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Alogliptin DPP inhibitor

Name: Alogliptin
Brand: Selleck Chemicals
SKU: S5365
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S5365

Alogliptin is a potent, selective inhibitor of the serine protease dipeptidyl peptidase IV (DPP-4) with IC50 values of 2.63 nM and exhibits greater than 10,000 fold selectivity over the closely related serine proteases DPP-8 and DPP-9.

Chemical Structure

Molecular Weight: 339.39

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Quality Control

Batch: S536501 DMSO]67 mg/mL]false]Ethanol]67 mg/mL]false]Water]18 mg/mL]false Purity: 99.93%

Cited in Nature Medicine for its top-tier quality
COA
SDS
Datasheet

99.93

Related Targets	HDAC Caspase Proteasome Secretase MMP HCV Protease Cysteine Protease Tyrosinase HIV Protease Serine Protease
Other DPP Inhibitors	Talabostat (Val-boroPro, PT-100) Mesylate Omarigliptin (MK-3102) Lobeliae Chinensis Extract Teneligliptin Hydrobromide Hydrate Brensocatib Puromycin aminonucleoside Anagliptin Trelagliptin Teneligliptin hydrobromide Trelagliptin succinate

Solubility

In vitro
Batch:

DMSO : 67 mg/mL (197.41 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 67 mg/mL

Water : 18 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

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Working concentration: mg/ml;

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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	339.39	Formula	C₁₈H₂₁N₅O₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	850649-61-5	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	SYR 322			Smiles	CN1C(=O)C=C(N(C1=O)CC2=CC=CC=C2C#N)N3CCCC(C3)N

Mechanism of Action

Targets/IC₅₀/Ki	DPP-4 (293E cells lysates) 2.93 nM
In vitro	Alogliptin is a potent (IC50 < 10 nM) inhibitor of DPP-4 and exhibits greater than 10,000 fold selectivity over the closely related serine proteases DPP-8 and DPP-9.Compound 10 is not an inhibitor of CYP-450 enzymes and does not block the hERG channel at concentrations up to 30μM.
In vivo	Absolute oral bioavailability of alogliptin in rats, dogs, and monkeys is 45%, 86%, and 72% to 88%, respectively. After a single oral dose of alogliptin, plasma DPP-4 inhibition is observed within 15 min and maximum inhibition is > 90% in rats, dogs, and monkeys; inhibition is sustained for 12 h in rats (43%) and dogs (65%) and 24 h in monkeys (> 80%). From Emax modeling, 50% inhibition of DPP-4 activity is observed at a mean alogliptin plasma concentration (EC50) of 3.4 to 5.6 ng/ml (10.0 to 16.5 nM) in rats, dogs, and monkeys. In Zucker fa/fa rats, a single dose of alogliptin (0.3, 1, 3, and 10 mg/kg) inhibites plasma DPP-4 (91% to 100% at 2 h and 20% to 66% at 24 h), increases plasma GLP-1 (2- to 3-fold increase in AUC0–20 min) and increases early-phase insulin secretion (1.5- to 2.6-fold increase in AUC0-20 min) and reduces blood glucose excursion (31%–67% decrease in AUC0–90 min) after oral glucose challenge. Alogliptin (30 and 100 mg/kg) has no effect on fasting plasma glucose in normoglycemic rats..
References	[1] https://www.ncbi.nlm.nih.gov/pubmed/?term=25464020 [2] https://www.ncbi.nlm.nih.gov/pubmed/?term=17441705 [3] https://www.ncbi.nlm.nih.gov/pubmed/?term=18538760 [4] https://www.ncbi.nlm.nih.gov/pubmed/?term=18499100

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03501277	Completed	Healthy Volunteers	Takeda	May 26 2018	Phase 1
NCT02276274	Completed	Clinical Pharmacology	Takeda	June 2014	Phase 3
NCT00957268	Completed	Diabetes Mellitus Type 2	Takeda	September 2009	Phase 1

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