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GSK837149A
产品别名
13616-29-0
GSK837149A
N,N′-Di[4-(4-Methyl-pyrimidin-2-ylsulfamoyl)phenyl]-urea
基本信息
Empirical Formula【经验(实验)分子式】 | C23H22N8O5S2 |
Molecular weight | 554.60 |
NACRES | NA.77 |
Biochem/physiol Actions【生化/生理作用】 | GSK837149A is the first selective inhibitor of human fatty acid synthase (FAS) known to act specifically and selectively on the KR activity of the enzyme. It was first isolated as a minor impurity in a sample found to be active against the enzyme in a high-throughput screening campaign. This compound and its analogs synthesized, all being symmetrical structures containing a bisulfonamide urea, act by inhibiting the beta-ketoacyl reductase activity of the enzyme. GSK837149A inhibits FAS in a reversible mode, with a Ki value of approximately 30 nm, and it possibly binds to the enzyme-ketoacyl-ACP complex. Although initial results suggest that cell penetration for these compounds is impaired, they still can be regarded as useful tools with which to probe and explore the beta-ketoacyl reductase active site in FAS, helping in the design of new inhibitors. |
Features and Benefits【特点和优势】 | This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here. |
产品性质
Quality Level【质量水平】 | 100 |
Assay【测定】 | ≥98% (HPLC) |
form【形式】 | solid |
color【颜色】 | white to off-white |
solubility【溶解性】 | DMSO: >10 mg/mL H2O: insoluble |
originator【创始人】 | GlaxoSmithKline |
storage temp.【储存温度】 | 2-8℃ |
packaging【包装】 | 5, 25 mg in glass bottle |
安全信息
Pictograms【象形图】 | GHS07 |
Signal word【警示用语:】 | Warning |
Hazard Statements | H319 |
Precautionary Statements | P305 + P351 + P338 |
Hazard Classifications【危险分类】 | Eye Irrit. 2 |
Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
WGK | WGK 2 |
Personal Protective Equipment【个人防护装备】 | dust mask type N95 (US), Eyeshields, Gloves |