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2402772-45-4

2402772-45-4 Structure

2402772-45-4 Structure
IdentificationBack Directory
[Name]

ATX inhibitor 5
[CAS]

2402772-45-4
[Synonyms]

ATX inhibitor 5
(E)-N'-(4-chlorobenzylidene)-4-((3-(trifluoromethyl)phenyl)amino)-7,8-dihydropyrido[4,3-d]pyrimidine-6(5H)-carbohydrazide
[Molecular Formula]

C22H18ClF3N6O
[MDL Number]

MFCD32671348
[Molecular Weight]

474.87
Chemical PropertiesBack Directory
[density ]

1.45±0.1 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

DMSO : 250 mg/mL (526.46 mM; Need ultrasonic)
[form ]

Solid
[pka]

10.89±0.20(Predicted)
[color ]

White to off-white
Hazard InformationBack Directory
[Uses]

ATX inhibitor 5 is a potent and orally active autotaxin (ATX) inhibitor, with an IC50 of 15.3 nM. ATX inhibitor 5 shows anti-hepatofibrosis effects and reduces CCl4-induced hepatic fibrosis level prominently[1].
[Biological Activity]

ATX inhibitor 5 is a potent and orally active autotaxin (ATX) inhibitor, with an IC50 of 15.3 nM. ATX inhibitor 5 shows anti-hepatofibrosis effects and reduces CCl4-induced hepatic fibrosis level prominently[1]. ATX inhibitor 5 (compound 10g) (IC50s=1.21 and 0.78 μM) displays activities against cardiac fibroblasts (CFs) and hepatic stellate cell (HSC)[1].ATX inhibitor 5 at 10 μM successfully suppresses collagen content induced by TGF-β[1]. ATX inhibitor 5 (20-40 mg/kg; p.o.; once daily for two weeks) reduces CCl4-induced hepatic fibrosis level prominently[1].
[in vivo]

ATX inhibitor 5 (20-40 mg/kg; p.o.; once daily for two weeks) reduces CCl4-induced hepatic fibrosis level prominently[1].

Animal Model:Male Konmin mice (8-week old, 22-25 g)[1]
Dosage:20, 40 mg/kg
Administration:Orally; once daily for two weeks
Result:Prominently reduced CCl4-induced hepatic fibrosis level.
[IC 50]

Autotaxin
[References]

[1]. Jiang N, et al.Optimization and evaluation of novel tetrahydropyrido[4,3-d]pyrimidine derivatives as ATX inhibitors for cardiac and hepatic fibrosis.Eur J Med Chem. 2020 Feb 1;187:111904.
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