TAK-063

SKU: orb1226695

Description

TAK-063 (Balipodect) is a highly potent, selective, orally active PDE10A inhibitor with IC50 of 0.3 nM, displays >15,000-fold selectivity over other PDE subtypes; increases cAMP and cGMP levels in the rodent striatum and upregulates phosphorylation levels of key substrates of cAMP- and cGMP-dependent protein kinases, strongly suppresses MK-801-induced hyperlocomotion in rodents (0.3 and 1 mg/kg p.o), improves cognitive functions associated with schizophrenia in rodent models,Schizophrenia Phase 2 Discontinued(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.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.

Key Properties

• CAS Number: 1238697-26-1
• MW: 428.4185
• Purity: >98% (HPLC)
• Formula: C₂₃H₁₇FN₆O₂
• SMILES: O=C1C(C2=CC=NN2C3=CC=CC=C3)=NN(C4=CC=C(N5N=CC=C5)C=C4F)C=C1OC
• Target: PDE
• Solubility: 10 mM in DMSO

Bioactivity

• 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. 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

TAK063 | Balipodect

Quick Database Links

Gene Symbol

PDE