| Identification | Back 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 Properties | Back 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 Information | Back Directory | [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]. | [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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