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

Saxagliptin  (Synonyms: BMS-477118)

製品番号: HY-10285 純度: 99.96%
COA 取扱説明書 Technical Support

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.

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Saxagliptin

Saxagliptin 構造式

CAS 番号 : 361442-04-8

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 55 在庫あり
Solution
10 mM * 1 mL in DMSO USD 55 在庫あり
Solid
5 mg $50 在庫あり
10 mg $70 在庫あり
25 mg $115 在庫あり
50 mg $175 在庫あり
100 mg $260 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 6 publication(s) in Google Scholar

Other Forms of Saxagliptin:

Saxagliptin 関連抗体

Top Publications Citing Use of Products

Dipeptidyl Peptidase アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
DPP-1 DPP-2 DPP-4 DPP-8 DPP-9

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

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

 

Cellular Effect
Cell Line Type Value Description References
Caco-2 IC50
50 1
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 3
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]
体外実験

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].

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

Saxagliptin 関連抗体

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.
体内実験

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
分子量

315.41

分子式

C18H25N3O2
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

N[C@@H]([C@](C[C@H](C1)C2)(C[C@@H]1C3)C[C@]23O)C(N([C@@H](C4)C#N)[C@@H]5[C@H]4C5)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

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

DMSO : ≥ 34 mg/mL (107.80 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 8.33 mg/mL (26.41 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
純度とドキュメンテーション

純度: 99.96%

COA (257 KB) RP-HPLC (275 KB)

取扱説明書 (2659 KB)
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Saxagliptin Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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.

Keywords:

Saxagliptin361442-04-8BMS-477118BMS477118BMS 477118Dipeptidyl PeptidaseDPPDPP-4diabetesglucagon-likepeptide-1insulinglucagonp-AKTβ-cateninc-mycproliferationInhibitorinhibitorinhibit

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