
Increased brain tissue levels of p-eNOS (normalized to eNOS) in a dose-dependent manner.
Significantly improved neurological deficits compared to I/R-only rats.
Dose-dependently alleviated brain cell shrinkage, nuclear deep staining, edema, and necrosis induced by I/R injury.
Had its protective effects reversed by pre-treatment with the PI3K inhibitor wortmannin.

Animal Model:

Sprague-Dawley (male, SPF grade, ~200 g at study start, induced via vitamin D3 injection and atherogenic diet)^[3]
Dosage:

20 mg/kg; 80 mg/kg
Administration:

p.o.; daily; 6 weeks
Result:

Decreased total cholesterol by 65.2%, triglycerides by 53.2%, LDL by 71.2%, and slightly increased HDL at 20 mg/kg dose.
Decreased total cholesterol by 76.7%, triglycerides by 77.9%, LDL by 79.0%, and slightly increased HDL at 80 mg/kg dose.
Decreased circulating endothelial cells by 42.2% at 20 mg/kg dose.
Decreased circulating endothelial cells by 60.0% at 80 mg/kg dose.
Decreased ALT by 13.0% and AST by 10.7% at 20 mg/kg dose.
Decreased ALT by 49.7% and AST by 14.3% at 80 mg/kg dose.
Restored total antioxidant capacity and SOD1 activity at both doses.
Decreased MDA generation by 12.8% at 20 mg/kg dose.
Decreased MDA generation by 23.8% at 80 mg/kg dose.
Reduced thoracic aorta lesion area by 18.9% relative to atherosclerotic controls at 20 mg/kg dose.
Reduced thoracic aorta lesion area by 49.0% relative to atherosclerotic controls at 80 mg/kg dose.
Reduced hepatic lipid accumulation, reversed elevated hepatic TG and LDL levels, and restored reduced hepatic HDL levels at both doses.
Dose-dependently inhibited the induction of antioxidant genes (pgc-1α, sod1, catalase, gpx-1) in the aorta and liver, and suppressed mRNA expression of hepatic fatty acid oxidation genes (pgc-1α, pparα, cpt1a) at both doses.

Chemical Information

CAS No. 76494-51-4
Appearance Solid
Formule C₈H₁₂N₂.xHCl
Color White to off-white
SMILES

CC1=C(C)N=C(C)C(C)=N1.[x HCl]
Synonyms

Chuanxiongzine hydrochloride; Tetramethylpyrazine hydrochloride
Structure Classification
- Alkaloids
- Other Alkaloids
Initial Source
- Plants
- Umbelliferae
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (11)

All Histological Imaging/StainingIn Vivo ImagingELISAIn Vivo Efficacy StudyCell Imaging/StainingCell Proliferation/Viability Assay

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Antioxidants (Basel)

Dopamine D2 Receptor Activation Blocks GluA2/ROS Positive Feedback Loop to Alienate Chronic-Migraine-Associated Pain Sensitization. [Abstract]

2024 Jun 14;13(6):725. PMID: 38929165
Biochem Pharmacol

Tetramethylpyrazine ameliorates sepsis-induced liver injury via inhibiting ferroptosis. [Abstract]

2025 Jul 26:241:117193. PMID: 40721008

Ligustrazine hydrochloride purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2025 Jul 26:241:117193. [Abstract]

Ligustrazine (TMP, 25-100 mg/kg; i.p.; once daily for 7 days) can ameliorate liver injury in septic mice: Pathological changes in liver tissues of mice in each group, yellow arrows: hepatic cords; black arrows: hepatocytes. H&E staining results showed that in the Sham group, the liver tissues were structurally intact and morphologically normal, with no cell necrosis; in the CLP group, hepatocytes were swollen and necrotic, and hepatic cords were disorganized, accompanied by extensive inflammatory cell infiltration; compared with the CLP group, liver tissue damage in the CLP + XBJ, CLP + TMP L (25 mg/kg), CLP + TMP M (50 mg/kg), and CLP + TMP H (100 mg/kg) groups was significantly improved, hepatic cord structure was restored, and inflammatory cell infiltration was reduced, with the most significant improvement in the CLP + XBJ and CLP + TMP H groups.

Ligustrazine hydrochloride purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2025 Jul 26:241:117193. [Abstract]

Effects of Ligustrazine (TMP, 25-100 mg/kg; i.p.; once daily for 7 days) on serum levels of IL-6, TNF-α, and IL-10 in septic mice.
Eur J Pharmacol

Tetramethylpyrazine ameliorates 5-fluorouracil-Induced cardiotoxicity by inhibiting PANoptosis and suppressing the p38 MAPK/JNK/ERK signaling pathway. [Abstract]

2025 Sep 17:178180. PMID: 40973012

Ligustrazine hydrochloride purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2025 Sep 17:178180. [Abstract]

Representative M-mode echocardiograms. Echocardiographic analysis revealed that Ligustrazine (TMP, 60 mg/kg; i.p.; once daily for 10 days) treatment significantly improved 5-FU (20 mg/kg; i.p.; once daily for 10 days)-induced cardiac dysfunction in BALB/c mice.

Ligustrazine hydrochloride purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2025 Sep 17:178180. [Abstract]

Morphological analysis showed that Ligustrazine (TMP, 60 mg/kg; i.p.; once daily for 10 days) attenuated 5-FU (20 mg/kg; i.p.; once daily for 10 days)-induced reductions in heart size, and significantly restored HW/TL ratio in BALB/c mice.

Ligustrazine hydrochloride purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2025 Sep 17:178180. [Abstract]

Representative images of cardiac tissue with HE staining. Images were taken at 40 × and 400 ×. HE staining revealed that Ligustrazine (TMP, 60 mg/kg; i.p.; once daily for 10 days) significantly ameliorated 5-FU (20 mg/kg; i.p.; once daily for 10 days)-induced cardiomyocyte disarray, inflammatory cell infiltration, and histological disruptions in BALB/c mice.

Ligustrazine hydrochloride purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2025 Sep 17:178180. [Abstract]

Representative micrographs were taken at 100 × magnification with a scale bar of 100 μm. Ligustrazine (TMP, 12.5 μM; 48 h) treatment significantly reversed the reduction in cell density induced by 5-FU (10 μM; 48 h).

Ligustrazine hydrochloride purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2025 Sep 17:178180. [Abstract]

Ligustrazine (TMP) (6.25-100 μM; 48 h) alone exhibited no cytotoxic effects on H9C2 cells. Co-treatment with TMP (12.5–50 μM; 48 h) significantly reversed the suppression of cell viability induced by 10 μM 5-FU.
Cell Signal

Tetramethylpyrazine protects against myocardial ischemia/reperfusion injury via regulating Myl2-mediated NLRP3 signaling pathway inhibition. [Abstract]

2025 Nov:135:112045. PMID: 40754120
Regen Ther

Therapeutic effects of Tetramethylpyrazine on Cartilage in Rat Model of Post-traumatic Osteoarthritis. [Abstract]

2026 Mar 7:32:101098. PMID: 41852452
Exp Cell Res

Tetramethylpyrazine inhibits neutrophil extracellular traps formation and alleviates hepatic ischemia/reperfusion injury in rat liver transplantation. [Abstract]

2021 Sep 1;406(1):112719. PMID: 34273405
Chem Biol Drug Des

Tetramethylpyrazine Targets HDAC6-Mediated PINK1 Degradation to Alleviate Chronic Intermittent Hypoxia-Induced Injury in Human Bronchial Epithelial Cells (16HBE). [Abstract]

2026 Jan;107(1):e70236. PMID: 41549472
Clin Exp Pharmacol Physiol

Ligustrazine and liguzinediol protect against doxorubicin-induced cardiomyocytes injury by inhibiting mitochondrial apoptosis and autophagy. [Abstract]

2023 Nov;50(11):867-877. PMID: 37574718
Vascular

Ligustrazine activate the PPAR-γ pathway and play a protective role in vascular calcification. [Abstract]

2022 Dec;30(6):1224-1231. PMID: 34670463
Research Square Print

November 8th, 2022
Research Square Print

October 11th, 2022.

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 100 mg/mL (Need ultrasonic)

View the Complete Stock Solution Preparation Table

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL; Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL; Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL; Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS

Solubility: 100 mg/mL; Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage
mg/kg
Animal Weight (Per Animal)
g
Dosing Volume (Per Animal)
μL
Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact

MedChemExpress (MCE) .

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (283 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
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MS (2659 KB)
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IR (2659 KB)
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OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Wang Z, et al. The protective effects of ligustrazine on ischemic stroke: a systematic review and meta-analysis of preclinical evidence and possible mechanisms. Front Pharmacol. 2024;15:1373663. Published 2024 Mar 13. [Content Brief]

[2]. Ding Y, et al. The protective effect of ligustrazine on rats with cerebral ischemia-reperfusion injury via activating PI3K/Akt pathway. Hum Exp Toxicol. 2019;38(10):1168-1177. [Content Brief]

[3]. Jiang F, et al. Ligustrazine improves atherosclerosis in rat via attenuation of oxidative stress. Pharm Biol. 2011;49(8):856-863. [Content Brief]

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1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Ligustrazine hydrochloride

11 Cited Publications

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Ligustrazine hydrochloride

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Publications Citing Use of MedChemExpress (MCE) Ligustrazine hydrochloride

Voir tous les produits spécifiques à Isoform Akt

Voir tous les produits spécifiques à Isoform NO Synthase

Voir tous les produits spécifiques à Isoform Aminotransferases (Transaminases)

Activité biologique

Chemical Information

Publications (11)

Solvant et solubilité

Pureté et documentation

Références

Calculators

Help & FAQs

Ligustrazine hydrochloride Related Classifications