fluoro-Dapagliflozin

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CAS NO:

1181681-43-5

包装与价格：

包装	价格(元)
5mg	询价
10mg	询价
50mg	询价

化学性质

Physical Appearance	A crystalline solid
Storage	Store at -20°C
M.Wt	410.9
Cas No.	1181681-43-5
Formula	C₂₁H₂₄ClFO₅
Synonyms	flouro-DAPA
Solubility	≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide
Chemical Name	(1S)-1,5-anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-4-deoxy-4-fluoro-D-glucitol
Canonical SMILES	ClC(C=CC([C@H]1[C@H](O)[C@@H](O)[C@H](F)[C@@H](CO)O1)=C2)=C2CC3=CC=C(OCC)C=C3
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

Ki: 5.3 and 330 nM for SGLT2 and SGLT1, respectively

fluoro-Dapagliflozin is a selective sodium-glucose cotransporter (SGLT) inhibitor.

Human Na(+)-D-glucose cotransporter (hSGLT) inhibitors constitute the newest class of diabetes drugs, blocking up to in-vivo 50% of renal glucose reabsorption.

In vitro: Dapagliflozin and fluoro-dapagliflozin could block glucose transport and glucose-coupled currents with around 100-fold specificity for hSGLT2 over hSGLT1. It was found that phlorizin and galacto-dapagliflozin rapidly dissociated from SGLT2, while fluoro-dapagliflozin dissociated from hSGLT2 at a rate 10-fold slower. In contrast, fluoro-dapagliflozin could quickly dissociate from hSGLT1 [1].

In vivo: Dapagliflozin, the close analog of fluoro-dapagliflozin, could acutely induce renal glucose excretion in normal and diabetic rats, improve glucose tolerance in normal rats, and reduce hyperglycemia in Zucker diabetic fatty at doses ranging from 0.1 to 1.0 mg/kg. Moreover, the once-daily dapagliflozin treatment was able to significantly lower fasting and fed glucose levels and led to a significant increase in glucose utilization rate [2].

Clinical trial: Clinical study found that dapagliflozin could lower hyperglycemia in treatment-naive patients with newly diagnosed type 2 diabetes, which made dapagliflozin a unique addition to existing treatment options for type 2 diabetes [3].

References:
[1] Hummel, C. S.,Lu, C.,Liu, J., et al. Structural selectivity of human SGLT inhibitors. American Journal of Physiology.Cell Physiology 302(2), C373-C382 (2012).
[2] Han, S. ,Hagan, D.L.,Taylor, J.R., et al. Dapagliflozin, a selective SGLT2 inhibitor, improves glucose homeostasis in normal and diabetic rats. Diabetes 57, 1723-1729 (2008).
[3] Ferrannini E, Ramos SJ, Salsali A, Tang W, List JF. Dapagliflozin monotherapy in type 2 diabetic patients with inadequate glycemic control by diet and exercise: a randomized, double-blind, placebo-controlled, phase 3 trial. Diabetes Care. 2010 Oct;33(10):2217-24.