TAK-653
- CAS No.
- 1358751-06-0
- Chemical Name:
- TAK-653
- Synonyms
- TAK-653;Osavampator;NBI-1065845);Osavampator(TAK-653;9-[4-(cyclohexyloxy)phenyl]-7-methyl-3H,4H-2λ?-pyrazino[2,1-c][1,2,4]thiadiazine-2,2-dione;9-(4-(Cyclohexyloxy)phenyl)-7-methyl-3,4-dihydropyrazino[2,1-c][1,2,4]thiadiazine 2,2-dioxide;Pyrazino[2,1-c][1,2,4]thiadiazine, 9-[4-(cyclohexyloxy)phenyl]-3,4-dihydro-7-methyl-, 2,2-dioxide
- CBNumber:
- CB38244135
- Molecular Formula:
- C19H23N3O3S
- Molecular Weight:
- 373.47
- MDL Number:
- MOL File:
- 1358751-06-0.mol
| Boiling point | 540.8±52.0 °C(Predicted) |
|---|---|
| Density | 1.38±0.1 g/cm3(Predicted) |
| storage temp. | Store at -20°C |
| 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 |
| FDA UNII | 9E3TOE5RIZ |
TAK-653 Chemical Properties,Uses,Production
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
[3] 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. Pharmacol Biochem Behav. 2021 Dec;211:173289. DOI:10.1016/j.pbb.2021.173289
TAK-653 Preparation Products And Raw materials
Raw materials
Preparation Products
TAK-653 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Xi an Biohorlden Industry Trade Co Ltd | +86-18829283179 +86-13636819721 | sales@horlden.com | China | 236 | 58 |
| Nantong Guangyuan Chemicl Co,Ltd | +undefined17712220823 | admin@guyunchem.com | China | 615 | 58 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32202 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10473 | 58 |
| Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | sales@chemhifuture.com | China | 3135 | 58 |
| Wuhan senwayer century chemical Co.,Ltd | +undefined-27-86652399 +undefined13627115097 | market02@senwayer.com | China | 923 | 58 |
| Hebei Miaoyin Technology Co.,Ltd | +86-17367732028 +86-17367732028 | kathy@hbyinsheng.com | China | 3512 | 58 |
| WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd. | 17702719238 17702719238 | sales@sun-shinechem.com | China | 1015 | 64 |
| ShangHai Caerulum Pharma Discovery Co., Ltd. | 18149758185 18149758185 | sales-cpd@caerulumpharma.com | China | 3466 | 58 |
View Lastest Price from TAK-653 manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2025-04-27 | TAK-653
1358751-06-0
|
US $58.00-188.00 / mg | 99.18% | 10g | TargetMol Chemicals Inc. | ||
 |
2025-04-18 | TAK-653
1358751-06-0
|
US $0.00-0.00 / g | 1g | 98% | 200g | Xi an Biohorlden Industry Trade Co Ltd | |
 |
2024-09-25 | TAK-653
1358751-06-0
|
US $0.00 / kg | 1kg | 99% min | 20 tons | Wuhan Senwayer Century Chemical Co.,Ltd |