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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
| ln Vitro |
MRP2 and BCRP were found to be substrates of CP-671,305, but not MDR1. While CP-671,305 is not a substrate of human OATP1B1 or OATP1B3, it is a high affinity substrate of human OATP2B1 (Km=4 μM). High affinity (Km=12 μM) for rat liver Oatp1a4 is demonstrated by CP-671,305[1]. CP-671,305 does not show competitive inhibition (IC50 > 50 μM) against CYP1A2, 2C9, 2C19, 2D6, and 3A4, the five major cytochrome P450 enzymes. Similarly, CP-671,305 did not cause any of the five major cytochrome P450 enzymes to become inactive over time [2].
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| ln Vivo |
CP-671,305 exhibits generally good pharmacokinetic properties, with systemic plasma clearance rates in Sprague-Dawley rats (9.60 ± 1.16 mL/min/kg) and beagle dogs (2.90 ± 0.81 mL/min/kg) after intravenous injection and lower in cynomolgus monkeys (2.94 ± 0.87 mL/min/kg) resulting in a plasma half-life > 5 hours. Following oral administration, moderate to high bioavailability was observed in rats (43-80%), dogs (45%), and monkeys (26%). In rats, oral pharmacokinetics are dose-dependent over the dose range studied (10 and 25 mg/kg) [2].
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| References |
[1]. Kalgutkar AS, et al. Role of transporters in the disposition of the selective phosphodiesterase-4 inhibitor (+)-2-[4-({[2-(benzo[1,3]dioxol-5-yloxy)-pyridine-3-carbonyl]-amino}-methyl)-3-fluoro-phenoxy]-propionic acid in rat and human. Drug Metab Dispos. 2007 Nov;35(11):2111-8. Epub 2007 Aug 8.
[2]. Kalgutkar AS, et al. Disposition of CP-671, 305, a selective phosphodiesterase 4 inhibitor in preclinical species. Xenobiotica. 2004 Aug;34(8):755-70 |
| Molecular Formula |
C23H19FN2O7
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|---|---|
| Molecular Weight |
454.40
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| CAS # |
445295-04-5
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| SMILES |
C[C@@H](Oc1ccc(CNC(=O)c2cccnc2Oc3ccc4OCOc4c3)c(F)c1)C(=O)O
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| InChi Key |
CNIGFESSDPOCKS-CYBMUJFWSA-N
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| InChi Code |
InChI=1S/C23H19FN2O7/c1-13(23(28)29)32-15-5-4-14(18(24)9-15)11-26-21(27)17-3-2-8-25-22(17)33-16-6-7-19-20(10-16)31-12-30-19/h2-10,13H,11-12H2,1H3,(H,26,27)(H,28,29)/t13-/m1/s1
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| Chemical Name |
(R)-2-(4-((((2-((Benzo(1,3)dioxol-5-yl)oxy)pyridin-3-yl)carbonyl)amino)methyl)-3-fluorophenoxy)propionic acid
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| Synonyms |
CP-671305; CP 671305; CP671305; UNII-9LH034R9R9.
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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 (~220.07 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.50 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 25.0 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: ≥ 2.5 mg/mL (5.50 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.50 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 | 2.2007 mL | 11.0035 mL | 22.0070 mL | |
| 5 mM | 0.4401 mL | 2.2007 mL | 4.4014 mL | |
| 10 mM | 0.2201 mL | 1.1004 mL | 2.2007 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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