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

RHC 80267 (Synonyms: U-57908)

Cat. No.: HY-107416 Purity: 99.51%
Handling Instructions

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).

For research use only. We do not sell to patients.

RHC 80267 Chemical Structure

RHC 80267 Chemical Structure

CAS No. : 83654-05-1

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25 mg USD 180 In-stock
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100 mg USD 510 In-stock
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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].

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].

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

Molecular Weight

394.51

Formula

C₂₀H₃₄N₄O₄

CAS No.

83654-05-1

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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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

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
10 mM 0.2535 mL 1.2674 mL 2.5348 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Keywords:

RHC 80267U-57908RHC80267RHC-80267U57908U 57908AcyltransferasemAChRCOXPhospholipaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseMuscarinic acetylcholine receptorCyclooxygenasePlateletdiacylglycerollipasecaninephospholipaseratpulmonaryarteriesacetylcholineelaxationInhibitorinhibitorinhibit

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RHC 80267
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