ChemicalBook Product Catalog Organic Chemistry Heterocyclic Compounds TAK-653

TAK-653

Product NameTAK-653
CAS1358751-06-0
MFC19H23N3O3S
MW373.47
EINECS
MOL File1358751-06-0.mol

Chemical Properties

Boiling point	540.8±52.0 °C(Predicted)
Density	1.38±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMSO: Slightly soluble: 0.1-1 mg/ml
pka	1.71±0.40(Predicted)
form	Solid
color	White to yellow
InChI	InChI=1S/C19H23N3O3S/c1-14-13-22-11-12-26(23,24)21-19(22)18(20-14)15-7-9-17(10-8-15)25-16-5-3-2-4-6-16/h7-10,13,16H,2-6,11-12H2,1H3
InChIKey	PXJBHEHFVQVDDS-UHFFFAOYSA-N
SMILES	S1(=O)(=O)CCN2C=C(C)N=C(C3=CC=C(OC4CCCCC4)C=C3)C2=N1

Usage And Synthesis

Uses

Osavampator (TAK-653) is a AMPA receptor positive allosteric modulator. Osavampator selectively binds to AMPA-R in a glutamate-dependent manner and induces Ca2+ influx in hGluA1i CHO cells (EC50 = 3.3 μM). Osavampator improves learning and memory in many models. Osavampator is can be used for the research of depressive disorders[1][2].

Biological Functions

TAK-653 is a selective positive allosteric modulator (PAM) of AMPA receptors exhibiting minimal agonistic activity, elicits an antidepressant-like response while maintaining a favorable safety profile in rat models.

in vivo

Osavampator (0.03-0.3 mg/kg, p.o., single dose) enhances visual learning and memory in normal rats^[2].
Osavampator (0.3 mg/kg, p.o., single dose) enhances sustained attention in the poor performing rats^[2].
Osavampator (0.06 mg/kg, p.o., single dose) improves working memory in monkeys^[2].
Osavampator (1 mg/kg, p.o., single dose) produces antidepressant-like effects in the rat RSBM (reduction of submissive behavior model)^[1].

Animal Model:	Normal rats^[2]
Dosage:	0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg
Administration:	Oral gavage (p.o.)
Result:	Improved the novelty discrimination index (NDI).

Animal Model:	Poor performing rats^[2]
Dosage:	0.3 mg/kg
Administration:	Oral gavage (p.o.)
Result:	Increased correct responses and decreased omissions in the poor performing rats.

Animal Model:	Fasted monkey^[2]
Dosage:	0.06 mg/kg
Administration:	Oral gavage (p.o.)
Result:	Significantly increased delayed match-to-sample (DMTS) accuracy at a 16-s delay interval. Maintained the beneficial effect 24 h after administration.

Animal Model:	submissive behavior model ^[1]
Dosage:	0.1 mg/kg, 1 mg/kg
Administration:	Oral gavage (p.o.)
Result:	Led to a significant reduction in dominance levels compared with vehicle treatment starting from the seventh day of treatment and maintained throughout the study period. Had a significant effect in reducing dominance levels at 0.1 and 1 mg/kg.

IC 50

5-LO

References

[1] Hara H, et al. TAK-653, an AMPA receptor potentiator with minimal agonistic activity, produces an antidepressant-like effect with a favorable safety profile in rats [J]. Pharmacology Biochemistry and Behavior, 2021, 211: 173289. DOI:10.1016/j.pbb.2021.173289
[2] Suzuki A, et al. Strictly regulated agonist-dependent activation of AMPA-R is the key characteristic of TAK-653 for robust synaptic responses and cognitive improvement [J]. Scientific Reports, 2021, 11(1): 14532. DOI:10.1038/s41598-021-93888-0

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