Product Details
| Product Name:
GSK256073 |
CAS No.:
862892-90-8 |
| Purity:
98.03% |
Supply Ability:
10g |
| Release date:
2024/11/18 |
Product Introduction
Bioactivity
| 名稱 | GSK256073 |
| 描述 | GSK256073 is an orally active GPR109A agonist. GSK256073 also is a long-lasting and non-flushing HCA2 (hydroxy-carboxylic acid receptor 2) full agonist (pEC50: 7.5). GSK256073 acutely improves glucose homeostasis via inhibition of lipolysis. |
| 體外活性 | GSK256073 (100 μM) suppresses cAMP elevation induced by isoprenaline (100 nM) in rat primary adipocytes. GSK256073 is approximately 10-fold more potent than niacin against human HCA2 (pEC50 value of 7.5 compared to 6.7 for niacin). In membranes prepared from Chinese hamster ovary cells expressing recombinant human HCA2, It has good activity versus the rat orthologue of HCA2 (pEC50 value of 6.9 compared to 6.4 for niacin) [2]. |
| 體內(nèi)活性 | GSK256073 (i.v.; 1-10 mg/kg) produces a dose-related decrease in NEFA, however, the enhanced in-ear temperature induced by 10 mg/kg i.v. GSK256073 is only 40% of that induced by 10 mg/kg i.v. niacin. GSK256073 (p.o.; 1, 30, and 100 mg/kg; in rat) displays that the fall in NEFA is of rapid onset and that the maximum is dose-related with inhibitions of 74, 81 and 88%, respectively. Although the duration was longer with a reduction of 91% still present 6 h post-dose at 10 mg/kg, triglycerides reduce is followed as a similar pattern [2]. |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 16.67 mg/mL (64.94 mM), Sonication is recommended.
|
| 關鍵字 | type 2 | GSK256073 | Inhibitor | mellitus | GSK-256073 | HM74A | HCA2 | homeostasis | GPCR | T2DM | dyslipidaemia | GSK 256073 | glucose | HCAR2 | diabete | inhibit | GPR109A | PUMA-G |
| 相關產(chǎn)品 | Vincamine | Monomethyl fumarate | Questiomycin A | 3-Hydroxyoctanoic Acid | CRTh2 antagonist 2 | Fezagepras sodium | Benzyl nicotinate | 1-methoxycyclopropanecarboxylic acid | TUG-1375 | CAY10595 | Timapiprant | NF-56-EJ40 |
| 相關庫 | 經(jīng)典已知活性庫 | 膜蛋白靶向化合物庫 | 抗糖尿病庫 | 抗癌臨床化合物庫 | 藥物功能重定位化合物庫 | 臨床期小分子藥物庫 | 已知活性化合物庫 | GPCR靶點分子庫 | 抗代謝疾病化合物庫 | 抗癌藥物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$2500.00/100mg |
VIP1Y
|
TargetMol Chemicals Inc.
|
2024-10-23 |
United States