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1238697-26-1-TAK-063 TAK-063

TAK-063

For research use only. Not for therapeutic Use.

  • CAT Number: I000951
  • CAS Number: 1238697-26-1
  • Molecular Formula: C₂₃H₁₇FN₆O₂
  • Molecular Weight: 428.42
  • Purity: ≥95%
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Related Small Molecules: Etelcalcetide HCl     LL-37 scrambled peptide acetate     PKG Substrate    

TAK-063（Cat No.:I000951）is an investigational small molecule compound developed by Takeda Pharmaceuticals, designed as a selective antagonist of the metabotropic glutamate receptor 1 (mGluR1). This receptor is involved in synaptic signaling in the brain and has been implicated in various neuropsychiatric disorders, including schizophrenia, anxiety, and depression. By inhibiting mGluR1, TAK-063 aims to modulate glutamate transmission, potentially alleviating symptoms of these conditions. Preclinical and clinical studies have shown promise in treating disorders linked to dysregulated glutamatergic activity. However, further trials are needed to evaluate its safety, efficacy, and long-term therapeutic potential.


Catalog Number I000951
CAS Number 1238697-26-1
Synonyms

TAK063; TAK 063

Molecular Formula C₂₃H₁₇FN₆O₂
Purity ≥95%
Target Phosphodiesterase (PDE)
Solubility 10 mM in DMSO
Storage -20°C
IC50 0.3 nM
IUPAC Name 1-(2-fluoro-4-pyrazol-1-ylphenyl)-5-methoxy-3-(2-phenylpyrazol-3-yl)pyridazin-4-one
InChI 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
InChIKey KVHRYLNQDWXAGI-UHFFFAOYSA-N
SMILES COC1=CN(N=C(C1=O)C2=CC=NN2C3=CC=CC=C3)C4=C(C=C(C=C4)N5C=CC=N5)F
Reference

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1:A strategy to improve the success rate of CNS drug development: TAK-063, a novel PDE10A inhibitor, as a case study. Kimura H.Nihon Yakurigaku Zasshi. 2017;149(4):160-166. doi: 10.1254/fpj.149.160. No abstract available. PMID: 28381659 <br />
2:TAK-063, a Novel Phosphodiesterase 10A Inhibitor, Protects from Striatal Neurodegeneration and Ameliorates Behavioral Deficits in the R6/2 Mouse Model of Huntington/’s Disease. Harada A, Suzuki K, Kimura H.J Pharmacol Exp Ther. 2017 Jan;360(1):75-83. Epub 2016 Nov 3. PMID: 27811172 <br />
3:TAK-063, a phosphodiesterase 10A inhibitor, modulates neuronal activity in various brain regions in phMRI and EEG studies with and without ketamine challenge. Tomimatsu Y, Cash D, Suzuki M, Suzuki K, Bernanos M, Simmons C, Williams SC, Kimura H.Neuroscience. 2016 Dec 17;339:180-190. doi: 10.1016/j.neuroscience.2016.10.006. Epub 2016 Oct 8. PMID: 27725212 <br />
4:A phase 1 study of the safety, tolerability, pharmacokinetics, and pharmacodynamics of TAK-063, a selective PDE10A inhibitor. Tsai M, Chrones L, Xie J, Gevorkyan H, Macek TA.Psychopharmacology (Berl). 2016 Oct;233(21-22):3787-3795. Epub 2016 Aug 30. PMID: 27572830 Free PMC Article<br />
5:A human [(11)C]T-773 PET study of PDE10A binding after oral administration of TAK-063, a PDE10A inhibitor. Takano A, Stenkrona P, Stepanov V, Amini N, Martinsson S, Tsai M, Goldsmith P, Xie J, Wu J, Uz T, Halldin C, Macek TA.Neuroimage. 2016 Nov 1;141:10-7. doi: 10.1016/j.neuroimage.2016.06.047. Epub 2016 Jul 15. PMID: 27423256 <br />
6:Brain PET measurement of PDE10A occupancy by TAK-063, a new PDE10A inhibitor, using [11 C]T-773 in nonhuman primates. Takano A, Stepanov V, Nakao R, Amini N, Gulyás B, Kimura H, Halldin C.Synapse. 2016 Jun;70(6):253-63. doi: 10.1002/syn.21896. Epub 2016 Mar 4. PMID: 26878349 <br />
7:TAK-063, a PDE10A Inhibitor with Balanced Activation of Direct and Indirect Pathways, Provides Potent Antipsychotic-Like Effects in Multiple Paradigms. Suzuki K, Harada A, Suzuki H, Miyamoto M, Kimura H.Neuropsychopharmacology. 2016 Aug;41(9):2252-62. doi: 10.1038/npp.2016.20. Epub 2016 Feb 5. PMID: 26849714 <br />
8:The Phosphodiesterase 10A Selective Inhibitor TAK-063 Improves Cognitive Functions Associated with Schizophrenia in Rodent Models. Shiraishi E, Suzuki K, Harada A, Suzuki N, Kimura H.J Pharmacol Exp Ther. 2016 Mar;356(3):587-95. doi: 10.1124/jpet.115.230482. Epub 2015 Dec 16. PMID: 26675680 Free Article<br />
9:Characterization of binding and inhibitory properties of TAK-063, a novel phosphodiesterase 10A inhibitor. Harada A, Suzuki K, Kamiguchi N, Miyamoto M, Tohyama K, Nakashima K, Taniguchi T, Kimura H.PLoS One. 2015 Mar 27;10(3):e0122197. doi: 10.1371/journal.pone.0122197. eCollection 2015. PMID: 25815469 Free PMC Article<br />
10:In vivo pharmacological characterization of TAK-063, a potent and selective phosphodiesterase 10A inhibitor with antipsychotic-like activity in rodents. Suzuki K, Harada A, Shiraishi E, Kimura H.J Pharmacol Exp Ther. 2015 Mar;352(3):471-9. doi: 10.1124/jpet.114.218552. Epub 2014 Dec 18. PMID: 25525190 Free Article

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