[CAS NO. 713121-80-3] ML-193
PRODUCTS SPECIFICATIONS [713121-80-3]
DESCRIPTION [713121-80-3]
Overview
| MDL | MFCD05999971 |
|---|---|
| Molecular Weight | 527.59 |
| Molecular Formula | C28H25N5O4S |
| SMILES | CC(C(C)=NO1)=C1NS(C(C=C2)=CC=C2NC(C3=CC(C4=CC=CC=N4)=NC5=C3C=C(C)C=C5C)=O)(=O)=O |
Summary
IC50 & Target
IC50: 221 nM (GPR55) [1]
In Vitro
ML-193 (0.01-100 μM; pretreated for 15 min) inhibits β-arrestin trafficking induced by L-α-lysophophosphatidylinositol (LPI, 10 μM) and ML186 (1 μM) with IC
50
s of 0.22 μM and 0.12 μM, respectively
[2]
.
ML-193 (0.01-10 μM; pretreated for 30 min) decreases the LPI-mediated ERK1/2 phosphorylation, with an IC
50
of 0.2 μM in U2OS cells
[2]
.
ML-193 (5 μM; pretreated for 30 min) attenuates the GPR55 agonists induced increases in hNSCs proliferation rates
[4]
.
ML-193 (5 μM; 10 d) attenuates the ML184-induced increases in hNSCs differentiation
[4]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
ML193 (1 and 5 µg/rat; intra-striatal at a rate of 1 μL/min) attenuates sensorimotor deficits and slip steps, increases motor coordination in PD rats [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male Wistar rats (200-250 g) were induced experimental Parkinson by 6-hydroxydopamine (6-OHDA, 10 µg/rat) [3] |
| Dosage: | 1 and 5 µg/rat |
| Administration: | Injected into the right striatum at a rate of 1 μL/min |
| Result: | Increased the time on the rotarod, decreased latency to remove the label and slip steps in 6-OHDA-lesioned rats. |
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 |
References
- [1] Heynen-Genel S, et, al. Screening for Selective Ligands for GPR55-Antagonists. Probe Reports from the NIH Molecular Libraries Program. 2010 Oct 30.
- [2] Kotsikorou E, et, al. Identification of the GPR55 antagonist binding site using a novel set of high-potency GPR55 selective ligands. Biochemistry. 2013 Dec 31;52(52):9456-69.
- [3] Fatemi I, et, al. The effect of intra-striatal administration of GPR55 agonist (LPI) and antagonist (ML193) on sensorimotor and motor functions in a Parkinson's disease rat model. Acta Neuropsychiatr. 2021 Feb;33(1):15-21.
- [4] Hill JD, et, al. Activation of GPR55 increases neural stem cell proliferation and promotes early adult hippocampal neurogenesis. Br J Pharmacol. 2018 Aug;175(16):3407-3421.