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Saxagliptin

Catalog No. T6203 CAS 361442-04-8

Synonyms: BMS-477118, Onglyza

Saxagliptin (BMS-477118) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM.

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Saxagliptin, CAS 361442-04-8

Pack Size	Availability	Price/USD
5 mg	In stock	$ 39.00
10 mg	In stock	$ 59.00
25 mg	In stock	$ 113.00
50 mg	In stock	$ 178.00
100 mg	In stock	$ 278.00
200 mg	In stock	$ 418.00
500 mg	In stock	$ 682.00
1 mL * 10 mM (in DMSO)	In stock	$ 43.00

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Purity: 99.95%

Purity: 98.05%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Saxagliptin (BMS-477118) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM.
Targets&IC50	DPP4:26 nM
In vitro	Saxagliptin has an inhibition constant Ki of 1.3 nM for DPP4 inhibition, which is 10-fold more potent than either vildagliptin or sitagliptin (another two DPP4 inhibitors) with Ki of 13 and 18 nM. In addition, Saxagliptin demonstrates greater specificity for DPP4 than for either the DPP8 or DPP9 enzymes (400- and 75- fold, respectively). The active metablite of saxagliptin is two-fold less potent than the parent. Both Saxagliptin and its metabolite are highly selective (>4000-fold) for the prevention of DPP4 compared with a range of other proteases (selectivity of sitagliptin and vildagliptin for DPP4 is >2600 and <250-fold, respectively, compared with DPP8 and DPP9). [2] Saxagliptin reduces the degradation of the incretin hormone glucagon-like peptide-1, thereby enhancing its actions, and is associated with improved β-cell function and suppression of glucagon secretion. [3]
In vivo	Maximal responses of Saxagliptin in glucose excursion in Zuckerfa/fa rats are associated with plasma DPP4 inhibition of approximately 60% vs. control, and no additional antihyperglycemic effects are seen at higher percent inhibition. Saxagliptin is highly effective at eliciting marked dose-dependent enhancements in glucose clearance in the dose range 0.13-1.3 mg/kg in ob/ob mice relative to controls. Saxagliptin dose-dependently elevate plasma insulin significantly at 15 min post-oGTT, with concomitant improvement in the glucose clearance curves at 60 min post-oGTT. [4]

Synonyms	BMS-477118, Onglyza
Molecular Weight	315.41
Formula	C18H25N3O2
CAS No.	361442-04-8

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 59 mg/mL (187.1 mM)

H2O: 58 mg/mL (183.9 mM)

Ethanol: 23 mg/mL (72.9 mM)

References and Literature

1. Tahrani AA, et al. Adv Ther. 2009, 26(3), 249-262. 2. Richter B, et al. Vasc Health Risk Manag. 2008, 4(4), 753-768. 3. Deacon CF, et al. Adv Ther. 2009, 26(5), 488-499. 4. Augeri DJ, et al. J Med Chem. 2005, 48(15), 5025-5037.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Highly Selective Inhibitor Library EMA Approved Drug Library Drug Repurposing Compound Library Anti-Diabetic Compound Library HIF-1 Signaling Pathway Compound Library Glycometabolism Compound Library FDA-Approved & Pharmacopeia Drug Library Protease Inhibitor Library Human Metabolite Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Saxagliptin 361442-04-8 Proteases/Proteasome Ubiquitination Proteasome DPP-4 BMS-477118 Inhibitor p-AKT DPP β-catenin Dipeptidyl Peptidase inhibit insulin Onglyza c-myc proliferation glucagon peptide-1 BMS477118 diabetes glucagon-like BMS 477118 inhibitor

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