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Terevalefim

Product Name
Terevalefim
CAS No.
1070881-42-3
Chemical Name
Terevalefim
Synonyms
Terevalefim;Terevalefim(ANG-3777);(E)-3-(2-(thiophen-2-yl)vinyl)-1H-pyrazole;1H-Pyrazole, 3-[(1E)-2-(2-thienyl)ethenyl]-;3-[(E)-2-(thiophen-2-yl)ethenyl]-2H-pyrazole;ANG-3777,Terevalefim,injury,acute,inhibit,ANG 3777,AKI,kidney,ANG3777,transplantation,c-Met/HGFR,HGF,Inhibitor
CBNumber
CB54868672
Molecular Formula
C9H8N2S
Formula Weight
176.24
MOL File
1070881-42-3.mol
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Terevalefim Property

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)
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Hazard and Precautionary Statements (GHS)

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Terevalefim Chemical Properties,Usage,Production

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

Raw materials

Preparation Products

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Terevalefim Suppliers

TargetMol Chemicals Inc.
Tel
+1-781-999-5354
Email
support@targetmol.com
Country
United States
ProdList
19973
Advantage
58

1070881-42-3, TerevalefimRelated Search:


  • (E)-3-(2-(thiophen-2-yl)vinyl)-1H-pyrazole
  • 1H-Pyrazole, 3-[(1E)-2-(2-thienyl)ethenyl]-
  • 3-[(E)-2-(thiophen-2-yl)ethenyl]-2H-pyrazole
  • Terevalefim
  • Terevalefim(ANG-3777)
  • ANG-3777,Terevalefim,injury,acute,inhibit,ANG 3777,AKI,kidney,ANG3777,transplantation,c-Met/HGFR,HGF,Inhibitor
  • 1070881-42-3