A potent inhibitor of hSGLT2
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Product Type

Small Molecule Modulators
Transporter & Exchanger Modulators

Research Area

fluoro-Dapagliflozin

Item No. 15951

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(1S)-1,5-anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-4-deoxy-4-fluoro-D-glucitol
CAS Number
1181681-43-5
Synonyms
  • flouro-DAPA
Molecular Formula
C21H24ClFO5
Formula Weight
410.9
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlEthanol:PBS(pH 7.2) (1:1): 0.5 mg/ml
λmax
224 nm
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
InChi Code
InChI=1S/C21H24ClFO5/c1-2-27-15-6-3-12(4-7-15)9-14-10-13(5-8-16(14)22)21-20(26)19(25)18(23)17(11-24)28-21/h3-8,10,17-21,24-26H,2,9,11H2,1H3/t17-,18-,19+,20-,21+/m1/s1
InChi Key
VYRXTNZYAGBKPS-ADAARDCZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    50 mg

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    Product Description

    Dapagliflozin (Item No. 11574) is a selective sodium-glucose cotransporter (SGLT) inhibitor that blocks glucose transport with about 100-fold selectivity for SGLT2 (Ki = 6 nM; EC50 = 1.1 nM) over SGLT1 (Ki = 390 nM).1,2 It improves glucose tolerance in normal rats and reduces hyperglycemia in Zucker diabetic fatty rats.3fluoro-Dapagliflozin is an analog of dapagliflozin that displays similar selectivity for inhibiting SGLT2 over SGLT1 (Kis = 5.3 and 330 nM, respectively).1 fluoro-Dapagliflozin (10 nM) significantly reduces phlorizin-sensitive sugar transport in COS-1 cells expressing human SGLT2.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hummel, C.S., Lu, C., Liu, J., et al. Structural selectivity of human SGLT inhibitors. Am. J. Physiol. Cell Physiol. 302(2), C373-C382 (2012).

    2. Chao, E.C., and Henry, R.R. SGLT2 inhibition - A novel strategy for diabetes treatment. Nat. Rev. Drug Discov. 9(7), 551-559 (2010).

    3. 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(6), 1723-1729 (2008).