Cat. No.: HY-10450

Dapagliflozin

(Synonyms: BMS-512148)

68 Cited Publications

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Based on 68 publication(s) in Google Scholar

Dapagliflozin (BMS-512148), a new type of agent used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine. Dapagliflozin induces HIF1 expression and attenuates renal IR injury.

For research use only. We do not sell to patients.

Purity: 99.95%
CAS No.: 461432-26-8
Formula: C₂₁H₂₅ClO₆
Molecular Weight:408.87

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Dapagliflozin Chemical Structure

CAS No.: 461432-26-8

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (68)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
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Biological Activity

Description

Dapagliflozin (BMS-512148), a new type of agent used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine^[1]. Dapagliflozin induces HIF1 expression and attenuates renal IR injury^[2].

IC₅₀ & Target

SGLT2

All SGLT Isoforms :

SGLT1
SGLT2

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	1.1 nM Compound: 6, dapagliflozin	Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]AMG accumulation Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]AMG accumulation	[PMID: 18260618]
CHO	EC₅₀	1390 nM Compound: 6, dapagliflozin	Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of [14C]AMG accumulation Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of [14C]AMG accumulation	[PMID: 18260618]
CHO	EC₅₀	3 nM Compound: 6, dapagliflozin	Inhibition of rat SGLT2 expressed in CHO cells assessed as inhibition of [14C]AMG accumulation Inhibition of rat SGLT2 expressed in CHO cells assessed as inhibition of [14C]AMG accumulation	[PMID: 18260618]
CHO	IC₅₀	1.4 nM Compound: 2	Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of sodium-dependent methyl-alpha-D-[U-14C]glucopyranoside uptake after 2 hrs Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of sodium-dependent methyl-alpha-D-[U-14C]glucopyranoside uptake after 2 hrs	[PMID: 20149653]
CHO	IC₅₀	1200 nM Compound: 2	Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of sodium-dependent methyl-alpha-D-[U-14C]glucopyranoside uptake after 2 hrs Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of sodium-dependent methyl-alpha-D-[U-14C]glucopyranoside uptake after 2 hrs	[PMID: 20149653]
CHO	IC₅₀	0.49 nM Compound: 9	Inhibition of human recombinant SGLT2 expressed in CHO cells by liquid scintillation counting Inhibition of human recombinant SGLT2 expressed in CHO cells by liquid scintillation counting	[PMID: 20181486]
CHO	IC₅₀	0.49 nM Compound: 1	Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting	[PMID: 20434909]
CHO	EC₅₀	3 nM Compound: 5	Inhibition of human SGLT2 expressed in CHO cells assessed as sodium-dependent [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting Inhibition of human SGLT2 expressed in CHO cells assessed as sodium-dependent [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting	[PMID: 21128592]
CHO	EC₅₀	428.5 nM Compound: 5	Inhibition of human SGLT1 expressed in CHO cells assessed as sodium-dependent [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting Inhibition of human SGLT1 expressed in CHO cells assessed as sodium-dependent [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting	[PMID: 21128592]
CHO	IC₅₀	0.49 nM Compound: 1	Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting	[PMID: 21193308]
CHO	IC₅₀	0.004 μM Compound: 2	Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]-alpha-methyl-D-glucopyranoside transport after 60 mins by scintillation counting Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]-alpha-methyl-D-glucopyranoside transport after 60 mins by scintillation counting	[PMID: 21398124]
CHO	IC₅₀	0.022 μM Compound: 2	Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]-alpha-methyl-D-glucopyranoside transport after 60 mins by scintillation counting in presence of 100% plasma Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]-alpha-methyl-D-glucopyranoside transport after 60 mins by scintillation counting in presence of 100% plasma	[PMID: 21398124]
CHO	IC₅₀	0.37 μM Compound: 2	Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of [14C]-alpha-methyl-D-glucopyranoside transport after 60 mins by scintillation counting Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of [14C]-alpha-methyl-D-glucopyranoside transport after 60 mins by scintillation counting	[PMID: 21398124]
CHO	IC₅₀	0.38 μM Compound: 2	Inhibition of SGLT6 expressed in CHO cells assessed as inhibition of [14C]-alpha-methyl-D-glucopyranoside transport after 60 mins by scintillation counting Inhibition of SGLT6 expressed in CHO cells assessed as inhibition of [14C]-alpha-methyl-D-glucopyranoside transport after 60 mins by scintillation counting	[PMID: 21398124]
CHO	IC₅₀	0.49 nM Compound: 1	Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counter Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counter	[PMID: 21514014]
CHO	IC₅₀	3 nM Compound: Dapagliflozin	Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]-Glucose uptake using [14C]-methyl glucopyranoside after 60 mins by microbeta plate counting Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of [14C]-Glucose uptake using [14C]-methyl glucopyranoside after 60 mins by microbeta plate counting	[PMID: 21565497]
CHO	IC₅₀	1.35 nM Compound: 1	Inhibition of human SGLT2 expressed in CHO cells using methyl-alpha-D-glucopyranoside by liquid scintillation counting Inhibition of human SGLT2 expressed in CHO cells using methyl-alpha-D-glucopyranoside by liquid scintillation counting	[PMID: 21592794]
CHO	IC₅₀	1.35 nM Compound: Dapagliflozin	Inhibition of human SGLT2 expressed in CHO cells assessed as reduction of [14C]-labeled AMG after 2 hrs by liquid scintillation counting Inhibition of human SGLT2 expressed in CHO cells assessed as reduction of [14C]-labeled AMG after 2 hrs by liquid scintillation counting	[PMID: 21868239]
CHO	IC₅₀	0.49 nM Compound: Dapagliflozin	Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting	[PMID: 21906953]
CHO	IC₅₀	1.3 nM Compound: 4	Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of sodium-dependent [14C]methyl-alpha-D-glucopyranoside uptake after 45 mins Inhibition of human SGLT2 expressed in CHO cells assessed as inhibition of sodium-dependent [14C]methyl-alpha-D-glucopyranoside uptake after 45 mins	[PMID: 22889351]
CHO	IC₅₀	800 nM Compound: 4	Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of sodium-dependent [14C]methyl-alpha-D-glucopyranoside uptake after 45 mins Inhibition of human SGLT1 expressed in CHO cells assessed as inhibition of sodium-dependent [14C]methyl-alpha-D-glucopyranoside uptake after 45 mins	[PMID: 22889351]
CHO	IC₅₀	0.49 nM Compound: 1	Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting Inhibition of human SGLT2 expressed in CHO cells assessed as [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting	[PMID: 24900297]
CHO	IC₅₀	5 nM Compound: 12	Competitive inhibition of full-length human SGLT2 expressed in CHO cells assessed as inhibition of sodium-dependent [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by scintillation counting Competitive inhibition of full-length human SGLT2 expressed in CHO cells assessed as inhibition of sodium-dependent [14C]-alpha-methyl-D-glucopyranoside uptake after 2 hrs by scintillation counting	[PMID: 25650254]
CHO-K1	IC₅₀	1.3 nM Compound: 3	Inhibition of human SGLT2 expressed in CHO-K1 cells by [14C]AMG uptake assay Inhibition of human SGLT2 expressed in CHO-K1 cells by [14C]AMG uptake assay	[PMID: 22652255]
CHO-K1	IC₅₀	800 nM Compound: 3	Inhibition of human SGLT1 expressed in CHO-K1 cells by [14C]AMG uptake assay Inhibition of human SGLT1 expressed in CHO-K1 cells by [14C]AMG uptake assay	[PMID: 22652255]
CHO-K1	EC₅₀	2.4 nM Compound: 12	Inhibition of human SGLT2 expressed in CHO-K1 cells incubated for 120 mins at 37 degC by [14C]-AMG uptake assay Inhibition of human SGLT2 expressed in CHO-K1 cells incubated for 120 mins at 37 degC by [14C]-AMG uptake assay	[PMID: 22818040]
CHO-K1	EC₅₀	593 nM Compound: 12	Inhibition of human SGLT1 expressed in CHO-K1 cells incubated for 120 mins at 37 degC by [14C]-AMG uptake assay Inhibition of human SGLT1 expressed in CHO-K1 cells incubated for 120 mins at 37 degC by [14C]-AMG uptake assay	[PMID: 22818040]
CHO-K1	IC₅₀	1 nM Compound: 1	Inhibition of human SGLT2 expressed in CHOK1 cells assessed as inhibition of [14C]-AMG uptake after 3 hrs by microbeta scintillation counting analysis Inhibition of human SGLT2 expressed in CHOK1 cells assessed as inhibition of [14C]-AMG uptake after 3 hrs by microbeta scintillation counting analysis	[PMID: 24842618]
CHO-K1	IC₅₀	891 nM Compound: 1	Inhibition of human SGLT1 expressed in CHOK1 cells assessed as inhibition of [14C]-AMG uptake after 3 hrs by microbeta scintillation counting analysis Inhibition of human SGLT1 expressed in CHOK1 cells assessed as inhibition of [14C]-AMG uptake after 3 hrs by microbeta scintillation counting analysis	[PMID: 24842618]
COS-7	IC₅₀	885 nM Compound: 1	Inhibition of human SGLT1 expressed in african green monkey COS7 cells assessed as methyl-alpha-D-[U-14C]glucopyranoside uptake by scintillation counting Inhibition of human SGLT1 expressed in african green monkey COS7 cells assessed as methyl-alpha-D-[U-14C]glucopyranoside uptake by scintillation counting	[PMID: 19700318]
COS-7	IC₅₀	0.89 μM Compound: 2	Inhibition of human SGLT1 transfected in COS-7 cells assessed as AMG uptake after 2 hrs by scintillation counting Inhibition of human SGLT1 transfected in COS-7 cells assessed as AMG uptake after 2 hrs by scintillation counting	[PMID: 19896374]
COS-7	IC₅₀	0.89 μM Compound: 1	Inhibition of human SGLT1 expressed in african green monkey COS7 cells assessed as inhibition of [14C]alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting Inhibition of human SGLT1 expressed in african green monkey COS7 cells assessed as inhibition of [14C]alpha-methyl-D-glucopyranoside uptake after 2 hrs by liquid scintillation counting	[PMID: 20576578]
COS-7	IC₅₀	3.2 nM Compound: 1	Inhibition of human SGLT2 expressed in african green monkey COS7 cells assessed as inhibition of [14C]-methyl-alpha-D-glucopyranoside uptake after 2 hrs by scintillation counting in presence of 25 % human plasma Inhibition of human SGLT2 expressed in african green monkey COS7 cells assessed as inhibition of [14C]-methyl-alpha-D-glucopyranoside uptake after 2 hrs by scintillation counting in presence of 25 % human plasma	[PMID: 21737266]
HEK293	IC₅₀	810 nM Compound: 4	Inhibition of human SGLT1 expressed in HEK293 cells assessed as inhibition of [14C]alpha-methylglucopyranoside uptake Inhibition of human SGLT1 expressed in HEK293 cells assessed as inhibition of [14C]alpha-methylglucopyranoside uptake	[PMID: 19785435]
HEK293	IC₅₀	6.7 nM Compound: 1	Inhibition of human SGLT2 expressed in HEK293 cells assessed as inhibition of [14C]alpha-methyl-D-glucopyranoside uptake after 1.5 hrs by liquid scintillation counting Inhibition of human SGLT2 expressed in HEK293 cells assessed as inhibition of [14C]alpha-methyl-D-glucopyranoside uptake after 1.5 hrs by liquid scintillation counting	[PMID: 20576578]
HEK293	IC₅₀	3100 nM Compound: 1	Inhibition of human SGLT1 expressed in human 293 cells assessed as inhibition of [14C]-methyl-alpha-D-glucopyranoside uptake after 1.5 hrs by scintillation counting in presence of 25 % human plasma Inhibition of human SGLT1 expressed in human 293 cells assessed as inhibition of [14C]-methyl-alpha-D-glucopyranoside uptake after 1.5 hrs by scintillation counting in presence of 25 % human plasma	[PMID: 21737266]
HEK293	IC₅₀	1.8 μM Compound: 4a	Inhibition of human SGLT1 expressed in HEK293 cells assessed as reduction in 2-deoxyglucose uptake pretreated for 10 mins followed by 2-deoxyglucose addition in presence of sodium buffer measured after 1 hr by resazurin dye based fluorescence assay Inhibition of human SGLT1 expressed in HEK293 cells assessed as reduction in 2-deoxyglucose uptake pretreated for 10 mins followed by 2-deoxyglucose addition in presence of sodium buffer measured after 1 hr by resazurin dye based fluorescence assay	[PMID: 28098449]
HEK293	IC₅₀	0.0008 μM Compound: 4a	Inhibition of human SGLT2 expressed in HEK293 cells assessed as reduction in 2-deoxyglucose uptake pretreated for 10 mins followed by 2-deoxyglucose addition in presence of sodium buffer measured after 1 hr by resazurin dye based fluorescence assay Inhibition of human SGLT2 expressed in HEK293 cells assessed as reduction in 2-deoxyglucose uptake pretreated for 10 mins followed by 2-deoxyglucose addition in presence of sodium buffer measured after 1 hr by resazurin dye based fluorescence assay	[PMID: 28098449]
HEK293	IC₅₀	0.8 nM Compound: 4a	Inhibition of human SGLT2 expressed in HEK293 cells assessed as reduction in 2-deoxyglucose uptake pretreated for 10 mins followed by 2-deoxyglucose addition in presence of sodium buffer measured after 1 hr by resazurin dye based fluorescence assay Inhibition of human SGLT2 expressed in HEK293 cells assessed as reduction in 2-deoxyglucose uptake pretreated for 10 mins followed by 2-deoxyglucose addition in presence of sodium buffer measured after 1 hr by resazurin dye based fluorescence assay	[PMID: 28098449]
NIH3T3	IC₅₀	12.3 μM Compound: 2	Inhibition of human full length SGLT1 expressed in NIH3T3 cells measured after 1 hr in presence of [14C]-methyl-alpha -D-glucopyranoside by scintillation counter method Inhibition of human full length SGLT1 expressed in NIH3T3 cells measured after 1 hr in presence of [14C]-methyl-alpha -D-glucopyranoside by scintillation counter method	[PMID: 31325786]
NIH3T3	IC₅₀	8.3 nM Compound: 2	Inhibition of human full length SGLT2 expressed in NIH3T3 cells measured after 1 hr in presence of [14C]-methyl-alpha -D-glucopyranoside by scintillation counter method Inhibition of human full length SGLT2 expressed in NIH3T3 cells measured after 1 hr in presence of [14C]-methyl-alpha -D-glucopyranoside by scintillation counter method	[PMID: 31325786]

In Vitro

Dapagliflozin (0-10 μM；24 hours) significantly increases the cell survival in hypoxic HK2 cell in a dose-dependent manner^[2].
Dapagliflozin (0-10 μM；2 hours) increases the HIF1 expression, increases AMPK and EKR phosphorylation in hypoxic HK2 cells, but shows no effect on the phosphorylation of AMPK and ERK in normoxic HK2 cells^[2]..

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

Hypoxic HK2 cells
Concentration:

0 μM, 1 μM, 2 μM, 5 μM, 10 μM
Incubation Time:

24 hours
Result:

Improved the cell viability in a dose-dependent manner compared with control cells.

Western Blot Analysis^[1]

Cell Line:

Hypoxic HK2 cells, Normoxic HK2 cells
Concentration:

0 μM, 1 μM, 2 μM, 5 μM, 10 μM
Incubation Time:

24 hours
Result:

Induced HIF1 expression in hypoxic and normoxic HK2 cells.

In Vivo

Dapagliflozin (oral administration; 10 mg/kg) causes a marked increase in urinary glucose in SGLT2i-mice, suppresses BAT thermogenesis by reducing sympathetic nerve activity and enhances hepatic gluconeogenesis and glycogenolysis^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 461432-26-8
Appearance Solid
Molecular Weight 408.87
Formula C₂₁H₂₅ClO₆
Color White to off-white
SMILES

O[C@H]1[C@H](C2=CC(CC3=CC=C(OCC)C=C3)=C(Cl)C=C2)O[C@H](CO)[C@@H](O)[C@@H]1O
Synonyms

BMS-512148
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (68)

All WBCell Proliferation/Viability AssayIF

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Journal Impact Factor

Nat Commun

IDH2 lactylation promotes angiogenesis in murine diabetic myocardial infarction via blocking Cav1-eNOS interaction. [Abstract]

2025 Dec 19. PMID: 41419771
Cardiovasc Res

Off-target effects of sodium-glucose co-transporter 2 blockers: empagliflozin does not inhibit Na+/H+ exchanger-1 or lower [Na+]i in the heart. [Abstract]

2021 Dec 17;117(14):2794-2806. PMID: 33135077
EBioMedicine

Liver autophagy-induced valine and leucine in plasma reflect the metabolic effect of sodium glucose co-transporter 2 inhibitor dapagliflozin. [Abstract]

2022 Dec:86:104342. PMID: 36423374

Dapagliflozin purchased from MedChemExpress. Usage Cited in: EBioMedicine. 2022 Dec:86:104342. [Abstract]

Dapagliflozin increases the LC3-II to LC3-I expression ratio in the liver.
Cell Rep Med

The SGLT2 inhibitor dapagliflozin ameliorates renal fibrosis in hyperuricemic nephropathy. [Abstract]

2024 Aug 20;5(8):101690. PMID: 39168099
Cardiovasc Diabetol

Effect of extracellular matrix stiffness on efficacy of Dapagliflozin for diabetic cardiomyopathy. [Abstract]

2024 Jul 24;23(1):273. PMID: 39049086
Adv Healthc Mater

Ultrasound-Triggered Nanobubbles for Endothelial-Targeted Drug Delivery in the Detection and Treatment of Doxorubicin-Induced Cardiotoxicity. [Abstract]

2026 Apr;15(16):e05898. PMID: 41691418
Cell Commun Signal

Inhibition of SGLT2 protects podocytes in diabetic kidney disease by rebalancing mitochondria-associated endoplasmic reticulum membranes. [Abstract]

2024 Nov 7;22(1):534. PMID: 39511548
Acta Pharmacol Sin

SGLT2 inhibitors ameliorate NAFLD in mice via downregulating PFKFB3, suppressing glycolysis and modulating macrophage polarization. [Abstract]

2024 Dec;45(12):2579-2597. PMID: 39294445
Acta Pharmacol Sin

Dapagliflozin attenuates pressure overload-induced myocardial remodeling in mice via activating SIRT1 and inhibiting endoplasmic reticulum stress. [Abstract]

2022 Jul;43(7):1721-1732. PMID: 34853445
Phytomedicine

The natural compound stachyose targets SGLT2-mediated metabolic reprogramming to ameliorate diabetic kidney disease. [Abstract]

2025 Aug 19:147:157182. PMID: 40848672
Free Radic Biol Med

Dapagliflozin attenuates diabetes-induced podocyte lipotoxicity via ERRα-Mediated lipid metabolism. [Abstract]

2025 Apr 19:S0891-5849(25)00238-2. PMID: 40258521
Biomed Pharmacother

Xelaglifam, a novel GPR40/FFAR1 agonist, exhibits enhanced β-arrestin recruitment and sustained glycemic control for type 2 diabetes. [Abstract]

2024 Jun 27:177:117044. PMID: 38941892
Biomed Pharmacother

Central administration of Dapagliflozin alleviates a hypothalamic neuroinflammatory signature and changing tubular lipid metabolism in type 2 diabetic nephropathy by upregulating MCPIP1. [Abstract]

2023 Dec:168:115840. PMID: 37931516
Biomed Pharmacother

Dapagliflozin attenuates myocardial hypertrophy via activating the SIRT1/HIF-1α signaling pathway. [Abstract]

2023 Sep:165:115125. PMID: 37421782
Biomed Pharmacother

Canagliflozin mitigates carfilzomib-induced endothelial apoptosis via an AMPK-dependent pathway. [Abstract]

2023 Aug:164:114907. PMID: 37247463
NPJ Regen Med

Intrinsic muscle stem cell dysfunction underlies functional deficits in models of type 1 diabetes. [Abstract]

2026 Jan 6;11(1):8. PMID: 41495072
Cell Mol Life Sci

Dapagliflozin targets SGLT2/SIRT1 signaling to attenuate the osteogenic transdifferentiation of vascular smooth muscle cells. [Abstract]

2024 Nov 9;81(1):448. PMID: 39520538
Biochem Pharmacol

The SGLT2 inhibitor dapagliflozin suppresses endothelial cell pyroptosis mediated by the NF-κB/NLRP3 pathway through downregulation of CTSB. [Abstract]

2025 Jun:236:116857. PMID: 40058708
Biochem Pharmacol

Canagliflozin exerts anti-inflammatory effects by inhibiting intracellular glucose metabolism and promoting autophagy in immune cells. [Abstract]

2018 Jun:152:45-59. PMID: 29551587

Dapagliflozin purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2018 Jun:152:45-59. [Abstract]

Effects of Dapagliflozin and Empagliflozin on p62 expression in LPS-untreated and LPS-treated RAW264.7 cells.
Food Funct

Resveratrol attenuates dapagliflozin-induced renal gluconeogenesis via activating the PI3K/Akt pathway and suppressing the FoxO1 pathway in type 2 diabetes. [Abstract]

2021 Feb 15;12(3):1207-1218. PMID: 33432947
Life Sci

Dapagliflozin attenuates post-infarction fibrosis via cardiomyocyte protection and fibroblast inhibition. [Abstract]

2025 Dec 15:383:124083. PMID: 41224193
Life Sci

Dapagliflozin delays renal fibrosis in diabetic kidney disease by inhibiting YAP/TAZ activation. [Abstract]

2023 Jun 1:322:121671. PMID: 37023953

Dapagliflozin purchased from MedChemExpress. Usage Cited in: Life Sci. 2023 Jun 1:322:121671. [Abstract]

Dapagliflozin (DAPA; 10, 20 μM; 24 h) significantly reverses the decrease in cell viability caused by high glucose in HK-2 cells.

Dapagliflozin purchased from MedChemExpress. Usage Cited in: Life Sci. 2023 Jun 1:322:121671. [Abstract]

Dapagliflozin (DAPA; 10 μM; 24 hours) significantly reduces the high glucose-induced increase in YAP/TAZ expression in HK-2 cells.

Dapagliflozin purchased from MedChemExpress. Usage Cited in: Life Sci. 2023 Jun 1:322:121671. [Abstract]

Dapagliflozin (DAPA; 10 μM; 24 hours) significantly decreases the expression of YAP/TAZ and increases the ratios of p-YAP/YAP and pTAZ/TAZ under high glucose conditions in HK-2 cells.
Drug Des Devel Ther

Appropriate Dose of Dapagliflozin Improves Cardiac Outcomes by Normalizing Mitochondrial Fission and Reducing Cardiomyocyte Apoptosis After Acute Myocardial Infarction. [Abstract]

2022 Jun 28;16:2017-2030. PMID: 35789742
Nutrients

Effect of Dapagliflozin and Magnesium Supplementation on Renal Magnesium Handling and Magnesium Homeostasis in Metabolic Syndrome. [Abstract]

2021 Nov 15;13(11):4088. PMID: 34836340
Int J Mol Sci

Comparison of the Effects of Sodium-Glucose Cotransporter 2 Inhibitors on Cardiac Fibroblast Properties. [Abstract]

2025 Oct 16;26(20):10098. PMID: 41155391
J Nutr Biochem

Dapagliflozin alleviated obesity-related follicular development dysfunction by regulating glucose metabolism and mitochondria function in granulosa cells. [Abstract]

2025 Sep 22:110126. PMID: 40992636
Int J Mol Sci

Dapagliflozin Treatment Augments Bioactive Phosphatidylethanolamine Concentrations in Kidney Cortex Membrane Fractions of Hypertensive Diabetic db/db Mice and Alters the Density of Lipid Rafts in Mouse Proximal Tubule Cells. [Abstract]

2023 Jan 11;24(2):1408. PMID: 36674924
Front Pharmacol

Dapagliflozin protects against nonalcoholic steatohepatitis in db/db mice. [Abstract]

2022 Aug 19:13:934136. PMID: 36059948
Int Immunopharmacol

Dapagliflozin alleviated seizures and cognition impairment in pilocarpine induced status epilepticus via suppressing microglia-mediated neuroinflammation and oxidative stress. [Abstract]

2025 Jan 30:148:114117. PMID: 39889414
Eur J Pharmacol

Dapagliflozin attenuates steatosis in livers of high-fat diet-induced mice and oleic acid-treated L02 cells via regulating AMPK/mTOR pathway. [Abstract]

2021 Sep 15:907:174304. PMID: 34224699
Front Endocrinol

Dapagliflozin Attenuates Renal Tubulointerstitial Fibrosis Associated With Type 1 Diabetes by Regulating STAT1/TGFβ1 Signaling. [Abstract]

2019 Jul 3:10:441. PMID: 31333586
Biochim Biophys Acta Mol Basis Dis

SIRT1-PINK1-Parkin axis orchestrated mitophagy and renal repair by dapagliflozin in diabetic nephropathy. [Abstract]

2025 Oct 15;1872(2):168074. PMID: 41106506
FASEB J

SGLT2 inhibitor dapagliflozin attenuates cardiac fibrosis and inflammation by reverting the HIF-2α signaling pathway in arrhythmogenic cardiomyopathy. [Abstract]

2022 Jul;36(7):e22410. PMID: 35713937
Bioengineered

Identification of circular RNAs and functional competing endogenous RNA networks in human proximal tubular epithelial cells treated with sodium-glucose cotransporter 2 inhibitor dapagliflozin in diabetic kidney disease. [Abstract]

2022 Feb;13(2):3911-3929. PMID: 35129424
iScience

Heart failure pleural fluid impairs endothelial barrier through miR 501-3p mediated ZO 1 remodeling. [Abstract]

2026 Apr 2;29(5):115549. PMID: 42058897
J Inflamm Res

2026 Jan 6.
J Cell Physiol

Dapagliflozin Interrupts Pro-Fibroinflammatory Interleukin 11-Tenascin C Mutual Reinforcement in Fibroblasts by Antagonizing Interleukin-11 Receptor Subunit Alpha. [Abstract]

2025 Jun;240(6):e70052. PMID: 40583258
Sci Rep

Effects of Empagliflozin and Dapagliflozin in alleviating cardiac fibrosis through SIRT6-mediated oxidative stress reduction. [Abstract]

2024 Dec 28;14(1):30764. PMID: 39730461
ACS Pharmacol Transl Sci

Dapagliflozin Protects Cardiomyocytes against Doxorubicin-Induced Toxicity by Modulating Sirtuin 1/Sirtuin 3 and Ferroptosis Pathway. [Abstract]

2026 Apr 3;9(5):1134-1152. PMID: 42130718
Circ J

Acute Dapagliflozin Administration Ameliorates Cardiac Surgery-Associated Acute Kidney Injury in a Rabbit Model. [Abstract]

2024 Aug 23;88(9):1488-1498. PMID: 38658352
Heliyon

Dapagliflozin impedes endothelial cell senescence by activating the SIRT1 signaling pathway in type 2 diabetes. [Abstract]

2023 Aug 21;9(8):e19152. PMID: 37664712
Vascul Pharmacol

Hyperglycaemic impairment of PAR2-mediated vasodilation: Prevention by inhibition of aortic endothelial sodium-glucose-co-Transporter-2 and minimizing oxidative stress. [Abstract]

2018 Oct:109:56-71. PMID: 29908295
Am J Physiol Renal Physiol

Dapagliflozin ameliorates high-fat diet-induced, megalin-mediated autolysosomal dysfunction in proximal tubules via suppression of megalin-dependent endocytosis. [Abstract]

2026 Jun 1;330(6):F712-F723. PMID: 42053449
Toxicol Appl Pharmacol

Dapagliflozin regulates kynurenine metabolism and microglial activation to alleviate diabetes-associated cognitive impairment. [Abstract]

2025 Dec 24:507:117696. PMID: 41453497
Hepatol Res

Canagliflozin Alleviates Metabolic Dysfunction-Associated Steatotic Liver Disease via Mitochondrial Protection and Enhanced Mitophagy. [Abstract]

2025 Aug 23. PMID: 40847917
Hum Exp Toxicol

Effect of taxifolin/dapagliflozin combination on colistin-induced nephrotoxicity in rats. [Abstract]

2021 Oct;40(10):1767-1780. PMID: 33882723
Int J Med Sci

Susceptibility to serious skin and subcutaneous tissue disorders and skin tissue distribution of sodium-dependent glucose co-transporter type 2 (SGLT2) inhibitors. [Abstract]

2018 Jun 13;15(9):937-943. PMID: 30008607
Acta Diabetol

Dapagliflozin ameliorates metabolic and hepatic outcomes in a mouse model of metabolic dysfunction-associated steatotic liver disease and diabetes. [Abstract]

2025 May 12. PMID: 40353918
Mol Biol Rep

Dapagliflozin promotes browning of white adipose tissue through the FGFR1-LKB1-AMPK signaling pathway. [Abstract]

2024 Apr 21;51(1):562. PMID: 38644407
Iran J Basic Med Sci

Dapagliflozin improves diabetic cardiomyopathy by suppressing the STAT3-YY1 signaling axis in cardiac fibroblasts. [Abstract]

2025;28(11):1563-1574. PMID: 41170186
PLoS One

Dapagliflozin mitigates myocardial inflammation and metabolic stress in heart failure through STAT1 inhibition: Evidence from multi-omics analyses and experimental exploration. [Abstract]

2026 Feb 27;21(2):e0343296. PMID: 41758878
Chem Biodivers

Modified Citrus Pectin Alleviates Diabetic Kidney Disease by Suppressing Pyroptosis in Renal Tubular Epithelial Cells via the Cx43-ERK1/2 Signaling Pathway. [Abstract]

2025 Jun 3:e00250. PMID: 40460282
Connect Tissue Res

Dapagliflozin attenuates lipotoxic tenocyte injury via PPARα activation and irisin-driven antioxidant pathways. [Abstract]

2025 Sep 17:1-13. PMID: 40959984
Drug Res (Stuttg)

Efficacy of Mitiglinide Combined with Dapagliflozin in Streptozotocin-nicotinamide-induced Type 2 Diabetic Rats and in Zucker Fatty Rats. [Abstract]

2015 Aug;65(8):416-21. PMID: 25188606
Cell Physiol Biochem

Dapagliflozin Aggravates Renal Injury via Promoting Gluconeogenesis in db/db Mice. [Abstract]

2018;45(5):1747-1758. PMID: 29495021

Dapagliflozin purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2018;45(5):1747-1758. [Abstract]

The expression of IRS1 significantly decreases. The phosphorylation levels of Akt1, Akt2, and S6 are significantly reduced in livers of db/db mice.
Nephron

Dapagliflozin Treatment Attenuates the Interaction Between the Renal Sodium Chloride co-transporter and Ezrin in Hypertensive Diabetic db/db Mice. [Abstract]

2025 Mar 21:1-30. PMID: 40122032
Bioanalysis

A simple and rapid LC-MS/MS method for quantitation of luseogliflozin in rat plasma and its application to a PK study. [Abstract]

2017 Jan;9(2):163-171. PMID: 27960548
OPEN MED-WARSAW

The co-treatment of rosuvastatin with dapagliflozin synergistically inhibited apoptosis via activating the PI3K/AKt/mTOR signaling pathway in myocardial ischemia/reperfusion injury rats. [Abstract]

2020 Dec 11;15(1):47-57. PMID: 33385063
Res Sq

2026 Feb 4.
bioRxiv

2026 Feb 3.
bioRxiv

2025 May 19.
bioRxiv

SGLT2 inhibitors protect against diabetic cardiomyopathy and atrial fibrillation through a CaMKII independent mechanism. [Abstract]

2024 Sep 23:2024.09.23.614368. PMID: 39386626
Research Square Preprint

2023 May 30.
Research Square Print

2023 Mar 15.
Research Square Print

2022 Jul.
Oxid Med Cell Longev

Dapagliflozin Ameliorates the Formation and Progression of Experimental Abdominal Aortic Aneurysms by Reducing Aortic Inflammation in Mice. [Abstract]

2022 Jan 28:2022:8502059. PMID: 35126822
Research Square Preprint

2021 Aug.
Research Square Preprint

2021 Mar.

Solvent & Solubility

In Vitro:

DMSO : 140 mg/mL (342.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4458 mL

12.2288 mL

24.4577 mL

5 mM

0.4892 mL

2.4458 mL

4.8915 mL

10 mM

0.2446 mL

1.2229 mL

2.4458 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 3.5 mg/mL (8.56 mM); Clear solution

This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 3.5 mg/mL (8.56 mM); Clear solution

This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 3.5 mg/mL (8.56 mM); Clear solution

This protocol yields a clear solution of ≥ 3.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (35.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Pelissier T, et al. The orofacial capsaicin test in rats: effects of different capsaicin concentrations and morphine. Pain. 2002 Mar;96(1-2):81-7. [Content Brief]

[2]. Chang YK, et al. Dapagliflozin, SGLT2 Inhibitor, Attenuates Renal Ischemia-Reperfusion Injury. PLoS One. 2016 Jul 8;11(7):e0158810. [Content Brief]

[3]. Chiba Y, et al. Dapagliflozin, a Sodium-Glucose Co-Transporter 2 Inhibitor, Acutely Reduces Energy Expenditure in BAT via Neural Signals in Mice. PLoS One. 2016 Mar 10;11(3):e0150756. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4458 mL	12.2288 mL	24.4577 mL	61.1441 mL
	5 mM	0.4892 mL	2.4458 mL	4.8915 mL	12.2288 mL
	10 mM	0.2446 mL	1.2229 mL	2.4458 mL	6.1144 mL
	15 mM	0.1631 mL	0.8153 mL	1.6305 mL	4.0763 mL
	20 mM	0.1223 mL	0.6114 mL	1.2229 mL	3.0572 mL
	25 mM	0.0978 mL	0.4892 mL	0.9783 mL	2.4458 mL
	30 mM	0.0815 mL	0.4076 mL	0.8153 mL	2.0381 mL
	40 mM	0.0611 mL	0.3057 mL	0.6114 mL	1.5286 mL
	50 mM	0.0489 mL	0.2446 mL	0.4892 mL	1.2229 mL
	60 mM	0.0408 mL	0.2038 mL	0.4076 mL	1.0191 mL
	80 mM	0.0306 mL	0.1529 mL	0.3057 mL	0.7643 mL
	100 mM	0.0245 mL	0.1223 mL	0.2446 mL	0.6114 mL

Keywords

Dapagliflozin

68 Cited Publications

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Dapagliflozin

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Publications Citing Use of MedChemExpress (MCE) Dapagliflozin

All SGLT Isoforms

Biological Activity

Chemical Information

Publications (68)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Dapagliflozin Related Classifications

Cat. No.: HY-10450