| Identification | Back Directory | [Name]
iGOT1-01 | [CAS]
882256-55-5 | [Synonyms]
iGOT1-01
1-Piperazinecarboxamide, 4-(1H-indol-4-yl)-N-phenyl- | [Molecular Formula]
C19H20N4O | [MDL Number]
MFCD00830676 | [MOL File]
882256-55-5.mol | [Molecular Weight]
320.39 |
| Chemical Properties | Back Directory | [Boiling point ]
620.8±55.0 °C(Predicted) | [density ]
1.314±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
13.94±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
iGOT1-01 is a potent aspartate aminotransferase 1 (glutamate oxaloacetate transaminase 1; GOT1) inhibitor. iGOT1-01 has IC50s of 85 μM and 11.3 μM in MDH coupled GOT1 enzymatic assay and GOT1/GLOX/HRP assay, respectively. iGOT1-01 has anti-cancer activity[1][2]. | [in vivo]
iGOT1-01 (compound 1a; 20 mg/kg; oral) has reasonable bioavailability and exposure properties (t1/2=0.7 hours, Cmax=4133 ng/mL, AUC(0-24 hours)=11734 hour?ng/mL)[1].
| Animal Model: | Female CD1 mice with 9 weeks old[1] | | Dosage: | 20 mg/kg (Pharmacokinetic Analysis) | | Administration: | Oral | | Result: | Has reasonable bioavailability and exposure properties (t1/2=0.7 hours, Cmax=4133 ng/mL, AUC(0-24 hours)=11734 hour?ng/mL). |
| [References]
[1] Justin Anglin, et al. Discovery and optimization of aspartate aminotransferase 1 inhibitors to target redox balance in pancreatic ductal adenocarcinoma. Bioorg Med Chem Lett. 2018 Sep 1;28(16):2675-2678. DOI:10.1016/j.bmcl.2018.04.061
[2] Melissa C Holt, et al. Biochemical Characterization and Structure-Based Mutational Analysis Provide Insight into the Binding and Mechanism of Action of Novel Aspartate Aminotransferase Inhibitors. Biochemistry. 2018 Nov 27;57(47):6604-6614. DOI:10.1021/acs.biochem.8b00914 |
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| Company Name: |
DC Chemicals
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| Tel: |
021-58447131 13564518121 |
| Website: |
www.chemicalbook.com/showsupplierproductslist927327/0_en.htm |
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