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| | 4-Thiazoleacetamide, 2-[(cyclopropylsulfonyl)amino]-α,α-dimethyl-N-[5-[6-(trifluoromethyl)-2-pyrazinyl]-2-pyridinyl]- Basic information |
| | 4-Thiazoleacetamide, 2-[(cyclopropylsulfonyl)amino]-α,α-dimethyl-N-[5-[6-(trifluoromethyl)-2-pyrazinyl]-2-pyridinyl]- Chemical Properties |
| density | 1.55±0.1 g/cm3(Predicted) | | pka | 6.74±0.20(Predicted) | | form | Solid | | color | White to off-white |
| | 4-Thiazoleacetamide, 2-[(cyclopropylsulfonyl)amino]-α,α-dimethyl-N-[5-[6-(trifluoromethyl)-2-pyrazinyl]-2-pyridinyl]- Usage And Synthesis |
| Uses | CTP Synthetase-IN-1 is a potent, orally active cytidine 5'-triphosphate synthetase (CTPS) inhibitor with IC50s of 32 nM and 18 nM for human CTPS1 and human CTPS2, respectively. CTP Synthetase-IN-1 has anti-inflammatory effects[1]. | | in vivo | CTP Synthetase-IN-1 (compound 27; 10-50 mg/kg; p.o; twice daily; for 18 days) shows significant pharmacological responses in collagen-induced arthritis (CIA) model[1]. | Animal Model: | Mouse collagen-induced arthritis (CIA) model[1] | | Dosage: |
10 mg/kg and 50 mg/kg | | Administration: | p.o; twice daily; for 18 days | | Result: | Resulted in improvements in specific indicators of disease severity. |
| | References | [1] Andrew Novak, et al. Discovery and Optimization of Potent and Orally Available CTP Synthetase Inhibitors for Use in Treatment of Diseases Driven by Aberrant Immune Cell Proliferation. J Med Chem. 2022 Dec 22;65(24):16640-16650. DOI:10.1021/acs.jmedchem.2c01446 |
| | 4-Thiazoleacetamide, 2-[(cyclopropylsulfonyl)amino]-α,α-dimethyl-N-[5-[6-(trifluoromethyl)-2-pyrazinyl]-2-pyridinyl]- Preparation Products And Raw materials |
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