Ramelteon - Moligand™, 10mM in DMSO , Melatonin receptor agonist, CAS No.196597-26-9, Melatonin receptor agonist

CAS: 196597-26-9 Cat. No.: R408222 분자식: C₁₆H₂₁NO₂ 분자량: 259.34 EC 번호: 688-929-3 PubChem CID: 208902

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

TAK-375 | (S)-N-[2-(1,6,7,8-Tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

개요

Information

Ramelteon Ramelteon (TAK-375) is a novel melatonin receptor agonist for human MT1 and MT2 receptors and chick forebrain melatonin receptors with K i of 14 pM, 112 pM and 23.1 pM, respectively.
In vitro

Ramelteon inhibits forskolin-stimulated cAMP production with IC50 of 21.2 pM in CHO cells. Ramelteon has high affinity with recombinant human MT1 and MT2 receptors with pKi of 10.05 and 9.70, respectively. Ramelteon inhibits Xenopus laevis melanophore pigment granule aggregation with pEC50 of 11.48. Ramelteon (1 nM) increases ERK1/2 phosphorylation not only in MT1/MT2 cerebellar granule cells but also in cerebellar granule cells expressing only one of the two melatonin receptors. 4P-PDOT blocks the stimulatory action of Ramelteon (1 nM) in MT1 KO cerebellar granule cells, while luzindole attenuates the action of Ramelteon (1 nM) in MT2 KO cerebellar granule cells. Ramelteon (100 μM) induces any pigment dispersion while melatonin completely disperses aggregated melanophores at 10 μM.

In vivo

Ramelteon (10 mg/kg, i/p) significantly reduces NREM sleep latency in rat and also produces a short-lasting increase in nonrapid eye movement (NREM) sleep duration, but the NREM power spectrum is unaltered. Ramelteon (0.1 mg/kg and 1 mg/kg, p.o.) accelerates reentrainment of running wheel activity rhythm to the new lightdark cycle in rats without affecting learning or memory. Ramelteon (0.03 mg/kg and 0.3 mg/kg, p.o.) significantly shortens latency to sleep onset and significantly increases total duration of sleep in freely moving monkeys without affecting the general behavior of the monkeys.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

동의어

TAK-375 | (S)-N-[2-(1,6,7,8-Tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide

사양 및 순도

Moligand™, 10mM in DMSO

생화학 및 생리적 메커니즘

Ramelteon (TAK-375) is a novel melatonin receptor agonist for human MT1 and MT2 receptors and chick forebrain melatonin receptors with K_i of 14 pM, 112 pM and 23.1 pM, respectively.

보관 조건

Store at -80°C

배송

Dry ice packs + Cold packs

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등급

Moligand™

작업 유형

AGONIST

작동 메커니즘

Melatonin receptor agonist

제품 특성

• ALogP: 2.7

이름과 식별자

• 이성체 SMILES: CCC(=O)NCC[C@@H]1CCC2=C1C3=C(C=C2)OCC3
• WGK 독일: 2
• PubChem CID: 208902
• 분자량: 259.34

관련 대상(인간)

MTNR1A Tclin Melatonin receptor type 1A (3 Activities)

Discover Target: MTNR1A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MTNR1B Tclin Melatonin receptor type 1B (3 Activities)

Discover Target: MTNR1B

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

화학 및 물리적 특성

• 특정 회전[α]: -57° (C=1,CHCl3)
• 발화점(°F): 35.6 °F
• 발화점(°C): 35.6°F
• 녹는점(°C): 116 °C

참고 문헌

1. Wang Guijie, Tian Fang, Li Yu, Liu Yang, Liu Chunfeng.  (2021)  Ramelteon Mitigates Free Fatty Acid (FFA)–Induced Attachment of Monocytes to Brain Vascular Endothelial Cells.  NEUROTOXICITY RESEARCH,  39  (6): (1937-1945).  [PMID:34792763] [10.1007/s12640-021-00422-1]