Saxagliptin (Synonyms: BMS-477118)

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

Cat. No.: HY-10285 Purity: 99.96%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

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

Saxagliptin Chemical Structure

CAS No. : 361442-04-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
Solid
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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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Saxagliptin:

5 Publications Citing Use of MCE Saxagliptin

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•Related Screening Libraries:

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View All Isoforms

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

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

DPP-4

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]

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 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

315.41

Formula

C₁₈H₂₅N₃O₂

CAS No.

361442-04-8

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

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 : ≥ 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)

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:

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)

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

Purity & Documentation

Purity: 99.96%

Select Batch:

Data Sheet (284 KB) SDS (393 KB)

COA (257 KB) RP-HPLC (275 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

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.

Saxagliptin 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 (Synonyms: BMS-477118)

Customer Review

Other Forms of Saxagliptin:

Saxagliptin Related Antibodies

5 Publications Citing Use of MCE Saxagliptin

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 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Saxagliptin Related Classifications

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Your Recently Viewed Products:

Customer Review

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