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

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).

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RHC 80267 Chemical Structure

RHC 80267 Chemical Structure

CAS No. : 83654-05-1

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5 mg USD 56 In-stock
10 mg USD 90 In-stock
25 mg USD 180 In-stock
50 mg USD 300 In-stock
100 mg USD 510 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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]

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].

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

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].

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

Molecular Weight

394.51

Formula

C20H34N4O4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O/N=C1CCCCC\1)NCCCCCCNC(O/N=C2CCCCC/2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (63.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5348 mL 12.6739 mL 25.3479 mL 63.3697 mL
5 mM 0.5070 mL 2.5348 mL 5.0696 mL 12.6739 mL
10 mM 0.2535 mL 1.2674 mL 2.5348 mL 6.3370 mL
15 mM 0.1690 mL 0.8449 mL 1.6899 mL 4.2246 mL
20 mM 0.1267 mL 0.6337 mL 1.2674 mL 3.1685 mL
25 mM 0.1014 mL 0.5070 mL 1.0139 mL 2.5348 mL
30 mM 0.0845 mL 0.4225 mL 0.8449 mL 2.1123 mL
40 mM 0.0634 mL 0.3168 mL 0.6337 mL 1.5842 mL
50 mM 0.0507 mL 0.2535 mL 0.5070 mL 1.2674 mL
60 mM 0.0422 mL 0.2112 mL 0.4225 mL 1.0562 mL
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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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RHC 80267
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