Name: Sitagliptin
Brand: Selleck Chemicals
SKU: S5079
Rating: 5 (24 reviews)

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Contrôle Qualité (Quality Control)

Lot : Pureté : 99.91%

99.91

Cibles apparentées	HDAC Caspase Proteasome Secretase MMP HCV Protease Cysteine Protease Tyrosinase HIV Protease Serine Protease
Autre DPP Inhibiteurs	Talabostat (Val-boroPro, PT-100) Mesylate Puromycin aminonucleoside MK-3102 (Omarigliptin) Brensocatib Trelagliptin Teneligliptin hydrobromide Trelagliptin succinate Anagliptin Gemigliptin Lobeliae Chinensis Extract

Informations chimiques, stockage et stabilité (Chemical Information, Storage & Stability)

Poids moléculaire	407.31	Formule	C₁₆H₁₅F₆N₅O	Stockage (À compter de la date de réception)	3 ans-20°Cpoudre
N° CAS	486460-32-6	--		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	MK-0431			Smiles	C1CN2C(=NN=C2C(F)(F)F)CN1C(=O)CC(CC3=CC(=C(C=C3F)F)F)N

Solubilité (Solubility)

In vitro
Lot:

DMSO : 81 mg/mL (198.86 mM)
(Le DMSO contaminé par l'humidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Ethanol : 81 mg/mL

Water : 5 mg/mL (Ultrasonic and heating for 10 minutes, at 60℃.)

DMSO : 81 mg/mL (198.86 mM)
(Le DMSO contaminé par l'humidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Ethanol : 81 mg/mL

Water : 7 mg/mL (Ultrasonic and heating for 10 minutes, at 60℃.)

Calculateur de molarité

Masse	Concentration	Volume	Poids moléculaire
=	×	×

Calculateur de dilution Calculateur de poids moléculaire

In vivo Lot:
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.
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.
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.
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.
Clear solution	5%DMSO 1 Corn oil Validé par les laboratoires Selleck. Si vous avez besoin d'ajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	10.000mg/ml (24.55mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validé par les laboratoires Selleck. Si vous avez besoin d'ajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	10.000mg/ml (24.55mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant l'expérience)

Dosage : mg/kg Poids moyen des animaux : g Volume de dosage par animal :μL Nombre d'animaux :

Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter d'abord s'il n'y a pas de formulation in vivo dans la section Solubilité.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter d'abord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH₂O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.

Note : 1. Veuillez vous assurer que le liquide est clair avant d'ajouter le solvant suivant.
2. Assurez-vous d'ajouter le(s) solvant(s) dans l'ordre. Vous devez vous assurer que la solution obtenue, lors de l'ajout précédent, est une solution claire avant de procéder à l'ajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.

Mécanisme d'action (Mechanism of Action)

Targets/IC₅₀/Ki	DPP-4 (Cell-free) 18 nM
In vitro	Sitagliptin exhibits a > 2600-fold margin of selectivity against DPP8, DPP9, and other members of the dipeptidyl peptidase family (i.e., potency against DPP-4 vs. DPP8/9). This compound reduces in vitro migration of isolated splenic CD4 T-cells through a pathway involving cAMP/PKA/Rac1 activation. It exerts a novel, direct action in order to stimulate GLP-1 secretion by the intestinal L cell through a DPP-4-independent, protein kinase A- and MEK-ERK1/2-dependent pathway. It therefore reduces the effect of autoimmunity on graft survival.
In vivo	Sitagliptin is well absorbed after oral administration with a bioavailability of 87%. It has an apparent terminal half-life of 10–12 h at doses of 25-100 mg and is excreted mainly (≈ 80%) as unchanged compound by the kidneys. This compound does not interfere with the P450 cytochrome enzymes nor have there been any reported significant drug-drug interactions. It has been shown to inhibit DPP-4 activity by > 90% within 1-2 h of administration. It has a short half-life in mice (1-2 h). Chronic sitagliptin treatment in a non-geneticmouse model of type 2 diabetes elicits significant improvement in glycemic control. The improved glucose homeostasis correlates with restoration of normal islet cell (α and β cells) mass, architecture and insulin secretion capacity in response to glucose stimulation. This compound prolongs islet graft survival in streptozotocin-induced and NOD mice. Administration of this chemical in vivo reduces lymph node and splenic CD4+ T-cell migration, measured in vitro, via incretin- and nonincretin-mediated effects, respectively, and splenic sDPP-IV-responsive CD4+ T-cells and lymph node incretin nonresponsive CD4+ T-cells selectively infiltrated islets of diabetic NOD mice, after tail vein injection. It significantly suppressed epileptogenesis in PTZ (pentylenetetrazole)-induced seizures. This compound counteracted neuronal damage and all biochemical, and histo-chemical alteration induced by PTZ. Oral sitagliptin can promote hippocampal neurogenesis, counteract hippocampal oxidative stress, and prevent the decline in mice cognition.
Références	[1] https://pubmed.ncbi.nlm.nih.gov/18182122/ [2] https://pubmed.ncbi.nlm.nih.gov/19073764/ [3] https://pubmed.ncbi.nlm.nih.gov/22186413/ [4] https://pubmed.ncbi.nlm.nih.gov/19765579/ [5] https://pubmed.ncbi.nlm.nih.gov/20368408/ [6] https://pubmed.ncbi.nlm.nih.gov/29032011/

Informations sur l'essai clinique (Clinical Trial Information)

(données du https://clinicaltrials.gov, mis à jour le 2026-02-18)

Numéro NCT	Recrutement	Conditions	Promoteur/Collaborateurs	Date de début	Phases
NCT06813014	NOT_YET_RECRUITING	Diabetes	University of Maryland, Baltimore	2026-12	PHASE4
NCT07365592	RECRUITING	Colorectal Cancer	Second Affiliated Hospital, Zhejiang University, School of Medicine	2026-04-09	PHASE1; PHASE2
NCT07108985	NOT_YET_RECRUITING	Diabetes Mellitus, Type 2; Hyperglycemia; Insulin Resistance	Yonsei University	2025-09	PHASE4
NCT07541781	RECRUITING	Glioma; Glioblastoma; Recurrent Glioma; Recurrent Glioblastoma; Grade 4 Malignant Glioma of Brain (Disorder)	Kailin Yang, MD, PhD	2026-06-11	PHASE1
NCT06246799	RECRUITING	Type 2 Diabetes (Adult Onset)	The University of Texas Health Science Center at San Antonio	2024-11-07	PHASE3
NCT07804381	NOT_YET_RECRUITING	Parkinson Disease	Yonsei University	2026-12-15	PHASE2

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Sitagliptin DPP Inhibiteur

Poids moléculaire: 407.31