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25mg |
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Purity: = 100%
PF-04418948 is a novel, potent and selective prostaglandin EP2 receptor antagonist. PF-04418948, with an apparent KB of 5.4 nM, caused a parallel, rightward shift in the butaprost-induced inhibition of the contractions induced by electrical field stimulation in the human myometrium. PF-04418948 caused the PGE2-induced relaxation curve in the dog bronchiole and the mouse trachea to shift parallel rightward, with KB values of 2.5 nM and apparent KB values of 1.3 nM, respectively. PF-04418948 produced an IC50 value of 2.7 nM when it reversed the PGE2-induced relaxation in the mouse trachea.
Targets |
EP2 ( IC50 = 16 nM )
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ln Vitro |
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ln Vivo |
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Animal Protocol |
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References |
Molecular Formula |
C23H20FNO5
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Molecular Weight |
409.41
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Exact Mass |
409.13
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Elemental Analysis |
C, 67.48; H, 4.92; F, 4.64; N, 3.42; O, 19.54
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CAS # |
1078166-57-0
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Related CAS # |
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Appearance |
Solid powder
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SMILES |
COC1=CC2=C(C=C1)C=C(C=C2)OCC3(CN(C3)C(=O)C4=CC=C(C=C4)F)C(=O)O
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InChi Key |
LWJGMYMNSNVCEM-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C23H20FNO5/c1-29-19-8-4-17-11-20(9-5-16(17)10-19)30-14-23(22(27)28)12-25(13-23)21(26)15-2-6-18(24)7-3-15/h2-11H,12-14H2,1H3,(H,27,28)
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Chemical Name |
1-(4-fluorobenzoyl)-3-[(6-methoxynaphthalen-2-yl)oxymethyl]azetidine-3-carboxylic acid
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Synonyms |
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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 |
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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) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.5 mg/mL (15.88 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.6 mg/mL (6.35 mM) (saturation unknown) in 2% DMSO + 40% PEG300 + 5% Tween80 + 53% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.11 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. Solubility in Formulation 4: ≥ 2.5 mg/mL (6.11 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 25.0 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. Solubility in Formulation 5: ≥ 2.5 mg/mL (6.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 6: 5% DMSO + 95% Corn oil: 0.5mg/ml (1.22mM) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4425 mL | 12.2127 mL | 24.4254 mL | |
5 mM | 0.4885 mL | 2.4425 mL | 4.8851 mL | |
10 mM | 0.2443 mL | 1.2213 mL | 2.4425 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 |
NCT01002963 | Completed | Drug: PF-04418948 | Healthy | Pfizer | September 2009 | Phase 1 |
EP2receptor-driven responses: relaxation of isolated mouse tracheal tissue. EP1receptor-mediated responses: contraction of guinea pig isolated tracheal tissue.Br J Pharmacol.2013 Jan;168(1):129-38. th> |
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EP2receptor-driven responses: relaxation of guinea pig isolated tracheal tissue. EP3receptor-mediated responses: depolarization of guinea pig isolated vagal tissue. td> |
EP4receptor-mediated responses: relaxation of rat and human isolated tracheal tissue.Br J Pharmacol.2013 Jan;168(1):129-38. td> |