1. Metabolic Enzyme/Protease
    Neuronal Signaling
    GPCR/G Protein
    Immunology/Inflammation
  2. Acyltransferase
    mAChR
    COX
    Phospholipase
  3. RHC 80267

RHC 80267 (Synonyms: U-57908)

目录号: HY-107416 纯度: 99.51%
产品使用指南

RHC 80267 (U-57908) 是一种有效的选择性二酰基甘油脂酶 (DAGL) 抑制剂 (对犬血小板的 IC50 为 4 μM)。RHC 80267 抑制胆碱酯酶活性,IC50 为 4 μM,从而增强了乙酰胆碱引起的松弛。RHC 80267 还抑制 COX 活性和磷脂酰胆碱的水解。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

RHC 80267 Chemical Structure

RHC 80267 Chemical Structure

CAS No. : 83654-05-1

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mg ¥900 In-stock
25 mg ¥1800 In-stock
50 mg ¥3000 In-stock
100 mg ¥5100 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

注册 MCE会员完成审核
即刻享有 哈根达斯、星巴克、KFC、百果园 等专属礼券

Top Publications Citing Use of Products

查看 Acyltransferase 亚型特异性产品:

查看 COX 亚型特异性产品:

查看 Phospholipase 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL) (with IC50 of 4 μM in canine platelets). RHC-80267 inhibits cholinesterase activity with an IC50 of 4 μM, thereby enhancing the relaxation evoked by acetylcholine. RHC 80267 also inhibits COX and the hydrolysis of phosphatidylcholine (PC)[1][2][3][4].

IC50 & Target

IC50: 4 μM (Canine diacylglycerol lipase), 4 μM (Cholinesterase);
COX;
Phosphatidylcholine[1][3][4]

体外研究
(In Vitro)

The potentiation by RHC 80267 of the relaxation to acetylcholine could be caused by the inhibition of cholinesterase: (1) RHC 80267 does not affect the responses to carbachol, the carbamyl derivative of acetylcholine which only differs from acetylcholine by its resistance to hydrolysis by cholinesterase, and (2) the effect of RHC 80267 is mimicked by the inhibitor of cholinesterase neostigmine, RHC 80267 showing no additional effect in the presence of a maximally effective concentration of neostigmine. The determination of the effect of RHC 80267 on the cholinesterase activity of brain homogenate confirmed that RHC 80267 inhibits this enzyme in the same range of concentrations increasing the relaxation to acetylcholine, namely at 1-10 μM[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

RHC 80267 (40 μM) enhances contractions induced by U46619 (a thromboxane A2 analog) in human and rat pulmonary arteries (hPAs and rPAs, respectively) and by angiotensin II (ANG II) in rPAs in an endothelium-dependent manner[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

394.51

Formula

C₂₀H₃₄N₄O₄

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (63.37 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5348 mL 12.6740 mL 25.3479 mL
5 mM 0.5070 mL 2.5348 mL 5.0696 mL
10 mM 0.2535 mL 1.2674 mL 2.5348 mL
*

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。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.34 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.34 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.34 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.34 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.34 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.34 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称:

 

* 需求量:

* 客户姓名:

 

* Email:

* 电话:

 

* 公司或机构名称:

   留言给我们:

Bulk Inquiry

Inquiry Information

产品名称:
RHC 80267
目录号:
HY-107416
需求量: