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galacto-Dapagliflozin Sale

目录号 : GC17190

A potent inhibitor of hSGLT2

galacto-Dapagliflozin Chemical Structure

Cas No.:1408245-02-2

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1mg
¥778.00
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5mg
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10mg
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50mg
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Sample solution is provided at 25 µL, 10mM.

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产品描述

Ki = 2 nM

galacto-Dapagliflozin is a potent inhibitor of human SGLT2.

Renal glucose transport is mediated by sodium-glucose cotransporters (SGLT) 1 and 2. In humans, SGLT2 is responsible for the majority of glucose reabsorption in the kidney.

In vitro: It was found that galacto-dapagliflozin was a selective inhibitor of hSGLT2, but was less potent than dapagliflozin for both transporters. Both phlorizin and galacto-dapagliflozin rapidly dissociated from SGLT2, while dapagliflozin and fluoro-dapagliflozin dissociated from hSGLT2 at a rate 10-fold slower. Dapagliflozin, fluoro-dapagliflozin, and galacto-dapagliflozin dissociated quickly from hSGLT1, and phlorizin readily exchanged with dapagliflozin bound to hSGLT1 [1].

In vivo: Male db/db mice were administered dapagliflozin for 12 weeks. Results showed that administration of dapagliflozin could ameliorate hyperglycemia, β-cell damage and albuminuria in db/db mice. Serum creatinine, creatinine clearance and blood pressure were not affected by administration of dapagliflozin. Dapagliflozin treatment was able to decrease macrophage infiltration in the kidney of db/db mice [2].

Clinical trial: Previous clinical study found that lowering the plasma glucose concentration with dapagliflozin could markedly improve β-cell function, which provided strong support for the glucotoxic effect of hyperglycemia on β-cell function [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] Terami N et al.  Long-term treatment with the sodium glucose cotransporter 2 inhibitor, dapagliflozin, ameliorates glucose homeostasis and diabetic nephropathy in db/db mice. PLoS One. 2014 Jun 24;9(6):e100777.
[3] Merovci A et al.  Dapagliflozin lowers plasma glucose concentration and improves β-cell function. J Clin Endocrinol Metab. 2015 May;100(5):1927-32.

Chemical Properties

Cas No. 1408245-02-2 SDF
化学名 (1S)-1,5-anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-D-galactitol
Canonical SMILES ClC(C=CC([C@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O1)=C2)=C2CC3=CC=C(OCC)C=C3
分子式 C21H25ClO6 分子量 408.9
溶解度 ≤30mg/ml in DMSO;50mg/ml in dimethyl formamide 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.4456 mL 12.2279 mL 24.4559 mL
5 mM 0.4891 mL 2.4456 mL 4.8912 mL
10 mM 0.2446 mL 1.2228 mL 2.4456 mL
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