Balipodect (Synonyms: TAK-063) |
Catalog No.GC19343
One-Click Copy Product Info
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Balipodect(TAK-063)는 IC50이 0.30nM인 매우 강력하고 선택적이고 경구 활성인 PDE10A 억제제입니다. 다른 PDE에 비해 >15000배 선택성.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1238697-26-1
Sample solution is provided at 25 µL, 10mM.
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TAK-063 is a highly potent, selective and orally active PDE10A inhibitor with IC50 of 0.30 nM; >15000-fold selectivity over other PDEs.IC50 value: 0.3 nM [1]Target: PDE10A inhibitorTAK-063 has potent inhibitory activity (IC50 = 0.30 nM), 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 [1]. TAK-063 at 0.3 and 1 mg/kg, p.o., increased cAMP and cGMP levels in the rodent striatum and upregulated phosphorylation levels of key substrates of cAMP-dependent and cGMP-dependent protein kinases. TAK-063 at 0.3 and 1 mg/kg, p.o., strongly suppressed MK-801-induced hyperlocomotion that is often used as a predictive model for antipsychotic-like activity in rodents. TAK-063 did not affect plasma prolactin or glucose levels at doses up to 3 mg/kg, p.o. TAK-063 at 3 mg/kg, p.o., elicited a weak cataleptic response compared with haloperidol and olanzapine [2].
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(22):9627-43.
[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.
Animal experiment: | Mice[1]Compound 27h was suspended in 0.5% (w/v) methylcellulose in distilled water. Compound 27h was administered orally (po). PCP hydrochloride (lot no. 010M4010) purchased from Sigma-Aldrich, Inc. (USA) was dissolved in saline and was administered subcutaneously (sc). All compounds were dosed in a volume of 20 mL/kg body weight. Hyperlocomotion was measured using a spontaneous motor analyzer MDC system (BrainScience idea. Co. Ltd., Japan). Mice were placed in locomotor chambers for more than 60 min for habituation. Animals were removed from each chamber and treated with either vehicle or compound 27h and then quickly returned to the chamber. The following doses were used: 0.1, 0.3, and 1.0 mg/kg, po. Sixty minutes after treatment with compound 27h, animals were again removed from the chambers and treated with either vehicle (saline) or PCP (5 mg/kg as a salt, sc) and then quickly transferred to the test chamber. Activity counts were recorded in successive 1 min bins, and the total number counts were determined for the 120 min period after PCP administration. |
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(22):9627-43. | |
| Cas No. | 1238697-26-1 | SDF | |
| Synonyms | TAK-063 | ||
| Canonical SMILES | FC1=CC(N2N=CC=C2)=CC=C1N3N=C(C4=CC=NN4C5=CC=CC=C5)C(C(OC)=C3)=O | ||
| Formula | C23H17FN6O2 | M.Wt | 428.42 |
| Solubility | DMSO : 25 mg/mL (58.35 mM);Water : < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3342 mL | 11.6708 mL | 23.3416 mL |
| 5 mM | 466.8 μL | 2.3342 mL | 4.6683 mL |
| 10 mM | 233.4 μL | 1.1671 mL | 2.3342 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 11 reference(s) in Google Scholar.)