(-)-U-50488 hydrochloride ((-)-Trans-(1S,2S)-U-50488 hydrochloride) 是一种选择性 κ-阿片受体 (KOR) 激动剂 (Kd=2.2 nM) 选择性大于 μ 阿片受体 (MOR) (Kd=430 nM)。(-)-U-50488 hydrochloride 比 (+) trans-(1R,2R) U-50488或 (±) 外消旋混合物 U-50488对映体更有效。(-)-U-50488 hydrochloride 对受感染的单核细胞来源巨噬细胞 (MDM) 具有持续有效的抗 HIV 作用。
| 生物活性 |
(-)-U-50488 hydrochloride ((-)-Trans-(1S,2S)-U-50488 hydrochloride) is a selective kappa-opioid receptor (KOR) agonist (b>Kd=2.2 nM) over μ-opioid receptor (MOR) (b>Kd=430 nM). (-)-U-50488 hydrochloride is a more active enantiomer than (+) trans-(1R,2R) U-50488 or the (±) trans-racemic mixture U-50488 . (-)-U-50488 hydrochloride has a potent and sustained anti-HIV effect in fected blood monocyte-derived macrophages (MDM). |
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| 体外研究 |
(-)-U-50488 hydrochloride (1 pM-100 nM; 7 days) exhibits a concentration-dependent inhibition of HIV-1 expression, the maximal inhibition at 10−13 M (approximately 73% suppression) in acutely infected blood monocyte-derived macrophages (MDM). |
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| 体内研究 |
(-)-U-50488 hydrochloride (intraperitoneal injection ; 5mg/kg; 2 hrs before 4% paraformaldehyde (PFA)) acutely induced pMeCP2-S421 (phosphorylation of the methyl-DNA binding protein MeCP2 at Ser421) and Fos selectively in the nucleus accumbens (NAc) but does not alter MeCP2 levels in any brain region.
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| 分子式 |
C19H26N2OCl2.HCl
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| 分子量 |
405.79
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| CAS号 |
114528-79-9
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| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis. |
客服小K 
客服小K
Data Sheet
