Tetramethylpyrazine

Synonyms: ligustrazine

Tetramethylpyrazine (ligustrazine, TMP) is a natural compound isolated from Chinese herbal medicine Ligusticum wallichii (Chuan Xiong) with anti-inflammation, antioxidant, antiplatelet, and antiapoptosis activities.

Tetramethylpyrazine Chemical Structure

Tetramethylpyrazine Chemical Structure

CAS: 1124-11-4

Selleck's Tetramethylpyrazine has been cited by 1 publication

Purity & Quality Control

Batch: S395601 Ethanol] 100 mg/mL] false] DMSO] 27 mg/mL] false] Water] 8 mg/mL] true Purity: 99.96%
99.96

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Biological Activity

Description Tetramethylpyrazine (ligustrazine, TMP) is a natural compound isolated from Chinese herbal medicine Ligusticum wallichii (Chuan Xiong) with anti-inflammation, antioxidant, antiplatelet, and antiapoptosis activities.
Targets
PDE [3]
In vitro
In vitro Tetramethylpyrazine (TMP) is described as "calcium antagonist" and produces a vasodilation effect via inhibiting Ca2+ influx and the release of intracellular Ca2+ at first. TMP could restrain mitochondrial ROS generation and upregulate the expression of PGC1, NRF1, and Tfam, which reflects mitochondrial biogenesis. TMP also exerts an endothelium protective property via downregulating the expression of ICAM-1 and HSP60. TMP can exert antiapoptosis ability by inhibiting macrophage COX-2. TMP can restrain LPS-induced IL-8 overexpression in HUVECs at both the protein and mRNA levels, which is possibly due to blocking the activation of the NF-kB-dependent pathway; the involvement of ERK and p38 MAPK signaling pathway has also been observed[1].
Cell Research Cell lines HL-60 cells
Concentrations 300 µg/mL
Incubation Time 24, 48, 60, 72 h
Method

Cell viability is determined by the MTT assay. HL-60 cells are treated with 300 µg/mL TMP, 0.5 µM As2O3, and 300 µg/mL TMP combined with 0.5 µM As2O3, respectively.

In Vivo
In vivo Akt and the endothelial isoform of nitric oxide synthase (eNOS) phosphorylation are significantly upregulated after Tetramethylpyrazine (TMP) pretreatment in vivo. TMP can suppress the proliferation of VSMC in rabbit aortic vascular. TMP can decrease the ANP mRNA expression in cardiomyocyte hypertrophy rat model and suppress the level of pJAK2, pJAK1, or pSTAT3, demonstrating that TMP can inhibit JAK-STAT signal transduction. TMP is reported to possess a broad spectrum of pharmacological effects, such as antioxidant, anti-inflammatory, antifibrosis effects. Early pharmacokinetic research has determined the metabolism rate of TMP and verified its in-vivo short half-life of T1/2=2.89 h[1]. TMP is found to protect ischemic brain damage, and promote cell proliferation and differentiation stimulated by ischemia[2].
Animal Research Animal Models A rat model of Parkinson's disease induced by MPTP (Wistar rats)
Dosages 20 mg/kg/d
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06122701 Not yet recruiting
Healthy
University Medicine Greifswald
November 20 2023 Not Applicable
NCT06025396 Active not recruiting
Cocaine Use Disorder|Substance Use Disorders|Healthy Volunteers
Tempero Bio Inc.|National Institute on Drug Abuse (NIDA)
January 6 2023 Phase 1
NCT05509595 Recruiting
Fibrous Dysplasia Of Bone
National Institute of Dental and Craniofacial Research (NIDCR)|National Institutes of Health Clinical Center (CC)
December 7 2022 Phase 2
NCT05357573 Active not recruiting
Tumor-Induced Osteomalacia (TIO)
Kyowa Kirin Co. Ltd.
September 7 2022 Phase 4

Chemical Information & Solubility

Molecular Weight 136.19 Formula

C8H12N2

CAS No. 1124-11-4 SDF Download Tetramethylpyrazine SDF
Storage (From the date of receipt)

In vitro
Batch:

Ethanol : 100 mg/mL

DMSO : 27 mg/mL ( (198.25 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 8 mg/mL


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