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CAS No. : 1361321-96-1
MCE 国际站:ACT-462206
产品活性:ACT-462206 是一种口服有效的双 Orexin 1/Orexin 2 受体拮抗剂,IC50 分别为 60 nM (Orexin 1) 和 11 nM (Orexin 2)。ACT-462206 能穿过血脑屏障,可用于失眠、压力/焦虑相关障碍和成瘾研究。
研究领域:GPCR/G Protein | Neuronal Signaling
作用靶点:Orexin Receptor (OX Receptor)
In Vitro: Orexins are released in a Ca2+-sensitive manner at axonal terminals and can then bind to two closely related G-protein-coupled receptors (GPCRs): orexin receptor type 1 (OX1) and orexin receptor type 2 (OX2).
ACT-462206 shows binding affinity with Kbs of 17 nM (hOX1), 2.4 nM (hOX2), 28 nM (rOX1), 9.9 nM (rOX2), 27 nM (dOX1), 4.2 nM (dOX2), respectively.
ACT-462206 inhibits Orexin activity with IC50s of 60 nM (hOX1), 11 nM (hOX2), 48 nM (rOX1), 9.6 nM (rOX2), 68 nM (dOX1), 26 nM (dOX2), respectively.
ACT-462206 inhibits CYP450 3A4T and 3A4M with IC50s of 15 μM and 29 μM, respectively.
In Vivo: ACT-462206 (compound 24) (100 mg/kg; p.o.; sampling at 3 h) can go cross blood brain barrier, with concentrations are 2267 ng/mL and 1219 ng/g in plasma and brain, respectively in male Wistar rats.
ACT-462206 (10-300 mg/kg; p.o.; single dose) shows sleep-promoting effects in male Wistar rats and in male Beagle dogs, with decreasing wakefulness and increasing non-rapid eye movement (non-REM) and REM sleep.
ACT-462206 (100, 300 mg/kg; p.o.; single dose) exerts anxiolytic-like effects, decreases the fear-potentiated startle reflexes in response to a sudden loud noise in rats, reduces the socialstress-induced increases of locomotion, body temperature, and heart rate.
Pharmacokinetics in different species
| Route | Dose (mg/kg) | AUC (ng•h/mL) | CL (mL/min/kg) | Vss (L/kg) | t1/2 (h) | cmax (ng/mL) | tmax (h) | F1/2 (%) |
rat | i.v. | 1 | 586 | 29 | 1.8 | 1.9 | / | / | / |
| p.o. | 10 | 2310 | / | / | / | 1600 | 0.5 | 39 |
dog | i.v. | 1 | 1490 | 11 | 1.4 | 1.7 | / | / | / |
| p.o. | 3 | 2750 | / | / | / | 426 | 0.5 | 52 |
相关产品:Clinical Compound Library Plus | Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Neuronal Signaling Compound Library | Clinical Compound Library | CNS-Penetrant Compound Library | Orally Active Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | Suntinorexton | MK-3697 | TCS-OX2-29 | IPSU | Vornorexant | Orexin B, human | Cudarolimab | Orexin receptor antagonist 4 | Orexin receptor antagonist 2 | Orexin receptor antagonist 3 | SB-408124 Hydrochloride | Fazamorexant | Almorexant-13C,d3 | SB-334867 free base | MK-1064 | Orexin B, rat, mouse | [Ala11,D-Leu15]-Orexin B(human) | JNJ-10397049 | Orexin 2 Receptor Agonist | Orexin A (human, rat, mouse) (acetate) | Almorexant | SB-674042 | GSK1059865 | OXA(17-33) TFA | Filorexant | Nivasorexant | Danavorexton
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货号: HY-101834
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