[CAS NO. 2133294-96-7] Foliglurax monohydrochloride

Name: Foliglurax monohydrochloride
Brand: Arctom Scientific
SKU: AS948142

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PRODUCTS SPECIFICATIONS [2133294-96-7]

Distributor

Catalog

AS948142

Brand

Arctom Scientific

CAS

2133294-96-7

DESCRIPTION [2133294-96-7]

Overview

MDL	-
Molecular Weight	457.97
Molecular Formula	C23H24ClN3O3S
SMILES	O/N=C1C=C(C2=CC3=C(C=CS3)C=N2)OC4=CC=C(CCCN5CCOCC5)C=C\14.Cl

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

Summary

Foliglurax monohydrochloride (PXT002331 monohydrochloride) is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator ( mGluR4 PAM) , with an EC ₅₀ of 79 nM ^[1] . Antiparkinsonian effect ^[1] .

IC50 & Target

mGlu ₄

79 nM (EC ₅₀ )

In Vitro

Foliglurax, a highly selective and potent mGlu4 receptor PAM with a marked brain-penetrance feature, might revolutionize the field of mGlu4 receptor drug targeting in CNS disorders ^[2] .

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT03331848	Prexton Therapeutics	Parkinson Disease	January 15, 2018	Phase 2
NCT02639221	Prexton Therapeutics	Parkinson´s Disease	January 2016	Phase 1
NCT04322227	H. Lundbeck A+S	Parkinson Disease\|Healthy	January 23, 2020	Phase 1
NCT04175132	H. Lundbeck A+S	Healthy\|Parkinson Disease	November 12, 2019	Phase 1
NCT04002895	H. Lundbeck A+S	Healthy	June 27, 2019	Phase 1
NCT03162874	Prexton Therapeutics	Parkinson Disease	July 4, 2017	Phase 2
NCT04275115	H. Lundbeck A+S	Healthy	February 10, 2020	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H ₂ O : 25 mg/mL ( 54.59 mM ; Need ultrasonic)

DMSO : 5 mg/mL ( 10.92 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1835 mL	10.9177 mL	21.8355 mL
5 mM	0.4367 mL	2.1835 mL	4.3671 mL
10 mM	0.2184 mL	1.0918 mL	2.1835 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: ≥ 0.5 mg/mL (1.09 mM); Clear solution
2.

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

Solubility: ≥ 0.5 mg/mL (1.09 mM); Clear solution
3.

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

Solubility: ≥ 0.5 mg/mL (1.09 mM); Clear solution

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