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WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.
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17702719238 17702719238 |
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sales@sun-shinechem.com |
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Product Name:CRT0273750
CAS:1979939-16-6
Purity:98% HPLC Package:50.0mg;100.0mg; 200.0mg;500mg;1g;5g; 10g
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| Company Name: |
ShangHai Biochempartner Co.,Ltd
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| Tel: |
17754423994 17754423994 |
| Email: |
2853530910@QQ.com |
| Products Intro: |
Product Name:CRT0273750
CAS:1979939-16-6
Purity:98% HPLC LCMS Package:100MG;1G
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| | 3H-Imidazo[4,5-b]pyridine-2-propanamide, N-[(1S)-1-(4-chlorophenyl)ethyl]-3-[[4-(trifluoromethoxy)phenyl]methyl]- Basic information |
| Product Name: | 3H-Imidazo[4,5-b]pyridine-2-propanamide, N-[(1S)-1-(4-chlorophenyl)ethyl]-3-[[4-(trifluoromethoxy)phenyl]methyl]- | | Synonyms: | 3H-Imidazo[4,5-b]pyridine-2-propanamide, N-[(1S)-1-(4-chlorophenyl)ethyl]-3-[[4-(trifluoromethoxy)phenyl]methyl]-;CRT0273750;blood,ATX/LPA,4T1,Inhibitor,inhibit,clearance,CRT0273750,LPA;N-[1(S)-(4-Chlorophenyl)-ethyl]-3-[3-(4-trifluoromethoxybenzyl)-3H-imidazo[4,5-b]pyridin-2-yl]-propionamide | | CAS: | 1979939-16-6 | | MF: | C25H22ClF3N4O2 | | MW: | 502.92 | | EINECS: | | | Product Categories: | | | Mol File: | 1979939-16-6.mol | ![3H-Imidazo[4,5-b]pyridine-2-propanamide, N-[(1S)-1-(4-chlorophenyl)ethyl]-3-[[4-(trifluoromethoxy)phenyl]methyl]- Structure](CAS/20210305/GIF/1979939-16-6.gif) |
| | 3H-Imidazo[4,5-b]pyridine-2-propanamide, N-[(1S)-1-(4-chlorophenyl)ethyl]-3-[[4-(trifluoromethoxy)phenyl]methyl]- Chemical Properties |
| Boiling point | 680.4±55.0 °C(Predicted) | | density | 1.35±0.1 g/cm3(Predicted) | | solubility | DMSO: Soluble | | form | A solid | | pka | 14.92±0.46(Predicted) | | color | White to off-white |
| | 3H-Imidazo[4,5-b]pyridine-2-propanamide, N-[(1S)-1-(4-chlorophenyl)ethyl]-3-[[4-(trifluoromethoxy)phenyl]methyl]- Usage And Synthesis |
| Description | CRT0273750 is an autotaxin inhibitor. CRT0273750 modulates LPA levels in plasma and is suitable for in vivo studies. CRT0273750 has an unexpected binding mode in that they do not interact with the active site zinc ions but instead occupy the hydrophobic LPC pocket extending from the active site of ATX together with occupying the LPA 'exit' channel. | | in vivo | The autotaxin-lysophosphatidic acid (ATX-LPA) axis has been implicated in several disease conditions including inflammation, fibrosis and cancer. This makes ATX an attractive drug target and its inhibition may lead to useful therapeutic agents. Through a high throughput screen (HTS), a series of small molecule inhibitors of ATX have been identified, which have subsequently been optimized for potency, selectivity and developability properties. This has delivered drug-like compounds such as 9v (CRT0273750) which modulate LPA levels in plasma and are suitable for in vivo studies. X-ray crystallography has revealed that these compounds have an unexpected binding mode in that they do not interact with the active site zinc ions but instead occupy the hydrophobic LPC pocket extending from the active site of ATX together with occupying the LPA 'exit' channel._x000D_
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Reference: Shah P, Cheasty A, Foxton C, Raynham T, Farooq M, Gutierrez IF, Lejeune A, Pritchard M, Turnbull A, Pang L, Owen P, Boyd S, Stowell A, Jordan A, Hamilton NM, Hitchin JR, Stockley M, MacDonald E, Quesada MJ, Trivier E, Skeete J, Ovaa H, Moolenaar WH, Ryder H. Discovery of potent inhibitors of the lysophospholipase autotaxin. Bioorg Med Chem Lett. 2016 Nov 15;26(22):5403-5410. doi: 10.1016/j.bmcl.2016.10.036. Epub 2016 Oct 14. PMID: 27780639. | | target | Novel potent inhibitor of the lysophospholipase autotaxin |
| | 3H-Imidazo[4,5-b]pyridine-2-propanamide, N-[(1S)-1-(4-chlorophenyl)ethyl]-3-[[4-(trifluoromethoxy)phenyl]methyl]- Preparation Products And Raw materials |
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