Description
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.
Product information
CAS Number: 2402772-45-4
Molecular Weight: 474.87
Formula: C22H18ClF3N6O
Chemical Name: N'-[(1E)-(4-chlorophenyl)methylidene]-4-{[3-(trifluoromethyl)phenyl]amino}-5H,6H,7H,8H-pyrido[4,3-d]pyrimidine-6-carbohydrazide
Smiles: O=C(N/N=C/C1C=CC(Cl)=CC=1)N1CC2=C(NC3=CC(=CC=C3)C(F)(F)F)N=CN=C2CC1
InChiKey: VHRNHTUEITYZIH-VPUKRXIYSA-N
InChi: InChI=1S/C22H18ClF3N6O/c23-16-6-4-14(5-7-16)11-29-31-21(33)32-9-8-19-18(12-32)20(28-13-27-19)30-17-3-1-2-15(10-17)22(24,25)26/h1-7,10-11,13H,8-9,12H2,(H,31,33)(H,27,28,30)/b29-11+
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 250 mg/mL (526.46 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
ATX inhibitor 5 (compound 10g) (IC50s=1.21 and 0.78 μM) displays activities against cardiac fibroblasts (CFs) and hepatic stellate cell (HSC). ATX inhibitor 5 at 10 μM successfully suppresses collagen content induced by TGF-β.
In Vivo:
ATX inhibitor 5 (20-40 mg/kg; p.o.; once daily for two weeks) reduces CCl4-induced hepatic fibrosis level prominently.
Products are for research use only. Not for human use.
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