[CAS NO. 1438416-21-7]  MJN110

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PRODUCTS SPECIFICATIONS [1438416-21-7]

Catalog
AS940628
Brand
Arctom Scientific
CAS
1438416-21-7

DESCRIPTION [1438416-21-7]

Overview

MDLMFCD26960823
Molecular Weight462.33
Molecular FormulaC22H21Cl2N3O4
SMILESO=C(N1CCN(C(C2=CC=C(Cl)C=C2)C3=CC=C(Cl)C=C3)CC1)ON4C(CCC4=O)=O

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


Summary

MJN110 is an orally active and selective monoacylglycerol lipase (MAGL) inhibitor with IC 50 s of 9.1 nM and 2.1 nM for hMAGL and 2-arachidonoylglycerol (2-AG), respectively [1] . MJN110 produces opioid-sparing effects and displays strong antihyperalgesic activity [2] .


IC50 & Target

IC50: 9.1 nM (hMAGL) and 2.1 nM (2-AG) [1]


In Vitro

MJN110 (0.01-1000 nM; 4 hours) has the primary serine hydrolase target, hMAGL, with an IC 50 of ~1 nM and 10- and 100-fold selectivity windows over ABHD6 and LYPLA1/2, respectively [2] .

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

Western Blot Analysis [2]

Cell Line: Human-derived PC3 cells
Concentration: 0.01, 0.1, 1, 10, 100, 1000 nM
Incubation Time: 4 hours
Result: HMAGL acted as the primary serine hydrolase target with an IC 50 of ~1 nM.

In Vivo

MJN110 (i.p.; 0.0818 mg/kg; twice daily for 5.5 days) reverses chronic constriction injury (CCI)-induced mechanical allodynia and thermal hyperalgesia in a dose-dependent manner. The respective ED 50 value (95% confidence limits) is 0.430 (0.233-0.793) mg/kg [1] .

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

Animal Model: Male C57BL/6J mice ranged from 18 to 35 g [1]
Dosage: 0.0818 mg/kg
Administration: I.p.; twice daily for 5.5 days
Result: Reversed CCI-induced mechanical allodynia and thermal hyperalgesia in a dose-dependent manner.

Appearance

Solid


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 : 250 mg/mL ( 540.74 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1630 mL 10.8148 mL 21.6296 mL
5 mM 0.4326 mL 2.1630 mL 4.3259 mL
10 mM 0.2163 mL 1.0815 mL 2.1630 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: ≥ 2.08 mg/mL (4.50 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (4.50 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (4.50 mM); Clear solution

* All of the co-solvents are available by MCE.


Synonyms

1-Piperazinecarboxylic acid, 4-[bis(4-chlorophenyl)methyl]-, 2,5-dioxo-1-pyrrolidinyl ester
2,5-Dioxopyrrolidin-1-yl 4-[bis(4-chlorophenyl)methyl]piperazine-1-carboxylate
MJN 110