ML382 is a potent and selective MrgX1 (Mas-related G protein-coupled receptor X1, MRGPRX1) positive allosteric modulator with EC50 of 190 nM. ML382 dose-dependently increases the potency of BAM8–22. In vivo, ML382 (5 μM) significantly increases inhibition of ICa by a low concentration of BAM8–22 (0.5 μM) in DRG neurons from MrgprX1 mice. ML382 enhances the inhibition of spinal synaptic transmission by BAM8-22 in MrgprX1 mice. ML382 (25 μM, 125 μM, and 250 μM; 5 μL; i.th.;) dose-dependently attenuates heat hypersensitivity in MrgprX1 mice. ML382 (lumbar puncture injection; 25 μM, 5 μL) leads to a significant increase in postconditioning time spent in the ML382-paired chamber, compared with the preconditioning value. ML382 inhibits nerve injury-induced ongoing pain in MrgprX1 mice.
|Solubility (25°C)||DMSO ≥ 90 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
 Zhe Li, et al. Proc Natl Acad Sci U S A . Targeting human Mas-related G protein-coupled receptor X1 to inhibit persistent pain
 Wandong Wen, et al. ChemMedChem . Discovery and characterization of 2-(cyclopropanesulfonamido)-N-(2-ethoxyphenyl)benzamide, ML382: a potent and selective positive allosteric modulator of MrgX1
AS1411 is a quadruplex-forming oligonucleotide aptamer that targets nucleolin. AS1411 has anti-tumor activity.
MOMIPP, a macropinocytosis inducer, is a PIKfyve inhibitor. MOMIPP penetrates the blood-brain barrier (BBB).
MOPIPP is a novel indolebased chalcone, and vacuolin-1, is a non-lethal vacuoleinducing 2-propyl analog of MOMIPP. MOPIPP induces cellular vacuolization and increases autophagosomes numbers. MOPIPP also triggers methuosis, and interrupts glucose uptake and glycolytic metabolism. MOPIPP can cross the blood-brain barrier and shows efficacy in suppressing tumor progression agaisnt glioblastoma cells.
|Methuosis inducer 1
Methuosis inducer 1 is a potent methuosis inducer. Methuosis inducer 1 has anticancer activity.
|Dextran (Mw 150000)
Dextran is a multipurpose branched glucan, which can improve plasma colloid osmotic pressure, increase blood volume, reduce platelet adhesion, inhibit red blood cell aggregation, reduce blood viscosity, reduce peripheral circulation resistance, and unclog microcirculation.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.