Tetramethylpyrazine

Catalog No.S3956 Synonyms: ligustrazine

Tetramethylpyrazine Chemical Structure

Molecular Weight(MW): 136.19

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

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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

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].

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].

Protocol

Cell Research:

[4]

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  • 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.


    (Only for Reference)
Animal Research:

[2]

+ Expand
  • Animal Models: A rat model of Parkinson's disease induced by MPTP (Wistar rats)
  • Formulation: 3% DMSO
  • Dosages: 20 mg/kg/d
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 27 mg/mL (198.25 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 136.19
Formula

C8H12N2

CAS No. 1124-11-4
Storage powder
in solvent
Synonyms ligustrazine

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03993821 Not yet recruiting Drug: Burosumab Cutaneous Skeletal Hypophosphatemia Syndrome (CSHS)|Epidermal Nevus Syndrome Laura Tosi|Children''s Research Institute|Ultragenyx Pharmaceutical Inc August 2019 Early Phase 1
NCT03748966 Recruiting Drug: Calcitriol X-linked Hypophosphatemia|Hypophosphatemic Rickets|Hypophosphatemic Rickets X-Linked Dominant Massachusetts General Hospital|National Institute of Arthritis and Musculoskeletal and Skin Diseases (NIAMS) March 28 2019 Early Phase 1
NCT03920072 Recruiting Drug: Burosumab X-linked Hypophosphatemia Kyowa Kirin Pharmaceutical Development Ltd March 7 2019 Phase 3
NCT03797729 Not yet recruiting Drug: Tirofiban|Drug: Normal saline ST Elevation Myocardial Infarction Shanghai Zhongshan Hospital February 2019 Phase 4
NCT03424525 Recruiting Drug: 11C-Trimethoprim Bacterial Infections University of Pennsylvania February 1 2018 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID