Empagliflozin (恩格列凈; BI 10773)

Empagliflozin (BI 10773) 是一種選擇性鈉葡萄糖協(xié)同轉(zhuǎn)運(yùn)蛋白-2 (SGLT-2) 抑制劑，抑制人 SGLT-2 的IC50 為 3.1 nM。貨號(hào)：HY-15409，CAS： 864070-44-0

參數(shù)品牌：MCE

產(chǎn)品參數(shù)

品牌：MCE

型號(hào)：HY-15409

起訂量：1

規(guī)格:：10mg

價(jià)格:：￥950

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Empagliflozin (Synonyms: 恩格列凈; BI 10773)

Empagliflozin (BI 10773) 是一種選擇性鈉葡萄糖協(xié)同轉(zhuǎn)運(yùn)蛋白-2 (SGLT-2) 抑制劑，抑制人 SGLT-2 的IC₅₀ 為 3.1 nM。

生物活性

Empagliflozin (BI 107730 is a selective sodium glucose cotransporter-2 (SGLT-2) inhibitor with an IC₅₀ of 3.1 nM for human SGLT-2

IC₅₀ & Target

IC50: 3.1 nM (SGLT-2), 1.1 μM (SGLT-5), 2 μM (SGLT-6), 8.3 μM (SGLT-1), 11 μM (SGLT-4)^[1]

體外研究(In Vitro)

Empagliflozin is a potent and competitive SGLT-2 inhibitor with an excellent selectivity profile and the highest selectivity window of the tested SGLT-2 inhibitors over hSGLT-1. Empagliflozin inhibits the uptake of [¹⁴C]-alpha-methyl glucopyranoside (AMG) via hSGLT-2 in a dose-dependent manner with an IC₅₀ of 3.1 nM, but is less potent for other SGLTs (IC₅₀ range: 1100-11000 nM). [³H]-Empagliflozin displays a high affinity for SGLT-2 with a mean K_d of 57±37 nM in the absence of glucose in kinetic binding experiments

體內(nèi)研究(In Vivo)

Glucose intolerance is significantly improved after 8 days of Empagliflozin treatment at either dose (3mg/kg Empagliflozin 3058±180 vs 10mg/kg Empagliflozin 3090±219). Therefore, acute treatment with Empagliflozin has a beneficial effect on hyperglycemia and glucose intolerance. Since there are no significant differences in blood glucose homeostasis with the two different doses of Empagliflozin, and random blood glucose levels of T1DM mice are significantly improved by 3mg/kg of Empagliflozin, the effect of the lower dose of Empagliflozin (3mg/kg) is investigated on preserving β-cell mass and function

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02863328	Novo Nordisk A+S	Diabetes\|Diabetes Mellitus, Type 2	August 10, 2016	Phase 3
NCT03060980	Intarcia Therapeutics	Diabetes Mellitus, Type 2	March 3, 2017	Phase 3
NCT03057977	Boehringer Ingelheim\|Eli Lilly and Company	Heart Failure	March 6, 2017	Phase 3

分子量：450.91

Formula：C₂₃H₂₇ClO₇

CAS 號(hào)：864070-44-0

中文名稱：恩格列凈

運(yùn)輸條件：Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性數(shù)據(jù)

DMSO : 50 mg/mL (110.89 mM; Need ultrasonic)

H₂O : 0.11 mg/mL (0.24 mM; Need ultrasonic and warming)

配制儲(chǔ)備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	2.2177 mL	11.0887 mL	22.1774 mL
5 mM	0.4435 mL	2.2177 mL	4.4355 mL
10 mM	0.2218 mL	1.1089 mL	2.2177 mL

*

請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。

In Vivo:

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

——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

1.

請(qǐng)依序添加每種溶劑： 0.5%HPMC
Solubility: 5 mg/mL (11.09 mM); Suspension solution; Need ultrasonic
2.

請(qǐng)依序添加每種溶劑： 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: ≥ 2.87 mg/mL (6.36 mM); Clear solution
3.

請(qǐng)依序添加每種溶劑： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.87 mg/mL (6.36 mM); Clear solution
4.

請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.61 mM); Clear solution
5.

請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.61 mM); Clear solution
6.

請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.61 mM); Clear solution

參考文獻(xiàn)

[1]. Grempler R, et al. Empagliflozin, a novel selective sodium glucose cotransporter-2 (SGLT-2) inhibitor: characterisation and comparison with other SGLT-2 inhibitors. Diabetes Obes Metab. 2012 Jan;14(1):83-90.

[2]. Cheng ST, et al. The Effects of Empagliflozin, an SGLT2 Inhibitor, on Pancreatic β-Cell Mass and Glucose Homeostasis in Type 1 Diabetes. PLoS One. 2016 Jan 25;11(1):e0147391.

[3]. Nikole J.ByrneBSc, et al. Empagliflozin Prevents Worsening of Cardiac Function in an Experimental Model of Pressure Overload-Induced Heart Failure. JACC Basic Transl Sci. 2017 Aug;2(4):347-354.

[4]. Sakaeda T, et al. Susceptibility to serious skin and subcutaneous tissue disorders and skin tissue distribution of sodium-dependent glucose co-transporter type 2 (SGLT2) inhibitors. Int J Med Sci. 2018 Jun 13;15(9):937-943.

Empagliflozin (恩格列凈; BI 10773)

Empagliflozin (BI 10773) 是一種選擇性鈉葡萄糖協(xié)同轉(zhuǎn)運(yùn)蛋白-2 (SGLT-2) 抑制劑，抑制人 SGLT-2 的IC50 為 3.1 nM。貨號(hào)：HY-15409，CAS： 864070-44-0

品牌：MCE

型號(hào)：HY-15409

起訂量：1

規(guī)格:：10mg

價(jià)格:：￥950

15906629305

在線客服

客服一

產(chǎn)品詳情

Empagliflozin (Synonyms: 恩格列凈; BI 10773)

Empagliflozin (BI 10773) 是一種選擇性鈉葡萄糖協(xié)同轉(zhuǎn)運(yùn)蛋白-2 (SGLT-2) 抑制劑，抑制人 SGLT-2 的IC₅₀ 為 3.1 nM。

生物活性

Empagliflozin (BI 107730 is a selective sodium glucose cotransporter-2 (SGLT-2) inhibitor with an IC₅₀ of 3.1 nM for human SGLT-2

IC₅₀ & Target

IC50: 3.1 nM (SGLT-2), 1.1 μM (SGLT-5), 2 μM (SGLT-6), 8.3 μM (SGLT-1), 11 μM (SGLT-4)^[1]

體外研究(In Vitro)

Empagliflozin is a potent and competitive SGLT-2 inhibitor with an excellent selectivity profile and the highest selectivity window of the tested SGLT-2 inhibitors over hSGLT-1. Empagliflozin inhibits the uptake of [¹⁴C]-alpha-methyl glucopyranoside (AMG) via hSGLT-2 in a dose-dependent manner with an IC₅₀ of 3.1 nM, but is less potent for other SGLTs (IC₅₀ range: 1100-11000 nM). [³H]-Empagliflozin displays a high affinity for SGLT-2 with a mean K_d of 57±37 nM in the absence of glucose in kinetic binding experiments

體內(nèi)研究(In Vivo)

Glucose intolerance is significantly improved after 8 days of Empagliflozin treatment at either dose (3mg/kg Empagliflozin 3058±180 vs 10mg/kg Empagliflozin 3090±219). Therefore, acute treatment with Empagliflozin has a beneficial effect on hyperglycemia and glucose intolerance. Since there are no significant differences in blood glucose homeostasis with the two different doses of Empagliflozin, and random blood glucose levels of T1DM mice are significantly improved by 3mg/kg of Empagliflozin, the effect of the lower dose of Empagliflozin (3mg/kg) is investigated on preserving β-cell mass and function

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02863328	Novo Nordisk A+S	Diabetes\|Diabetes Mellitus, Type 2	August 10, 2016	Phase 3
NCT03060980	Intarcia Therapeutics	Diabetes Mellitus, Type 2	March 3, 2017	Phase 3
NCT03057977	Boehringer Ingelheim\|Eli Lilly and Company	Heart Failure	March 6, 2017	Phase 3

分子量：450.91

Formula：C₂₃H₂₇ClO₇

CAS 號(hào)：864070-44-0

中文名稱：恩格列凈

運(yùn)輸條件：Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性數(shù)據(jù)

DMSO : 50 mg/mL (110.89 mM; Need ultrasonic)

H₂O : 0.11 mg/mL (0.24 mM; Need ultrasonic and warming)

配制儲(chǔ)備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	2.2177 mL	11.0887 mL	22.1774 mL
5 mM	0.4435 mL	2.2177 mL	4.4355 mL
10 mM	0.2218 mL	1.1089 mL	2.2177 mL

*

請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。

In Vivo:

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

——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

1.

請(qǐng)依序添加每種溶劑： 0.5%HPMC
Solubility: 5 mg/mL (11.09 mM); Suspension solution; Need ultrasonic
2.

請(qǐng)依序添加每種溶劑： 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: ≥ 2.87 mg/mL (6.36 mM); Clear solution
3.

請(qǐng)依序添加每種溶劑： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.87 mg/mL (6.36 mM); Clear solution
4.

請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.61 mM); Clear solution
5.

請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.61 mM); Clear solution
6.

請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.61 mM); Clear solution

參考文獻(xiàn)

[1]. Grempler R, et al. Empagliflozin, a novel selective sodium glucose cotransporter-2 (SGLT-2) inhibitor: characterisation and comparison with other SGLT-2 inhibitors. Diabetes Obes Metab. 2012 Jan;14(1):83-90.

[2]. Cheng ST, et al. The Effects of Empagliflozin, an SGLT2 Inhibitor, on Pancreatic β-Cell Mass and Glucose Homeostasis in Type 1 Diabetes. PLoS One. 2016 Jan 25;11(1):e0147391.

[3]. Nikole J.ByrneBSc, et al. Empagliflozin Prevents Worsening of Cardiac Function in an Experimental Model of Pressure Overload-Induced Heart Failure. JACC Basic Transl Sci. 2017 Aug;2(4):347-354.

[4]. Sakaeda T, et al. Susceptibility to serious skin and subcutaneous tissue disorders and skin tissue distribution of sodium-dependent glucose co-transporter type 2 (SGLT2) inhibitors. Int J Med Sci. 2018 Jun 13;15(9):937-943.

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Empagliflozin (Synonyms: 恩格列凈; BI 10773)

Empagliflozin (恩格列凈; BI 10773)

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Empagliflozin (Synonyms: 恩格列凈; BI 10773)