research use only
Cat.No.S3956
| Related Targets | PD-1/PD-L1 CXCR STING AhR CD markers Interleukins Anti-infection Antioxidant COX Histamine Receptor |
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| Other Immunology & Inflammation related Inhibitors | Cl-amidine Bestatin (Ubenimex) Bindarit (AF 2838) Tranilast Tempol Sinomenine GI254023X (GI4023) ATP Geniposidic acid CORM-3 |
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In vitro |
DMSO
: 100 mg/mL
(734.26 mM)
Ethanol : 100 mg/mL Water : 4 mg/mL (超声加热五分钟,水浴60℃) |
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In vivo |
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| Molecular Weight | 136.19 | Formula | C8H12N2 |
Storage (From the date of receipt) | |
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| CAS No. | 1124-11-4 | Download SDF | Storage of Stock Solutions |
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| Targets/IC50/Ki |
PDE
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| 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.
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| 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. TMP is found to protect ischemic brain damage, and promote cell proliferation and differentiation stimulated by ischemia.
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References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06122701 | Not yet recruiting | Healthy |
University Medicine Greifswald |
November 20 2023 | Not Applicable |
| NCT06025396 | Completed | Cocaine Use Disorder|Substance Use Disorders|Healthy Volunteers |
Tempero Bio Inc.|National Institute on Drug Abuse (NIDA) |
January 6 2023 | Phase 1 |
| NCT05509595 | Active not 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 |
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