| Company Name: |
TargetMol Chemicals Inc.
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| Tel: |
4008200310 |
| Email: |
marketing@tsbiochem.com |
| Products Intro: |
Product Name:Terevalefim;ANG-3777,Terevalefim,injury,acute,inhibit,ANG 3777,AKI,kidney,ANG3777,transplantation,c-Met/HGFR,HGF,Inhibitor
CAS:1070881-42-3
Purity:98% Package:1 mL;10 mg;100 mg;2 mg;200 mg;25 mg;5 mg;50 mg;500 mg;
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| Company Name: |
Shanghai?Medlife?Pharm-Tech?Co.,?Ltd
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| Tel: |
021-59167510 18117107507 |
| Email: |
vip@med-life.cn |
| Products Intro: |
Product Name:Terevalefim
CAS:1070881-42-3
Purity:>=99% Package:50mg;100mg;10mM*1mLinDMSO;5mg;25mg;10mg;200mg
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| | Terevalefim Basic information |
| Product Name: | Terevalefim | | Synonyms: | Terevalefim;3-[(E)-2-(thiophen-2-yl)ethenyl]-2H-pyrazole;1H-Pyrazole, 3-[(1E)-2-(2-thienyl)ethenyl]-;(E)-3-(2-(thiophen-2-yl)vinyl)-1H-pyrazole;Terevalefim（ANG-3777）;ANG-3777,Terevalefim,injury,acute,inhibit,ANG 3777,AKI,kidney,ANG3777,transplantation,c-Met/HGFR,HGF,Inhibitor | | CAS: | 1070881-42-3 | | MF: | C9H8N2S | | MW: | 176.24 | | EINECS: | | | Product Categories: | | | Mol File: | 1070881-42-3.mol |  |
| | Terevalefim Chemical Properties |
| Boiling point | 369.3±11.0 °C(Predicted) | | density | 1.318±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO : 100 mg/mL (567.41 mM; Need ultrasonic) | | pka | 14.05±0.10(Predicted) |
| | Terevalefim Usage And Synthesis |
| Description | Terevalefim (ANG-3777) is a hepatocyte growth factor (HGF) mimetic that in preclinical and phase 2 studies has demonstrated the ability to activate the c-Met receptor and the pathways associated with that activation, improving renal function in induced-AKI in animals and long-term graft function occurring in renal transplantation recipients with signs of DGF[1-2]. | | Biological Functions | ANG-3777 (Terevalefim) is an HGF mimetic that in vitro induces the same c-Met cascades and cellular effects as endogenous HGF. In animals, ANG-3777 stimulates tubular repair and regeneration, resulting in improved renal function following ischemia reperfusion injury. In humans, ANG-3777 has been shown to improve renal function up to 1 year after kidney transplantation in patients with signs of delayed graft function[1]. | | in vitro | In vitro, ANG-3777 reduces apoptosis and increases cell proliferation, migration, morphogenesis, and angiogenesis in injured kidneys. In animal models, ANG-3777 mitigates the effects of renal damage secondary to ischemia reperfusion injury and nephrotoxic chemicals[1]. | | in vivo | In vivo, Terevalefim results in dimerization and phosphorylation, and thus activation of the c-Met receptor, followed by activation of c-Met signaling cascades. The presence of c-Met is needed for ANG-3777 activity, and ANG-3777 selectively phosphorylates c-Met. Furthermore, c-Met phosphorylation induced by ANG-3777 occurs in a dose- and time-dependent manner with selective phosphorylation of c-Met and its downstream effector of ERK. No phosphorylation of IFGR, Tie2, EGFR, or FGFR occurs[2]. | | References | [1] Ayad S, et al. Hepatocyte Growth Factor Mimetic ANG-3777 for Cardiac Surgery–Associated Acute Kidney Injury. Kidney International Reports, 2020; 5: 2325–2332.
[2] Vincenti F, et al. Phase 3 trial design of the hepatocyte growth factor mimetic ANG-3777 in renal transplant recipients with delayed graft function. Kidney International Reports, 2021; 6: 296-303. |
| | Terevalefim Preparation Products And Raw materials |
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