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| 5mg |
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Dutogliptin (formerly PHX-1149; PHX1149) is a novel, potent and orally bioavailable dipeptidyl peptidase-4 (DPP4) inhibitor with antidiabetic effects. It has exhibited improved glycemic control in type 2 diabetic patients.
| ln Vivo |
Dutogliptin exhibits a Tmax of 3–4 hours and a half-life of 10–13 hours, along with minimal plasma protein binding (11%), fast absorption, and both. Because dutogliptin is metabolically stable, it neither stimulates nor inhibits significant CYP450 activity [2].
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|---|---|
| ADME/Pharmacokinetics |
Biological Half-Life
10-13 hours |
| References |
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| Additional Infomation |
Dutogliptin has been investigated for the treatment of Diabetes Mellitus, Type II.
Dutogliptin is a potent, water soluble, selective and orally bioavailable, boronic acid-based inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity. Dutogliptin irriversibly binds to DPP-4. Mechanism of Action Dutogliptin is a potent and selective inhibitor of DPP4, a serine protease that has emerged as an important target for the treatment of type 2 diabetes. Inhibiting DPP4 increases the physiological levels of regulatory peptides, such as GLP-1, an important modulator of insulin response and digestion. |
| Molecular Formula |
C₁₀H₂₀BN₃O₃
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|---|---|
| Molecular Weight |
241.10
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| Exact Mass |
241.16
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| CAS # |
852329-66-9
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| Related CAS # |
Dutogliptin tartrate;890402-81-0
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| PubChem CID |
11253490
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
17
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| Complexity |
278
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| Defined Atom Stereocenter Count |
2
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| SMILES |
B([C@@H]1CCCN1C(=O)CN[C@@H]2CCNC2)(O)O
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| InChi Key |
DVJAMEIQRSHVKC-BDAKNGLRSA-N
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| InChi Code |
InChI=1S/C10H20BN3O3/c15-10(7-13-8-3-4-12-6-8)14-5-1-2-9(14)11(16)17/h8-9,12-13,16-17H,1-7H2/t8-,9+/m1/s1
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| Chemical Name |
Boronic acid, ((2R)-1-(((3R)-3-pyrrolidinylamino)acetyl)-2-pyrrolidinyl)-
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| Synonyms |
Dutogliptin PHX 1149 PHX1149 PHX-1149
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~300 mg/mL (~1244.30 mM)
H2O : ~100 mg/mL (~414.77 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 7.5 mg/mL (31.11 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 75.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 7.5 mg/mL (31.11 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 75.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 7.5 mg/mL (31.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.1477 mL | 20.7383 mL | 41.4766 mL | |
| 5 mM | 0.8295 mL | 4.1477 mL | 8.2953 mL | |
| 10 mM | 0.4148 mL | 2.0738 mL | 4.1477 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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