| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| 500mg |
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| 1g |
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| Other Sizes |
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| ln Vivo |
PW0787 (0.3, 1, 3 or 10 mg/kg; IP) displays antipsychotic-like activity by significantly inhibiting amphetamine-induced hyperlocomotor behavior in mice [1]. PW0787 was evaluated in rats following a single oral (PO) dose of 20 mg/kg or intravenous (IV) administration of 10 mg/kg. PW0787 has excellent plasma exposure after PO (AUC0-inf = 13,749 ng·h/mL) and IV administration (AUC0-inf=9030 ng·h/mL), as well as high post-PO maximum serum concentration (Cmax= 3407 ng/mL). mL) and IV administration (Cmax=6726 ng/mL). In addition, PW0787 showed good plasma volume of distribution (Vss=1.5 L/kg) and acceptable plasma clearance (CL=1.1 L/h/kg) after 10 mg/kg IV. Excellent oral bioavailability (F) was observed, with a value of 76% [1].
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| Animal Protocol |
Animal/Disease Models: Naive male C57/BL6 black mouse weighing between 24 and 31 g
Doses: 0.3, 1, 3 or 10 mg/kg (dissolve in 0.9% saline containing 20% HP-β-CD, adjust solution (final pH) to 7.4) Route of Administration: IP Experimental Results: Both the 3 mg/kg and 10 mg/kg doses inhibited amphetamine (AMPH)-induced horizontal activity. |
| References |
[1]. Wang P, et al. Discovery of Potent and Brain-Penetrant GPR52 Agonist that Suppresses Psychostimulant Behavior. J Med Chem. 2020;63(22):13951-13972.
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| Molecular Formula |
C23H20F4N4O2
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|---|---|
| Molecular Weight |
460.433
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| Exact Mass |
460.15
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| Elemental Analysis |
C, 60.00; H, 4.38; F, 16.50; N, 12.17; O, 6.95
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| CAS # |
2624131-45-7
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| SMILES |
O=C(C1=CC=CC2=C1CCN2C3=NC=NC(CC4=CC(C(F)(F)F)=CC(F)=C4)=C3)NCCO
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| InChi Key |
OLNVWBLTVAPNME-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H20F4N4O2/c24-16-9-14(8-15(11-16)23(25,26)27)10-17-12-21(30-13-29-17)31-6-4-18-19(2-1-3-20(18)31)22(33)28-5-7-32/h1-3,8-9,11-13,32H,4-7,10H2,(H,28,33)
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| Chemical Name |
1-(6-(3-fluoro-5-(trifluoromethyl)benzyl)pyrimidin-4-yl)-N-(2-hydroxyethyl)indoline-4-carboxamide
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| Synonyms |
PW0787; PW 0787; PW-0787;
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~50 mg/mL (~108.60 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.43 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 (5.43 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1719 mL | 10.8594 mL | 21.7188 mL | |
| 5 mM | 0.4344 mL | 2.1719 mL | 4.3438 mL | |
| 10 mM | 0.2172 mL | 1.0859 mL | 2.1719 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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