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  2. Metabolic Enzyme/Protease
  3. Dipeptidyl Peptidase
  4. Saxagliptin

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

目錄號(hào): HY-10285 純度: 99.96%
COA 產(chǎn)品使用指南 技術(shù)支持

Saxagliptin (BMS-477118) 是一種有效，選擇性，可逆，競(jìng)爭(zhēng)性和具有口服活性的二肽基肽酶 4 (DPP-4) (Ki = 0.6-1.3 nM) 抑制劑。Saxagliptin 可用于 2 型糖尿病的研究。

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Saxagliptin Chemical Structure

Saxagliptin Chemical Structure

CAS No. : 361442-04-8

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥385
In-stock
1 mg ￥175
In-stock
5 mg ￥350
In-stock
10 mg ￥490
In-stock
25 mg ￥805
In-stock
50 mg ￥1225
In-stock
100 mg ￥1820
In-stock
200 mg   詢價(jià)  
500 mg   詢價(jià)  

* Please select Quantity before adding items.

Other Forms of Saxagliptin:

查看 Dipeptidyl Peptidase 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Saxagliptin (BMS-477118) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin has the peotential for type 2 diabetes mellitus research[1][2][3].

IC50 & Target

DPP-4

 

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
Caco-2 IC50
50 nM
Compound: Saxagliptin
Inhibition of DPP4 in human Caco2 cells using H-Ala-Pro-7-amido-4-trifluoromethylcoumarin as substrate after 1 hr by fluorescence assay
Inhibition of DPP4 in human Caco2 cells using H-Ala-Pro-7-amido-4-trifluoromethylcoumarin as substrate after 1 hr by fluorescence assay
[PMID: 23623674]
U-87MG ATCC IC50
1720 μM
Compound: Saxagliptin
Inhibition of FAP in human U87MG cells using Suc-Gly-Pro-AMC as substrate by fluorescence based assay
Inhibition of FAP in human U87MG cells using Suc-Gly-Pro-AMC as substrate by fluorescence based assay
[PMID: 32527554]
體外研究
(In Vitro)

Saxagliptin (100?nM; 48 hours; INS-1 832/13 cells) treatment significantly induceS β-cell proliferation[1].
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[1].
Saxagliptin acts by preventing the degradation of glucagon-like peptide-1 and hence increases secretion of insulin and decreases secretion of glucagon[3].

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

Cell Viability Assay[1]

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

Western Blot Analysis[1]

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.
體內(nèi)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[1].
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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

315.41

Formula

C18H25N3O2
CAS 號(hào)
性狀

固體

顏色

White to off-white

中文名稱

沙格列汀；沙克列汀
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)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)

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : ≥ 34 mg/mL (107.80 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

H2O 中的溶解度 : 10 mg/mL (31.70 mM; 超聲助溶)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 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 (protect from light, stored under nitrogen)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

* 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn)：

以下溶解方案，請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 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。

  • 方案 一

    請(qǐng)依序添加每種溶劑： PBS

    Solubility: 8.33 mg/mL (26.41 mM); 澄清溶液; 超聲助溶 (<60°C)

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.96%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 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 (protect from light, stored under nitrogen)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 3.1705 mL 15.8524 mL 31.7048 mL 79.2619 mL
5 mM 0.6341 mL 3.1705 mL 6.3410 mL 15.8524 mL
10 mM 0.3170 mL 1.5852 mL 3.1705 mL 7.9262 mL
15 mM 0.2114 mL 1.0568 mL 2.1137 mL 5.2841 mL
20 mM 0.1585 mL 0.7926 mL 1.5852 mL 3.9631 mL
25 mM 0.1268 mL 0.6341 mL 1.2682 mL 3.1705 mL
30 mM 0.1057 mL 0.5284 mL 1.0568 mL 2.6421 mL
DMSO 40 mM 0.0793 mL 0.3963 mL 0.7926 mL 1.9815 mL
50 mM 0.0634 mL 0.3170 mL 0.6341 mL 1.5852 mL
60 mM 0.0528 mL 0.2642 mL 0.5284 mL 1.3210 mL
80 mM 0.0396 mL 0.1982 mL 0.3963 mL 0.9908 mL
100 mM 0.0317 mL 0.1585 mL 0.3170 mL 0.7926 mL

* 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過濾除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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