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

Saxagliptin hydrochloride  (Synonyms: BMS-477118 hydrochloride)

Cat. No.: HY-16448 Purity: 99.71%
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Saxagliptin hydrochloride (BMS-477118 hydrochloride) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin hydrochloride has the peotential for type 2 diabetes mellitus research.

For research use only. We do not sell to patients.

Saxagliptin hydrochloride Chemical Structure

Saxagliptin hydrochloride Chemical Structure

CAS No. : 709031-78-7

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10 mg USD 75 In-stock
25 mg USD 140 In-stock
50 mg USD 220 In-stock
100 mg USD 330 In-stock
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Based on 4 publication(s) in Google Scholar

Other Forms of Saxagliptin hydrochloride:

Saxagliptin hydrochloride Related Antibodies

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Description

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

IC50 & Target

Ki: 0.6-1.3 nM (Dipeptidyl peptidase-4 (DPP-4))[2]
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].

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

Saxagliptin hydrochloride Related Antibodies

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.
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].

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

351.87

Formula

C18H26ClN3O2
CAS No.
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.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

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

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (355.24 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 100 mg/mL (284.20 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8420 mL 14.2098 mL 28.4196 mL
5 mM 0.5684 mL 2.8420 mL 5.6839 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 (sealed storage, away from moisture and light). 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.

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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=
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C2

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V2

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

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 (sealed storage, away from moisture and light). 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 2.8420 mL 14.2098 mL 28.4196 mL 71.0490 mL
5 mM 0.5684 mL 2.8420 mL 5.6839 mL 14.2098 mL
10 mM 0.2842 mL 1.4210 mL 2.8420 mL 7.1049 mL
15 mM 0.1895 mL 0.9473 mL 1.8946 mL 4.7366 mL
20 mM 0.1421 mL 0.7105 mL 1.4210 mL 3.5524 mL
25 mM 0.1137 mL 0.5684 mL 1.1368 mL 2.8420 mL
30 mM 0.0947 mL 0.4737 mL 0.9473 mL 2.3683 mL
40 mM 0.0710 mL 0.3552 mL 0.7105 mL 1.7762 mL
50 mM 0.0568 mL 0.2842 mL 0.5684 mL 1.4210 mL
60 mM 0.0474 mL 0.2368 mL 0.4737 mL 1.1841 mL
80 mM 0.0355 mL 0.1776 mL 0.3552 mL 0.8881 mL
100 mM 0.0284 mL 0.1421 mL 0.2842 mL 0.7105 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 hydrochloride Related Classifications

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  • 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:

Saxagliptin709031-78-7BMS-477118BMS477118BMS 477118Dipeptidyl PeptidaseDPPDPP-4diabetesglucagon-likepeptide-1insulinglucagonp-AKTβ-cateninc-mycproliferationInhibitorinhibitorinhibit

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