Tetramethylpyrazine

Catalog No.S3956 Synonyms: ligustrazine

For research use only.

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

CAS No. 1124-11-4

Purity & Quality Control

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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

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 (from reference)

Cell Research:

[4]

  • 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]

  • Animal Models: A rat model of Parkinson's disease induced by MPTP (Wistar rats)
  • 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 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(N=C(C(=N1)C)C)C

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04960384 Not yet recruiting Drug: FGF-2|Drug: Placebo Tympanic Membrane Perforation NYU Langone Health August 2021 Phase 2
NCT04842032 Not yet recruiting Drug: KRN23 X-linked Hypophosphatemia (XLH) Kyowa Kirin Co. Ltd. May 2021 Phase 4
NCT04842019 Not yet recruiting Drug: KRN23 X-linked Hypophosphatemia (XLH) Kyowa Kirin Co. Ltd. May 2021 Phase 4
NCT04695860 Recruiting Drug: Burosumab X-linked Hypophosphatemia Wuerzburg University Hospital|Kyowa Kirin January 7 2021 Phase 3

(data from https://clinicaltrials.gov, updated on 2021-09-06)

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