Dapagliflozin (達ge列凈; BMS-512148) 返回列表頁

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型號
HY-10450
品牌
MCE
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所在地
杭州市

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CAS號	461432-26-8	產地	國產
規(guī)格	5mg	級別	化工級
證書	ISO系列證書

CAS號

461432-26-8

產地

國產

規(guī)格

5mg

級別

化工級

證書

ISO系列證書

Dapagliflozin (Synonyms: da格列凈; BMS-512148)

Dapagliflozin (BMS-512148) 是一種競爭性葡萄糖協(xié)同轉運蛋白2 (SGLT2) 抑制劑，可導致尿液中葡萄糖的排泄，用于糖尿病 (DM) 的研究。Dapagliflozin 誘導 HIF1 表達并減輕腎臟 IR 損傷。

生物活性

Dapagliflozin (BMS-512148), a new type of drug 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^[1]

體外研究(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]..

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.

體內研究(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].

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT03074630	Amsterdam UMC, location VUmc\|Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA)	Diabetes Mellitus, Type 2\|Hypercholesterolemia	May 2016	Phase 4
NCT05429593	Novo Nordisk A+S	Healthy Volunteers	June 22, 2022	Phase 1
NCT05139914	Boston University\|American Heart Association	Diabetes Mellitus, Type 2\|Endothelial Dysfunction	May 31, 2022	Phase 4

分子量：408.87

性狀：Solid

Formula：C₂₁H₂₅ClO₆

CAS 號：461432-26-8

中文名稱：達ge列凈；達帕格列凈；達格列嗪

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

4°C, sealed storage, away from moisture

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

溶解性數(shù)據(jù)

In Vitro:

DMSO : ≥ 100 mg/mL (244.58 mM)

H₂O : 50 mg/mL (122.29 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

配制儲備液

濃度溶劑體積質量	1 mg	5 mg	10 mg

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

請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 儲存時，請在 6 個月內使用，-20°C 儲存時，請在 1 個月內使用。

In Vivo:

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：

——為保證實驗結果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

1.

請依序添加每種溶劑： PBS
Solubility: 33.33 mg/mL (81.52 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
2.

請依序添加每種溶劑： 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: ≥ 2.5 mg/mL (6.11 mM); Clear solution
3.

請依序添加每種溶劑： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.11 mM); Clear solution
4.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (5.09 mM); Clear solution
5.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.09 mM); Clear solution
6.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.09 mM); Clear solution
7.

請依序添加每種溶劑： 1% DMSO 99% saline
Solubility: ≥ 0.5 mg/mL (1.22 mM); Clear solution

參考文獻

[1]. Pedersen MG, et al. Dapagliflozin stimulates glucagon secretion at high glucose: experiments and mathematical simulations of human A-cells. Sci Rep. 2016 Aug 18;6:31214.  [Content Brief]
[2]. 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]
[3]. Chang YK, et al. Dapagliflozin, SGLT2 Inhibitor, Attenuates Renal Ischemia-Reperfusion Injury. PLoS One. 2016 Jul 8;11(7):e0158810.  [Content Brief]

注：產品僅用于科研