1. GPCR/G Protein Neuronal Signaling
  2. Opioid Receptor
  3. (-)-U-50488 hydrochloride

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

目录号: HY-15997 纯度: ≥98.0%
COA 产品使用指南

(-)-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。

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(-)-U-50488 hydrochloride Chemical Structure

(-)-U-50488 hydrochloride Chemical Structure

CAS No. : 114528-79-9

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规格 价格 是否有货 数量
1 mg ¥1863
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5 mg ¥4100
In-stock
10 mg ¥7000
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Customer Review

Other Forms of (-)-U-50488 hydrochloride:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

MCE 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].

MCE 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
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro: 

H2O 中的溶解度 : 50 mg/mL (123.22 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4643 mL 12.3216 mL 24.6433 mL
5 mM 0.4929 mL 2.4643 mL 4.9287 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: ≥98.0%

参考文献

(-)-U-50488 hydrochloride 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 2.4643 mL 12.3216 mL 24.6433 mL 61.6082 mL
5 mM 0.4929 mL 2.4643 mL 4.9287 mL 12.3216 mL
10 mM 0.2464 mL 1.2322 mL 2.4643 mL 6.1608 mL
15 mM 0.1643 mL 0.8214 mL 1.6429 mL 4.1072 mL
20 mM 0.1232 mL 0.6161 mL 1.2322 mL 3.0804 mL
25 mM 0.0986 mL 0.4929 mL 0.9857 mL 2.4643 mL
30 mM 0.0821 mL 0.4107 mL 0.8214 mL 2.0536 mL
40 mM 0.0616 mL 0.3080 mL 0.6161 mL 1.5402 mL
50 mM 0.0493 mL 0.2464 mL 0.4929 mL 1.2322 mL
60 mM 0.0411 mL 0.2054 mL 0.4107 mL 1.0268 mL
80 mM 0.0308 mL 0.1540 mL 0.3080 mL 0.7701 mL
100 mM 0.0246 mL 0.1232 mL 0.2464 mL 0.6161 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
(-)-U-50488 hydrochloride
目录号:
HY-15997
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