|1-(2,4-二羟基-6-(((2S,3R,4S,5S,6R)-3,4,5-三羟基-6-(羟甲基)四氢-2H-吡喃-2-基)氧基)苯基)-3-(4-羟基苯基)丙-1-酮|CsnPharm

CAS No.: 60-81-1

Phlorizin/根皮苷 Catalog No. CSN11698

Synonyms: 根皮苷;Floridzin;Phlorizoside

Phlorizin is an inhibitor of hSGLT1 (Ki=300 nM) and hSGLT2 (Ki= 39 nM). It can be found in a number of fruit trees.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 SGLT1

Ki:300nM SGLT2

Ki:39nM
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 K_i 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].
动物研究
剂量
Rat: 5 mg/kg - 20 mg/kg^[3] (i.v.); 50 mg/kg - 200 mg/kg^[3] (p.o.); 100 mg/kg^[4] (s.c., b.i.d.) Mice: 400 mg/kg^[5] (s.c.)

给药途径
i.v., p.o., s.c.
临床研究

动物研究
剂量	Rat: 5 mg/kg - 20 mg/kg^[3] (i.v.); 50 mg/kg - 200 mg/kg^[3] (p.o.); 100 mg/kg^[4] (s.c., b.i.d.) Mice: 400 mg/kg^[5] (s.c.)
给药途径	i.v., p.o., s.c.

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... more >>esity Collapse <<	Not Applicable	Completed	-	-
NCT02088853	Healthy Conditions	Not Applicable	Completed	-	Sweden ... more >> Dept of Gastrosurgical R&E, Sahlgrenska Universityhospital Gothenburg, Sweden, SE41345 Collapse <<

参考文献

[1] Hummel CS, Lu C, et al. Structural selectivity of human SGLT inhibitors. Am J Physiol Cell Physiol. 2012;302(2):C373-82.
[2] Ghezzi C, Loo DDF, Wright EM. Physiology of renal glucose handling via SGLT1, SGLT2 and GLUT2. Diabetologia. 2018;61(10):2087-2097.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2914 mL
- 11.4571 mL
- 22.9142 mL
- 5 mM
- 0.4583 mL
- 2.2914 mL
- 4.5828 mL
- 10 mM
- 0.2291 mL
- 1.1457 mL
- 2.2914 mL

技术信息

CAS号

60-81-1

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H24O10

运输

蓝冰

分子量

436.41

别名

根皮苷;Floridzin;Phlorizoside;Phlorrhizin

溶解度

DMSO	85.0 mg/mL (194.8 mM) warming
Water	Insoluble
Ethanol	87.0 mg/mL (199.4 mM) warming

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

靶点	Description	IC50
SGLT1		Ki:300nM
SGLT2		Ki:39nM

Phlorizin/根皮苷 Catalog No. CSN11698

靶点选择性

请登录您的专属账户

确认信息