Dapagliflozin (2S)-1,2-propanediol hydrate
CAS No. 960404-48-2
Dapagliflozin (2S)-1,2-propanediol hydrate( BMS-512148 | BMS512148 | BMS 512148 )
Catalog No. M16859 CAS No. 960404-48-2
A potent, selective, orally active hSGLT2 inhibitor with EC50 of 1.12 nM.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 5MG | 39 | In Stock |
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| 10MG | 55 | In Stock |
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| 25MG | 67 | In Stock |
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| 50MG | 84 | In Stock |
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| 100MG | 105 | In Stock |
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| 500MG | 255 | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NameDapagliflozin (2S)-1,2-propanediol hydrate
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NoteResearch use only, not for human use.
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Brief DescriptionA potent, selective, orally active hSGLT2 inhibitor with EC50 of 1.12 nM.
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DescriptionA potent, selective, orally active hSGLT2 inhibitor with EC50 of 1.12 nM; displays >300-fold selectivity over hSGLT1 (EC50=330 nM), highly selectivity versus GLUT transporters; also is a potent selective inhibitor of rSGLT2 (EC50=3 nM), with 200-fold selectivity versus rSGLT1; significantly improves glucose homeostasis, reduces blood glucose levels in hyperglycemic streptozotocin (STZ) rats.Diabetes Approved(In Vitro):Dapagliflozin ((2S)-1,2-propanediol, hydrate) (0-10 μM; 24 hours) significantly increases the cell survival in hypoxic HK2 cell in a dose-dependent manner.Dapagliflozin ((2S)-1,2-propanediol, hydrate) (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.
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In VitroDapagliflozin ((2S)-1,2-propanediol, hydrate) (0-10 μM; 24 hours) significantly increases the cell survival in hypoxic HK2 cell in a dose-dependent manner.Dapagliflozin ((2S)-1,2-propanediol, hydrate) (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. Cell Viability Assay Cell Line:Hypoxic HK2 cell 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 Cell Line:Hypoxic HK2 cell, 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.
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In Vivo——
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SynonymsBMS-512148 | BMS512148 | BMS 512148
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PathwayGPCR/G Protein
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TargetSGLT
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RecptorSGLT2
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Research AreaMetabolic Disease
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IndicationDiabetes
Chemical Information
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CAS Number960404-48-2
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Formula Weight502.9823
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Molecular FormulaC24H35ClO9
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Purity>98% (HPLC)
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Solubility10 mM in DMSO
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SMILESCCOC1=CC=C(C=C1)CC2=C(C=CC(=C2)C3C(C(C(C(O3)CO)O)O)O)Cl.CC(CO)O.O
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Chemical NameD-Glucitol, 1,5-anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-, (1S)-, compd. with (2S)-1,2-propanediol, hydrate (1:1:1)
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Meng W, et al. J Med Chem. 2008 Mar 13;51(5):1145-9.
2. Han S, et al. Diabetes. 2008 Jun;57(6):1723-9.
3. Wilson C. Nat Rev Endocrinol. 2010 Oct;6(10):531.
4. Komoroski B, et al. Clin Pharmacol Ther. 2009 May;85(5):513-9.
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