产品
编 号：F045284
分子式：C19H27Cl3N2O
分子量：405.79
分子式：C19H27Cl3N2O
分子量：405.79
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
结构图
CAS No: 114528-79-9
产品详情
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).
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.Animal Model:C57BL/6J mice
Dosage:5 mg/kg
Administration:Intraperitoneal?injection; single dose; 2 hrs before 4% PFA
Result:Induced pMeCP2-S421 in the brain acutely.
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).(-)-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.
(-)-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).
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.Animal Model:C57BL/6J mice
Dosage:5 mg/kg
Administration:Intraperitoneal?injection; single dose; 2 hrs before 4% PFA
Result:Induced pMeCP2-S421 in the brain acutely.
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).(-)-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.
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