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| 5mg |
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Purity: ≥98%
Balipodect (formerly also known as TAK-063) is a novel, highly potent, orally bioavailable and selective phosphodiesterase 10A (PDE10A) inhibitor with potential usefulness in the treatment of schizophrenia. It inhibits PDE10A with an IC50 of 0.30 nM. TAK-063 has also excellent selectivity (>15000-fold selectivity over other PDEs), and favorable pharmacokinetics, including high brain penetration, in mice. Oral administration of TAK-063 to mice elevated striatal 3',5'-cyclic adenosine monophosphate (cAMP) and 3',5'-cyclic guanosine monophosphate (cGMP) levels at 0.3 mg/kg and showed potent suppression of phencyclidine (PCP)-induced hyperlocomotion at a minimum effective dose (MED) of 0.3 mg/kg.
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Balipodect (TAK-063) exhibits favorable pharmacokinetics, including high brain penetration in mice, and excellent selectivity (>15000-fold selectivity over other PDEs). When mice were given Balipodect (TAK-063) orally, their striatal levels of 3',5'-cyclic adenosine monophosphate (cAMP) and 3',5'-cyclic guanosine monophosphate (cGMP) increased to 0.3 mg/kg. Additionally, at a minimum effective dose (MED) of 0.3 mg/kg, there was a significant suppression of phencyclidine (PCP)-induced hyperlocomotion[1]. At 0.3 and 1 mg/kg, po, balipodect (TAK-063) raised the levels of cAMP and cGMP in the rodent striatum and elevated the phosphorylation of important substrates of cAMP-dependent and cGMP-dependent protein kinases. At 0.3 and 1 mg/kg, po, balipodect (TAK-063) significantly reduced the hyperlocomotion induced by MK-801, which is frequently utilized as a model to predict antipsychotic-like activity in rodents. When combined with haloperidol and olanzapine, balipodect (TAK-063) at 3 mg/kg, po, elicited a weak cataleptic response[2]. At doses up to 3 mg/kg, po, balipodect (TAK-063) did not affect plasma prolactin or glucose levels.
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| References |
[1]. Kunitomo J, et al. Discovery of 1-[2-Fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one (TAK-063), a Highly Potent, Selective, and Orally Active Phosphodiesterase 10A (PDE10A) Inhibitor. J Med Chem. 2014 Nov 26;57(
[2]. Suzuki K, et al. In Vivo Pharmacological Characterization of TAK-063, a Potent and Selective Phosphodiesterase 10A Inhibitor with Antipsychotic-Like Activity in Rodents. J Pharmacol Exp Ther. 2014 Dec 18. pii: jpet.114.218552 |
| Molecular Formula |
C23H17FN6O2
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| Molecular Weight |
428.42
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| CAS # |
1238697-26-1
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| Related CAS # |
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| SMILES |
FC1C([H])=C(C([H])=C([H])C=1N1C([H])=C(C(C(C2=C([H])C([H])=NN2C2C([H])=C([H])C([H])=C([H])C=2[H])=N1)=O)OC([H])([H])[H])N1C([H])=C([H])C([H])=N1
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| InChi Key |
KVHRYLNQDWXAGI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H17FN6O2/c1-32-21-15-29(19-9-8-17(14-18(19)24)28-13-5-11-25-28)27-22(23(21)31)20-10-12-26-30(20)16-6-3-2-4-7-16/h2-15H,1H3
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| Chemical Name |
1-(2-fluoro-4-(1H-pyrazol-1-yl)phenyl)-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one
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| Synonyms |
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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: ≥ 2.5 mg/mL (5.84 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 (5.84 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 | 2.3342 mL | 11.6708 mL | 23.3416 mL | |
| 5 mM | 0.4668 mL | 2.3342 mL | 4.6683 mL | |
| 10 mM | 0.2334 mL | 1.1671 mL | 2.3342 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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