产品说明书
Phlorizin
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同义名 : | 根皮甙 ;Phloridzin;Floridzin;Phlorrhizin.;Phlorizoside;Phloretin-2'-O-beta-glucoside;Phloretin 2'-glucoside;AI3-19835;phloretin-2'-β-D-glucopyranoside;NSC 2833 |
| CAS号 : | 60-81-1 | |
| 货号 : | A163609 | |
| 分子式 : | C21H24O10 | |
| 纯度 : | 98% | |
| 分子量 : | 436.409 | |
| MDL号 : | MFCD00006591 | |
| 存储条件： |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 50 mg/mL(114.57 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO H2O: 1 mg/mL(2.29 mM)，配合低频超声助溶 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Sodium-linked glucose transporters (SGLTs) is a class of membrane-associated carrier protein that carry glucose into cells. Phloridzin is an inhibitor against human SGLT1 (hSGLT1) and human SGLT2 (hSGLT2), two isoforms of SGLTs, with IC50 values of 400 and 65 nM, respectively. Also for phloridzin, the Ki values were 140 and 11 nM for hSGLT1 and hSGLT2, respectively. In hSGLT2 experiment, the half-time inhibition of 1 μM phloridzin of 100 mM glucose Na+/sugar current was 9s, and the recovery time from imbibition was 30s. In hSGLT1 experiment, 10 μM phloridzin inhibited 0.5 mM D-glucose-induced current with an on time course of 2s and a recovery time from inhibition of 10s[1]. In rats, intravenous injection of phloridzin (10 mg/kg) increased the excretion of Me-4FDG into the urinary bladder 60 min after the injection. Also, a bolus of phloridzin, which was injected 20 minutes after F-Dapa, resulted in a rapid displacement of F-Dapa to a new steady state in vivo[2]. | ||
| 作用机制 | The sugar moiety of phloridzin interacts with the glucose binding site of SGLT1 and SGLT2. The aglycone of phloridzin is also responsible for selectivity of phloridzin for SGLTs[1]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT02333461 | Overweight Ob... 展开 >>esity 收起 << | Not Applicable | Completed | - | - |
| NCT02088853 | Healthy Conditions | Not Applicable | Completed | - | Sweden ... 展开 >> Dept of Gastrosurgical R&E, Sahlgrenska Universityhospital Gothenburg, Sweden, SE41345 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.29mL 0.46mL 0.23mL |
11.46mL 2.29mL 1.15mL |
22.91mL 4.58mL 2.29mL |
| 参考文献 |
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