Saxagliptin hydrate (Synonyms: BMS-477118 hydrate)

Name: Saxagliptin hydrate
Brand: MedChemExpress
SKU: HY-10285A
Rating: 5.0 (5 reviews)

Cat. No.: HY-10285A Purity: 98.13%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

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

Saxagliptin hydrate Chemical Structure

CAS No. : 945667-22-1

Size	Price	Stock	Quantity
5 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 115	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 175	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 260	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 5 publication(s) in Google Scholar

Other Forms of Saxagliptin hydrate:

5 Publications Citing Use of MCE Saxagliptin hydrate

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DPP-1 DPP-2 DPP-4 DPP-8 DPP-9

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

DPP-4

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.

Cell Proliferation 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

333.43

Formula

C₁₈H₂₇N₃O₃

CAS No.

945667-22-1

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.O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (299.91 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.9991 mL	14.9957 mL	29.9913 mL
5 mM	0.5998 mL	2.9991 mL	5.9983 mL
10 mM	0.2999 mL	1.4996 mL	2.9991 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
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: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: ≥99.0%

Select Batch:

Data Sheet (285 KB) SDS (393 KB)

COA (260 KB)

Handling Instructions (2659 KB)

References

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

[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. [Content Brief]

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.9991 mL	14.9957 mL	29.9913 mL	74.9783 mL
	5 mM	0.5998 mL	2.9991 mL	5.9983 mL	14.9957 mL
	10 mM	0.2999 mL	1.4996 mL	2.9991 mL	7.4978 mL
	15 mM	0.1999 mL	0.9997 mL	1.9994 mL	4.9986 mL
	20 mM	0.1500 mL	0.7498 mL	1.4996 mL	3.7489 mL
	25 mM	0.1200 mL	0.5998 mL	1.1997 mL	2.9991 mL
	30 mM	0.1000 mL	0.4999 mL	0.9997 mL	2.4993 mL
	40 mM	0.0750 mL	0.3749 mL	0.7498 mL	1.8745 mL
	50 mM	0.0600 mL	0.2999 mL	0.5998 mL	1.4996 mL
	60 mM	0.0500 mL	0.2499 mL	0.4999 mL	1.2496 mL
	80 mM	0.0375 mL	0.1874 mL	0.3749 mL	0.9372 mL
	100 mM	0.0300 mL	0.1500 mL	0.2999 mL	0.7498 mL

Saxagliptin hydrate Related Classifications

Metabolic Disease

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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Saxagliptin hydrate (Synonyms: BMS-477118 hydrate)

Customer Review

Other Forms of Saxagliptin hydrate:

Saxagliptin hydrate Related Antibodies

5 Publications Citing Use of MCE Saxagliptin hydrate

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Dipeptidyl Peptidase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Saxagliptin hydrate Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Saxagliptin hydrate Related Classifications

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