C5119-5mg | fluoro-Dapagliflozin [1181681-43-5] Clinisciences

Background

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.

Product Citation

1. Lin Y, Nan J, et al. "Canagliflozin impairs blood reperfusion of ischaemic lower limb partially by inhibiting the retention and paracrine function of bone marrow derived mesenchymal stem cells." EBioMedicine. 2020;52:102637. PMID:31981975

Chemical Properties

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
SDF	Download SDF
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
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Purity ≥ 95.00%

COA (Certificate Of Analysis)
MSDS (Material Safety Data Sheet)

fluoro-Dapagliflozin [1181681-43-5]

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Background

Product Citation

Chemical Properties

Quality Control