(-)-U-50488 hydrochloride(Synonyms: (-)-Trans-(1S,2S)-U-50488 hydrochloride)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

(-)-U-50488 hydrochloride (Synonyms: (-)-Trans-(1S,2S)-U-50488 hydrochloride)

(-)-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 (HY-15997A) 或 (±) 外消旋混合物 U-50488 (HY-15997B) 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。

(-)-U-50488 hydrochloride(Synonyms: (-)-Trans-(1S,2S)-U-50488 hydrochloride)

(-)-U-50488 hydrochloride Chemical Structure

CAS No. : 114528-79-9

规格 价格 是否有货
5 mg ￥1300 询问价格 & 货期

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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 (HY-15997A) or the (±) trans-racemic mixture U-50488 (HY-15997B). (-)-U-50488 hydrochloride has a potent and sustained anti-HIV effect in fected blood monocyte-derived macrophages (MDM)[1].

IC50 & Target

Kd: 2.2 nM (kappa-opioid receptor (KOR))
Kd: 430 nM (μ-opioid receptor (MOR))[1]
体外研究
(In Vitro)

(-)-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)[2].
(-)-U-50488 hydrochloride (10–13 M; 7-14 days) (10−13 M) markedly inhibits HIV-1 expression both at 7 and 14 days after infection, it has a sustained inhibitory effect on HIV-1 infection in MDM[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

(-)-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[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J mice[1]
Dosage: 5 mg/kg
Administration: Intraperitoneal injection; single dose; 2 hrs before 4% PFA
Result: Induced pMeCP2-S421 in the brain acutely.

分子量

405.79

Formula

C19H27Cl3N2O
CAS 号

114528-79-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Kirti Kumari Sharma, et al. The search for the “next” euphoric non-fentanil novel synthetic opioids on the illicit drugs market: current status and horizon scanning. Forensic Toxicol. 2019;37(1):1-16.

    [2]. Anthony S Zannas, ET AL. Regulation and function of MeCP2 Ser421 phosphorylation in U50488-induced conditioned place aversion in mice. Psychopharmacology (Berl). 2017 Mar;234(6):913-923.

    [3]. C C Chao,et al. U50488 inhibits HIV-1 expression in acutely infected monocyte-derived macrophages. Drug Alcohol Depend. 2001 Apr 1;62(2):149-54.

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