Company Name: |
ChemeGen(Shanghai) Biotechnology Co.,Ltd.
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Tel: |
18818260767 |
Email: |
sales@chemegen.com |
Products Intro: |
Product Name:KT203 CAS:1402612-64-9 Purity:98% Package:10 mg;50 mg;100 mg;500 mg;1 g;5 g;10 g
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Company Name: |
MedBioPharmaceutical Technology Inc
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Tel: |
021-69568360 18916172912 |
Email: |
order@med-bio.cn |
Products Intro: |
Product Name:4′-[1-[[2-(Phenylmethyl)-1-piperidinyl]carbonyl]-1H-1,2,3-triazol-4-yl]-[1,1′-biphenyl]-3-carboxylic acid CAS:1402612-64-9 Purity:98% Package:10mg; 5mg Remarks:Medbio
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| 4′-[1-[[2-(Phenylmethyl)-1-piperidinyl]carbonyl]-1H-1,2,3-triazol-4-yl]-[1,1′-biphenyl]-3-carboxylic acid Basic information |
Product Name: | 4′-[1-[[2-(Phenylmethyl)-1-piperidinyl]carbonyl]-1H-1,2,3-triazol-4-yl]-[1,1′-biphenyl]-3-carboxylic acid | Synonyms: | 4′-[1-[[2-(Phenylmethyl)-1-piperidinyl]carbonyl]-1H-1,2,3-triazol-4-yl]-[1,1′-biphenyl]-3-carboxylic acid;KT203;4′-(1-(2-benzylpiperidine-1-carbonyl)-1H-1,2,3-triazol-4-yl)-[1,1′-biphenyl]-3-carboxylic acid;[1,1'-Biphenyl]-3-carboxylic acid, 4'-[1-[[2-(phenylmethyl)-1-piperidinyl]carbonyl]-1H-1,2,3-triazol-4-yl]-;KT203 >=98% (HPLC);KT-203,KT203 | CAS: | 1402612-64-9 | MF: | C28H26N4O3 | MW: | 466.53 | EINECS: | | Product Categories: | | Mol File: | 1402612-64-9.mol | |
| 4′-[1-[[2-(Phenylmethyl)-1-piperidinyl]carbonyl]-1H-1,2,3-triazol-4-yl]-[1,1′-biphenyl]-3-carboxylic acid Chemical Properties |
Boiling point | 724.3±62.0 °C(Predicted) | density | 1.28±0.1 g/cm3(Predicted) | storage temp. | Store at -20°C | solubility | ≤10mg/ml in DMSO;10mg/ml in dimethyl formamide | form | crystalline solid | pka | 4.02±0.10(Predicted) | color | White to yellow |
| 4′-[1-[[2-(Phenylmethyl)-1-piperidinyl]carbonyl]-1H-1,2,3-triazol-4-yl]-[1,1′-biphenyl]-3-carboxylic acid Usage And Synthesis |
Biological Activity | kt203 is an abhd6 inhibitor.abhd6, a unique and highly conserved enzyme in mammals, is prominently expressed in brain, liver, kidney, and brown adipose tissue based on global gene expression analysis and activitybased protein profiling (abpp). | in vitro | the in-vitro potency of kt203 was studied and it was found that kt203 was able to potently inhibit abhd6 as measured by gelbased competitive abpp and 2-ag hydrolysis assays. moreover, the in-situ potency was then measured by treating neuro2a cells with varying concentrations of kt203 for 4 h and the results showed that kt203 inhibited abhd6 with ic50 values in the subnanomolar range [1]. | in vivo | in a previous animal study, mice were treated intraperitoneally with kt203 at various doses (0.1-1 mg/kg) for 4 h. results showed that kt203 had near-complete blockade of abhd6 in the liver at the highest dose tested. at lower doses, kt203 showed about 80% inhibition of abhd6 in the liver. notably, kt203 exhibited impressive selectivity in the mouse liver even at higher doses, showing little cross-reactivity against the numerous carboxylesterase enzymes that are common off-targets of mechanism-based sh inhibitors in rodents. in addition, kt203 showed good selectivity against other brain and liver shs as judged by gelbased abpp, suggesting a single major off-target, carboxylesterase-1 (ces1) [1]. | IC 50 | < 5 nm | references | [1] hsu kl, tsuboi k, chang jw, whitby lr, speers ae, pugh h, cravatt bf. discovery and optimization of piperidyl-1,2,3-triazole ureas as potent, selective, and in vivo-active inhibitors of α/β-hydrolase domain containing 6 (abhd6). j med chem. 2013 nov 14;56(21):8270-9. |
| 4′-[1-[[2-(Phenylmethyl)-1-piperidinyl]carbonyl]-1H-1,2,3-triazol-4-yl]-[1,1′-biphenyl]-3-carboxylic acid Preparation Products And Raw materials |
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