Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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Other Sizes |
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Purity: ≥98%
PF-06291874 is a novel, highly potent glucagon receptor antagonist with favorable pharmacokinetics such as low in vivo clearance and excellent oral bioavailability in both rats and dogs. PF-06291874 has the potential to be beneficial in the treatment of individuals with type 2 diabetes. PF-06291874 reduces glucose levels with a low risk of hypoglycemia and has a good pharmacokinetic profile that makes it suitable for once-daily dosing. It was also well tolerated.
ln Vitro |
PF-06291874 exposure has a half-life of roughly 19.7–22.7 hours and is roughly dose-proportional. The rate of PF-06291874 is quick on and off. PF-06291874 has a mean free fraction of approximately 0.55% and is strongly bound to human plasma protein[3].
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ln Vivo |
Exposure to PF-06291874 is approximately dose-proportional, with a half-life of ∼19.7-22.7 hours. PF-06291874 has fast opening and closing rates. PF-06291874 is highly bound to human plasma proteins with an average free fraction of ∼0.55% [3].
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References |
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Molecular Formula |
C26H28F3N3O4
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Molecular Weight |
503.5134
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Exact Mass |
503.2
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Elemental Analysis |
C, 62.02; H, 5.61; F, 11.32; N, 8.35; O, 12.71
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CAS # |
1393124-08-7
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Appearance |
Solid powder
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SMILES |
CCC[C@@H](C1=CC=C(C=C1)C(=O)NCCC(=O)O)OC2=CC(=C(C(=C2)C)N3C=C(C=N3)C(F)(F)F)C
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InChi Key |
IBDYYOQKQCCSDP-QFIPXVFZSA-N
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InChi Code |
InChI=1S/C26H28F3N3O4/c1-4-5-22(18-6-8-19(9-7-18)25(35)30-11-10-23(33)34)36-21-12-16(2)24(17(3)13-21)32-15-20(14-31-32)26(27,28)29/h6-9,12-15,22H,4-5,10-11H2,1-3H3,(H,30,35)(H,33,34)/t22-/m0/s1
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Chemical Name |
3-[[4-[(1S)-1-[3,5-dimethyl-4-[4-(trifluoromethyl)pyrazol-1-yl]phenoxy]butyl]benzoyl]amino]propanoic acid
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Synonyms |
PF6291874; PF-06291874; PF-6291874; PF 6291874; PF 06291874; PF06291874
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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 |
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: ~100 mg/mL (~198.6 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.13 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 20.8 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: ≥ 2.08 mg/mL (4.13 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 20.8 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: ≥ 2.08 mg/mL (4.13 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 | 1.9861 mL | 9.9303 mL | 19.8606 mL | |
5 mM | 0.3972 mL | 1.9861 mL | 3.9721 mL | |
10 mM | 0.1986 mL | 0.9930 mL | 1.9861 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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT01794364 | Completed | Drug: PF-06291874 Other: placebo |
Healthy | Pfizer | January 2013 | Phase 1 |
NCT01856595 | Completed | Drug: PF-06291874 Drug: Placebo |
Diabetes Mellitus, Type 2 | Pfizer | May 13, 2013 | Phase 1 |
NCT02554877 | Completed | Drug: PF-06291874 Drug: Placebo |
Type 2 Diabetes Mellitus | Pfizer | October 2015 | Phase 2 |
NCT02175121 | Completed | Drug: PF-06291874 Drug: Placebo |
Diabetes Mellitus, Type II | Pfizer | August 2014 | Phase 2 |
NCT01499017 | Terminated | Drug: PF-06291874 or placebo Drug: PF-06291874 or Placebo |
Healthy | Pfizer | November 2011 | Phase 1 |