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- 详细信息
- 文献和实验
- 技术资料
- 英文名:
(2S,3R,4R,5S,6R)-2-(3-((2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)methyl)-4-ethylphenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol
- 供应商:
上海安毕达生物科技有限公司
- CAS号:
1291094-73-9
- 规格:
50μL/1mL/1mg/5mg/10mg
| 规格: | 50μL | 产品价格: | ¥249.0 |
|---|---|---|---|
| 规格: | 1mL | 产品价格: | ¥1619.0 |
| 规格: | 1mg | 产品价格: | ¥560.0 |
| 规格: | 5mg | 产品价格: | ¥1470.0 |
| 规格: | 10mg | 产品价格: | ¥2380.0 |
The sodium-glucose co-transporters (SGLTs) 1 and 2 play an important role in glucose and sodium transport in the kidneys and gastrointestinal tract. SGLT1 is expressed in the small intestine, where is needed for glucose and galactose absorption. Inhibition of SGLT1 results in glucose and galactose malabsorption1. Licogliflozin is a combined inhibitor of SGLT1 and SGLT2 and is hypothesized to further enhance the effects on renal sodium and glucose handling via inhibition of both cotransporter subtypes in the proximal renal tubule. Licogliflozin demonstrated significant weight loss (~6%) versus placebo, with favorable changes in metabolic parameters and incretin hormones. Dual inhibition of SGLT1/2 with licogliflozin in the gut and kidneys is an attractive strategy for treating obesity and diabetes2. Oral absorption of licogliflozin was rapid (tmax < 1 h) with absorption estimated at 87%, 100% and 77% in rats, dogs and humans, respectively. Excretion of licogliflozin-related radioactivity was rapid and nearly complete following oral administration with total radioactivity recovery ranging from 73% in dogs, 92.5% in humans, to 100% in rats. Elimination of licogliflozin was predominantly via metabolism with the majority of the radioactivity dose (∼54-74%) excreted as metabolites across species3.
溶解方案(细胞实验)
DMSO 中的溶解度 : 100 mg/mL (240.12 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)|H2O 中的溶解度 : 2 mg/mL (4.80 mM; 超声助溶)
溶解方案(动物实验)
"方案 一": "请依序添加每种溶剂:10% DMSO 90% (20% SBE-β-CD in Saline)Solubility: ≥ 2.5 mg/mL (6.00 mM); 澄清溶液 此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。"
"方案 二": "请依序添加每种溶剂:10% DMSO 90% Corn OilSolubility: ≥ 2.5 mg/mL (6.00 mM); 澄清溶液 此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。"
"方案 一": "请依序添加每种溶剂:PBSSolubility: 10 mg/mL (24.01 mM); 澄清溶液; 超声助溶 (<60°C)"
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文献和实验He YL, Haynes W, et al. The effects of licogliflozin, a dual SGLT1/2 inhibitor, on body weight in obese patients with or without diabetes. Diabetes Obes Metab. 2019. 21(6), 1311-1321.
Lydia Wang-Lakshman,et al. Pharmacokinetics, metabolism, and excretion of licogliflozin, a dual inhibitor of SGLT1/2, in rats, dogs, and humans. Xenobiotica. 2021. 51(4), 413-426.
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