Saxagliptin|361442-04-8|(沙格列汀; BMS-477118)-陌孚医药/Medlife

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Saxagliptin (Synonyms: 沙格列汀; BMS-477118)

目录号: PC15719 纯度: ≥98%

CAS No. :361442-04-8

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中文名称	Saxagliptin
中文别名	沙克列汀;(1S,3S,5S)-2-[(2S)-2-氨基-2-(3-羟基三环[3.3.1.13,7]癸烷-1-基)乙酰基]-2-氮杂双环[3.1.0]己烷-3-腈;沙格列汀;沙格列汀TFA盐;沙格列汀标准品;沙格列汀标准品及杂质;沙格列汀对照品及相关杂质;沙格列汀三氟乙酸盐;沙格列汀杂质;沙格列汀杂质及标准品;沙克列汀一水合物;沙克列汀杂质;盐酸沙格列汀（碱）;沙格列汀-13C,D2TFA盐;(1S,3S,5S)-2-[(2S)-2-氨基-2-(3-羟基三环[3.3.1.1(3,7)]癸烷-1-基)乙酰基]-2-氮杂双环[3.1.0]己烷-3-腈
英文名称	Saxagliptin
英文别名	Saxagliptin;(1S,3S,5S)-2-[(2S)-2-Amino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile;BMS 477118;Onglyza;Saxagliptin Onglyza BMS 477118;Saxagliptin Hydrochloride(free base);Saxagliptin ;(1R,3S,5R)-2-((S)-2-amino-2-((1r,3R,5R,7S)-3-hydroxyadamantan-1-yl)acetyl)-2-azabicyclo[3.1.0]hexane-3-carbonitrile;BMS-477118;(1S,3S,5S)-2-[(2S)-2-Amino-2-(3-hydroxytricyclo[3.3.1.1(3,7)]dec-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile;2-azabicyclo[3.1.0]hexane-3-carbonitrile, 2-[(2S)-2-amino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-, (1S,3S,5S)
Cas No.	361442-04-8
分子式	C₁₈H₂₅N₃O₂
分子量	315.41
包装储存	-20°C, protect from light, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

生物活性

Saxagliptin (BMS-477118) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (K_i = 0.6-1.3 nM) inhibitor. Saxagliptin has the peotential for type 2 diabetes mellitus research.

性状

Solid

IC50 & Target[1][2]

DPP-4

体外研究(In Vitro)

Saxagliptin (100?nM; 48 hours; INS-1 832/13 cells) treatment significantly induceS β-cell proliferation.
Saxagliptin (100?nM; 48 hours; INS-1 832/13 cells) treatment increases the p-AKT and active β-catenin protein levels, paralleled with the increase of c-myc and cyclin D1 protein expression.
Saxagliptin acts by preventing the degradation of glucagon-like peptide-1 and hence increases secretion of insulin and decreases secretion of glucagon.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	INS-1 832/13 cells
Concentration:	100?nM
Incubation Time:	48 hours
Result:	Significantly induced β-cell proliferation.

Western Blot Analysis

Cell Line:	INS-1 832/13 cells
Concentration:	100?nM
Incubation Time:	48 hours
Result:	Increased the p-AKT and active β-catenin protein levels, paralleled with the increase of c-myc and cyclin D1 protein expression.

体内研究(In Vivo)

Saxagliptin (1 mg/kg; for 12 weeks) treatment in high-fat diet/streptozotocin-induced diabetic rats, significant improvement in pancreas insulin secretion capacity evaluated by hyperglycemia clamp and increased β-cell to α-cell areas ratio are observed.
Saxagliptin dose-dependently inhibits plasma DPP-4 activity in Han-Wistar rats, by ~70% at 7 hours postdose with 1 mg/kg and by ~90% at 7 hours postdose with 10 mg/kg. At 24 hours postdose, ~20% and 70% inhibition, respectively, remained.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

ClinicalTrial

参考文献

[1]. Chun-Jun Li, et al. Saxagliptin Induces β-Cell Proliferation through Increasing Stromal Cell-Derived Factor-1α In Vivo and 体外研究. Front Endocrinol (Lausanne). 2017 Nov 27;8:326. [Information]

[2]. Darshan J Dave. Saxagliptin: A dipeptidyl peptidase-4 inhibitor in the treatment of type 2 diabetes mellitus. J Pharmacol Pharmacother. 2011 Oct;2(4):230-5. [Information]

[3]. Carolyn F Deacon, et al. Saxagliptin: a new dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes. Adv Ther. 2009 May;26(5):488-99. [Information]

溶解度数据

体外研究:

DMSO : ≥ 34 mg/mL (107.80 mM)

H₂O : 10 mg/mL (31.70 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.1705 mL	15.8524 mL	31.7048 mL
5 mM	0.6341 mL	3.1705 mL	6.3410 mL
10 mM	0.3170 mL	1.5852 mL	3.1705 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： PBS
Solubility: 8.33 mg/mL (26.41 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

搜索质检报告(COA)

产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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