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Purity: ≥98%
PF-06256142 is a novel, potent and selective orthosteric agonist of the D1 receptor with D1 EC50 of 30 nM and D1 binding Ki of 12 nM. In comparison to other catechol-containing agonists and dopamine, it has lessened receptor desensitization. For the better part of four decades, the search for D1 subtype-selective agonists possessing drug-like qualities has been an ongoing challenge. As catecholamines, all known D1-selective agonists cause receptor desensitization and have fast metabolisms, which limits their use as treatments for long-term conditions like schizophrenia and Parkinson's disease. Our high-throughput screening efforts on D1 yielded a single non-catecholamine hit PF-4211 (6) that was developed into a series of potent D1 receptor agonist leads with high oral bioavailability and CNS penetration. This series' locked biaryl ring system, which causes atropisomerism, is a crucial structural component.
| Targets |
Human D1 Receptor ( IC50 = 33 nM )
|
|---|---|
| ln Vitro |
PF-06256142, an antagonist, demonstrates IC50 values less than 5 μM at the following 4 targets: H1 (4.6 μM), M1 (4.9 μM), CB1 (2.1 μM), and Nav 1.5 (1.1 μM) [1].
PF-06256142 exhibits an IC50 for hERG of roughly 12 μM [1]. PF-06256142 demonstrates a 4.8 nM Ki for D5, which is significantly more selective than D2 (Ki>10 μM)[1]. |
| ln Vivo |
PF-06256142 shows a strong oral bioavailability (rat 85%) after oral dosing (5 mg/kg)[1].
PF-06256142 has a terminal elimination half-life (2.3 hours) in rats after being injected intravenously at a dose of 5.0 mg/kg[1]. |
| Animal Protocol |
Rat
5.0 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis) Intravenous injection and oral administration |
| References |
| Molecular Formula |
C21H16N4O2
|
|---|---|
| Molecular Weight |
356.37734413147
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| Exact Mass |
356.13
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| Elemental Analysis |
C, 70.77; H, 4.53; N, 15.72; O, 8.98
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| CAS # |
1609583-14-3
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| Related CAS # |
(Rac)-PF-06256142; 1609580-97-3; (R)-PF-06256142; 1609583-15-4
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| PubChem CID |
75201901
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| Appearance |
Solid powder
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| LogP |
4.3
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
|
| Heavy Atom Count |
27
|
| Complexity |
520
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
HWAIAGZSWHOLLK-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C21H16N4O2/c1-13-11-15(27-21-17-6-10-26-18(17)5-7-23-21)3-4-16(13)20-14(2)24-12-19-22-8-9-25(19)20/h3-12H,1-2H3
|
| Chemical Name |
4-[3-methyl-4-(6-methylimidazo[1,2-a]pyrazin-5-yl)phenoxy]furo[3,2-c]pyridine
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| Synonyms |
PF-06256142; PF 06256142; PF06256142
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| HS Tariff Code |
2934.99.03.00
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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: ~200 mg/mL (~561.2 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (14.03 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 50.0 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: ≥ 5 mg/mL (14.03 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 50.0 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: ≥ 5 mg/mL (14.03 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 | 2.8060 mL | 14.0300 mL | 28.0599 mL | |
| 5 mM | 0.5612 mL | 2.8060 mL | 5.6120 mL | |
| 10 mM | 0.2806 mL | 1.4030 mL | 2.8060 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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