TAK-653 | CAS#1358751-06-0 | AMPA receptor potentiator

MedKoo Cat#: 465874 | Name: TAK-653

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

TAK-653 is a novel AMPA receptor potentiator, strictly potentiating a glutamate-induced Ca2+ influx in hGluA1i-expressing CHO cells through structural interference at Ser743 in GluA1,

Chemical Structure

TAK-653

CAS#1358751-06-0

Theoretical Analysis

MedKoo Cat#: 465874

Name: TAK-653

CAS#: 1358751-06-0

Chemical Formula: C19H23N3O3S

Exact Mass: 373.1460

Molecular Weight: 373.47

Elemental Analysis: C, 61.10; H, 6.21; N, 11.25; O, 12.85; S, 8.58

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 750.00	2 Weeks

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Related CAS #

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Synonym

TAK-653; TAK653; TAK 653; NBI-1065845; NBI1065845; NBI 1065845; osavampator

IUPAC/Chemical Name

9-(4-(cyclohexyloxy)phenyl)-7-methyl-3,4-dihydropyrazino[2,1-c][1,2,4]thiadiazine 2,2-dioxide

InChi Key

PXJBHEHFVQVDDS-UHFFFAOYSA-N

InChi Code

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

SMILES Code

CC1=CN(CC2)C(C(C3=CC=C(OC4CCCCC4)C=C3)=N1)=NS2(=O)=O

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

To be determined

Shelf Life

>2 years if stored properly

Drug Formulation

To be determined

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 373.47 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Witkin JM, Martin AE, Golani LK, Xu NZ, Smith JL. Rapid-acting antidepressants. Adv Pharmacol. 2019;86:47-96. doi: 10.1016/bs.apha.2019.03.002. Epub 2019 Apr 24. PMID: 31378256. 2: O'Donnell P, Dijkstra FM, Damar U, Quanhong L, de Goede AA, Xu L, Pascual- Leone A, Buhl DL, Zuiker R, Ruijs TQ, Heuberger JAAC, MacMullin P, Lubell M, Asgharnejad M, Murthy V, Rotenberg A, Jacobs GE, Rosen L. Transcranial magnetic stimulation as a translational biomarker for AMPA receptor modulation. Transl Psychiatry. 2021 May 27;11(1):325. doi: 10.1038/s41398-021-01451-2. PMID: 34045439; PMCID: PMC8160137. 3: Suzuki A, Kunugi A, Tajima Y, Suzuki N, Suzuki M, Toyofuku M, Kuno H, Sogabe S, Kosugi Y, Awasaki Y, Kaku T, Kimura H. Strictly regulated agonist-dependent activation of AMPA-R is the key characteristic of TAK-653 for robust synaptic responses and cognitive improvement. Sci Rep. 2021 Jul 15;11(1):14532. doi: 10.1038/s41598-021-93888-0. Erratum in: Sci Rep. 2021 Jul 21;11(1):15255. doi: 10.1038/s41598-021-94772-7. PMID: 34267258; PMCID: PMC8282797. 4: Suzuki A, Kunugi A, Tajima Y, Suzuki N, Suzuki M, Toyofuku M, Kuno H, Sogabe S, Kosugi Y, Awasaki Y, Kaku T, Kimura H. Author Correction: Strictly regulated agonist-dependent activation of AMPA-R is the key characteristic of TAK-653 for robust synaptic responses and cognitive improvement. Sci Rep. 2021 Jul 21;11(1):15255. doi: 10.1038/s41598-021-94772-7. Erratum for: Sci Rep. 2021 Jul 15;11(1):14532. doi: 10.1038/s41598-021-93888-0. PMID: 34290388; PMCID: PMC8295271. 5: Hara H, Suzuki A, Kunugi A, Tajima Y, Yamada R, Kimura H. 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. Epub 2021 Oct 14. PMID: 34655652. 6: Dijkstra F, O'Donnell P, Klaassen E, Buhl D, Asgharnejad M, Rosen L, Zuiker R, van Gerven J, Jacobs G. Central nervous system effects of TAK-653, an investigational alpha-amino-3-hydroxy-5-methyl-4-isoxazole receptor (AMPAR) positive allosteric modulator in healthy volunteers. Transl Psychiatry. 2022 Sep 24;12(1):408. doi: 10.1038/s41398-022-02148-w. PMID: 36153330; PMCID: PMC9509332. 7: Suzuki A, Hara H, Kimura H. Role of the AMPA receptor in antidepressant effects of ketamine and potential of AMPA receptor potentiators as a novel antidepressant. Neuropharmacology. 2023 Jan 1;222:109308. doi: 10.1016/j.neuropharm.2022.109308. Epub 2022 Oct 29. PMID: 36341809. 8: Lin S, Ionescu A, Maynard-Scott J, Kennedy M, Walling DP, Furey M, Singh JB. Effects of the selective AMPA modulator NBI-1065845 on the pharmacokinetics of midazolam or ethinyl estradiol-levonorgestrel in healthy adults. Clin Transl Sci. 2024 May;17(5):e13791. doi: 10.1111/cts.13791. PMID: 38700236; PMCID: PMC11067504. 9: Osaka H, Kanazawa T. Emerging trends in antipsychotic and antidepressant drug development: Targeting nonmonoamine receptors and innovative mechanisms. PCN Rep. 2023 Nov 20;2(4):e157. doi: 10.1002/pcn5.157. PMID: 38868733; PMCID: PMC11114387.