Gosogliptin
Based on 1 publication(s) in Google Scholar
Gosogliptin is a potent and selective inhibitor of dipeptidyl peptidase-IV (DPP-IV).
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- Pureté: 99.83%
- CAS No.: 869490-23-3
- Formule: C17H24F2N6O
- Masse moléculaire:366.41
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Chemical Information
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- Protocole
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Publications Citing Use of MedChemExpress (MCE) Gosogliptin
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Activité biologique
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DPP-4 |
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Cell Line
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Type | Value | Description | References |
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| COS-1 | IC50 |
10300 nM
Compound: 5, PF-00734200
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Inhibition of human FAP expressed in african green monkey COS1 cells
Inhibition of human FAP expressed in african green monkey COS1 cells
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[PMID: 19275964] |
Gosogliptin (PF-00734200) is a potent, orally active, selective, and competitive inhibitor of DPP-IV, the enzyme mainly responsible for the degradation of the incretin peptides GLP-1 and glucose-dependent insulinotropic polypeptide. Gosogliptin demonstrates greater than 200-fold selectivity over other members of the DPP family (DPP-2, DPP-3, DPP-8, and DPP-9) and the related serine proteases, fibroblast activation protein, aminopeptidase P, and propyl oligopeptidase, enzymes that possess similar catalytic activities. Gosogliptin demonstrates rapid and reversible inhibition of plasma DPP-4 activity when administered orally to rats, dogs, and monkeys. In various nonclinical models, Gosogliptin stimulates insulin secretion and improves glucose tolerance[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 869490-23-3
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Appearance Solid
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Masse moléculaire 366.41
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Formule C17H24F2N6O
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Color White to yellow
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SMILES
O=C([C@H](C1)NC[C@H]1N2CCN(CC2)C3=NC=CC=N3)N4CC(CC4)(F)F
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Synonyms
PF-00734200; PF-734200
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Solvant et solubilité
DMSO : 100 mg/mL (272.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (13.65 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (13.65 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocole
Studies to identify the P450 isoform(s) responsible for formation of M5 are conducted using chemical inhibition and incubation in recombinant P450 isozymes. Inhibition studies are performed with each of the following inhibitors: Furafylline (10 μM for CYP1A2), Sulfaphenazole (10 μM for CYP2C9), Quinidine (10 μM for CYP2D6), (+)N-3-benzylnirvanol (10 μM for CYP2C19), and Ketoconazole (1 μM for CYP3A4). Incubations (1 ml) are performed in duplicate with NADPH (1.3 mM) in 1.5 mL plastic Eppendorf tubes open to air at 37°C in a shaking water bath. Samples are preincubated at 37°C for 5 min before the addition of NADPH. Each incubation contains microsomes (2 mg/mL protein), 100 mM potassium phosphate buffer (pH 7.4), 10 mM MgCl2, 10 μM Gosogliptin (PF-00734200), and one of the above inhibitors. A control sample is also prepared without inhibitor. Additional controls using marker substrates (each at 10 μM), in the presence and absence of P450-specific inhibitors, are used to confirm inhibition results and included Phenacetin (CYP1A2), Tolbutamide (CYP2C9), (S)-Mephenytoin (CYP2C19), Dextromethorphan (CYP2D6), and Testosterone (CYP3A4). At 0 and 30 min, incubations are quenched with an equal volume of ice-cold acetonitrile. Samples are then placed on ice for 15 min to allow precipitation of protein and subsequently centrifuged at 1800g for 5 min. An aliquot is removed from each sample and injected onto the HPLC/MS system[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats[2]
A group of SD rats (n=3/gender) is administered a single 5 mg/kg oral dose of [14C] Gosogliptin for the mass balance study. For biliary excretion experiments, another group of two male and two female bile duct-cannulated rats is administered a single 5 mg/kg oral dose of [14C] Gosogliptin in similar fashion. The dose is formulated as a suspension in 0.5% methyl cellulose on the day before dose administration. Each rat received an approximate dose of ∼60 μCi of radiolabeled material. Urine and feces are collected from intact animals for 7 days at 0 to 8, 8 to 24, 24 to 48, 48 to 72, 72 to 96, 96 to 120, 120 to 144, and 144- to 168-h intervals after the dose. The first feces sample is collected at 0 to 24 h after the dose. Bile and urine samples are collected from bile duct-cannulated animals at 0- to 8-, 8- to 24-, and 24- to 48-h intervals after the dose. The volumes of urine and bile samples are recorded, and all of the biological samples are stored at -20°C until analysis. For determination of pharmacokinetic parameters and identification of circulating metabolites, a third group of jugular vein-cannulated rats (n=10/gender) is given an oral dose of 5 mg/kg [14C] Gosogliptin. Blood from two animals per gender is collected at 0.5, 1, 2, 4, and 8 h postdose in heparinized (lithium heparin anticoagulant) tubes. The blood samples are centrifuged at 1000g for 10 min to obtain the plasma. Plasma is transferred to clean tubes and stored at -20°C until analysis.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Dai H, et al. The pharmacokinetics of PF-734200, a DPP-IV inhibitor, in subjects with renal insufficiency. Br J Clin Pharmacol. 2011 Jul;72(1):85-91. [Content Brief]
[2]. Sharma R, et al. Metabolism, excretion, and pharmacokinetics of ((3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone, a dipeptidyl peptidase inhibitor, in rat, dog and human. Drug Metab Dispos. 2012 Nov;40(11):2143-61. [Content Brief]
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7292 mL | 13.6459 mL | 27.2918 mL | 68.2296 mL |
| 5 mM | 0.5458 mL | 2.7292 mL | 5.4584 mL | 13.6459 mL | |
| 10 mM | 0.2729 mL | 1.3646 mL | 2.7292 mL | 6.8230 mL | |
| 15 mM | 0.1819 mL | 0.9097 mL | 1.8195 mL | 4.5486 mL | |
| 20 mM | 0.1365 mL | 0.6823 mL | 1.3646 mL | 3.4115 mL | |
| 25 mM | 0.1092 mL | 0.5458 mL | 1.0917 mL | 2.7292 mL | |
| 30 mM | 0.0910 mL | 0.4549 mL | 0.9097 mL | 2.2743 mL | |
| 40 mM | 0.0682 mL | 0.3411 mL | 0.6823 mL | 1.7057 mL | |
| 50 mM | 0.0546 mL | 0.2729 mL | 0.5458 mL | 1.3646 mL | |
| 60 mM | 0.0455 mL | 0.2274 mL | 0.4549 mL | 1.1372 mL | |
| 80 mM | 0.0341 mL | 0.1706 mL | 0.3411 mL | 0.8529 mL | |
| 100 mM | 0.0273 mL | 0.1365 mL | 0.2729 mL | 0.6823 mL |
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