化合物IPSU T5503
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Product IntroductionBioactivity英文名: IPSU描述: IPSU 是可口服和脑渗透性的选择性OX2R 拮抗剂，pKi 值为7.85。体外活性: BBAC or the selective OX2R antago
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Product Introduction
Bioactivity
英文名: IPSU
描述: IPSU 是可口服和脑渗透性的选择性OX2R 拮抗剂，pKi 值为7.85。
体外活性: BBAC or the selective OX2R antagonist IPSU bind rapidly and reach equilibrium very quickly in binding and/or functional assays[1].
体内活性: IPSU?exhibits an acceptable absolute oral bioavailability and a brain/blood concentration ratio that indicated favorable brain penetration.?IPSU increases sleep when dosed during the mouse active phase (lights off);?IPSU induces sleep primarily by increasing NREM sleep.?IPSU shows a fast onset of action, with a clear increase in total sleep time during the first hour afterdosing.?The effect lasts 4-5 h, after which time the total sleep time per hour is the same as on vehicle day[2]
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 30 mg/mL (73.98 mM)
关键字: inhibit | IPSU | HCRT Receptor | Hypocretin Receptor | Orexin Receptor (OX Receptor) | Inhibitor
相关产品: DORA-22 | Orexin B, rat, mouse Acetate | SB-334867 free base | Almorexant | Daridorexant hydrochloride | MK-1064 | SB-649868 | [Ala11,D-Leu15]-Orexin B acetate | MK-3697 | ACT-462206
相关库: Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Neuronal Signaling Compound Library | Inhibitor Library | GPCR Compound Library | Orally Active Compound Library | NO PAINS Compound Library | Bioactive Compound Library
Bioactivity
英文名: IPSU
描述: IPSU 是可口服和脑渗透性的选择性OX2R 拮抗剂，pKi 值为7.85。
体外活性: BBAC or the selective OX2R antagonist IPSU bind rapidly and reach equilibrium very quickly in binding and/or functional assays[1].
体内活性: IPSU?exhibits an acceptable absolute oral bioavailability and a brain/blood concentration ratio that indicated favorable brain penetration.?IPSU increases sleep when dosed during the mouse active phase (lights off);?IPSU induces sleep primarily by increasing NREM sleep.?IPSU shows a fast onset of action, with a clear increase in total sleep time during the first hour afterdosing.?The effect lasts 4-5 h, after which time the total sleep time per hour is the same as on vehicle day[2]
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 30 mg/mL (73.98 mM)
关键字: inhibit | IPSU | HCRT Receptor | Hypocretin Receptor | Orexin Receptor (OX Receptor) | Inhibitor
相关产品: DORA-22 | Orexin B, rat, mouse Acetate | SB-334867 free base | Almorexant | Daridorexant hydrochloride | MK-1064 | SB-649868 | [Ala11,D-Leu15]-Orexin B acetate | MK-3697 | ACT-462206
相关库: Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Neuronal Signaling Compound Library | Inhibitor Library | GPCR Compound Library | Orally Active Compound Library | NO PAINS Compound Library | Bioactive Compound Library
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