1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. Balipodect

Balipodect (Synonyms: TAK-063)

Cat. No.: HY-12472 Purity: 98.69%
Handling Instructions

Balipodect (TAK-063) is a highly potent, selective and orally active PDE10A inhibitor with IC50 of 0.30 nM; >15000-fold selectivity over other PDEs.

For research use only. We do not sell to patients.

Balipodect Chemical Structure

Balipodect Chemical Structure

CAS No. : 1238697-26-1

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Solution
10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 92 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 84 In-stock
Estimated Time of Arrival: December 31
10 mg USD 108 In-stock
Estimated Time of Arrival: December 31
50 mg USD 300 In-stock
Estimated Time of Arrival: December 31
100 mg USD 528 In-stock
Estimated Time of Arrival: December 31
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Description

Balipodect (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 & Target

IC50: 0.3 nM (PDE10A)[1].

In Vivo

Balipodect (TAK-063) has excellent selectivity (>15000-fold selectivity over other PDEs), and favorable pharmacokinetics, including high brain penetration, in mice. Oral administration of Balipodect (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].
Balipodect (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. Balipodect (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. Balipodect (TAK-063) did not affect plasma prolactin or glucose levels at doses up to 3 mg/kg, p.o. Balipodect (TAK-063) at 3 mg/kg, p.o., elicited a weak cataleptic response compared with haloperidol and olanzapine[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

428.42

Formula

C₂₃H₁₇FN₆O₂

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (58.35 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.84 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.84 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Product Name:
Balipodect
Cat. No.:
HY-12472
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