Foliglurax HCl | CAS# 2133294-96-7 (HCl) | glutamate receptor positive modulator

MedKoo Cat#: 414651 | Name: Foliglurax HCl

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Foliglurax HCl is a glutamate receptor positive modulator. The metabotropic glutamate receptor 4 (mGluR4) is an emerging target for the treatment of Parkinson’s disease (PD).

Chemical Structure

Foliglurax HCl

CAS#2133294-96-7 (HCl)

Theoretical Analysis

MedKoo Cat#: 414651

Name: Foliglurax HCl

CAS#: 2133294-96-7 (HCl)

Chemical Formula: C23H24ClN3O3S

Exact Mass: 457.1227

Molecular Weight: 457.97

Elemental Analysis: C, 60.32; H, 5.28; Cl, 7.74; N, 9.18; O, 10.48; S, 7.00

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 750.00	2 Weeks
10mg	USD 1,250.00	2 Weeks

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Related CAS #

Foliglurax 2HCl 1883329-51-8 (free base) 2133294-96-7 (HCl)

Synonym

Foliglurax monohydrochloride; Foliglurax hydrochloride; Foliglurax HCl; Foliglurax (monohydrochloride)

IUPAC/Chemical Name

(E)-6-(3-morpholinopropyl)-2-(thieno[3,2-c]pyridin-6-yl)-4H-chromen-4-one oxime hydrochloride

InChi Key

LOBGNYCFXPNFJB-LUINMZRLSA-N

InChi Code

InChI=1S/C23H23N3O3S.ClH/c27-25-19-13-22(20-14-23-17(15-24-20)5-11-30-23)29-21-4-3-16(12-18(19)21)2-1-6-26-7-9-28-10-8-26;/h3-5,11-15,27H,1-2,6-10H2;1H/b25-19+;

SMILES Code

O/N=C1C=C(C2=CC3=C(C=CS3)C=N2)OC4=C\1C=C(CCCN5CCOCC5)C=C4.[H]Cl

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

To be determined

Shelf Life

>2 years if stored properly

Drug Formulation

To be determined

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 457.97 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Bourque M, Morissette M, Conquet F, Charvin D, Di Paolo T. Foliglurax, a positive allosteric modulator of the metabotrophic glutamate receptor 4, protects dopaminergic neurons in MPTP-lesioned male mice. Brain Res. 2023 Jun 15;1809:148349. doi: 10.1016/j.brainres.2023.148349. Epub 2023 Mar 25. PMID: 36972837. 2: Doller D, Bespalov A, Miller R, Pietraszek M, Kalinichev M. A case study of foliglurax, the first clinical mGluR4 PAM for symptomatic treatment of Parkinson's disease: translational gaps or a failing industry innovation model? Expert Opin Investig Drugs. 2020 Dec;29(12):1323-1338. doi: 10.1080/13543784.2020.1839047. Epub 2020 Nov 11. PMID: 33074728. 3: Rascol O, Medori R, Baayen C, Such P, Meulien D; AMBLED Study Group. A Randomized, Double-Blind, Controlled Phase II Study of Foliglurax in Parkinson's Disease. Mov Disord. 2022 May;37(5):1088-1093. doi: 10.1002/mds.28970. Epub 2022 Feb 26. PMID: 35218231; PMCID: PMC9303267. 4: Witkin JM, Pandey KP, Smith JL. Clinical investigations of compounds targeting metabotropic glutamate receptors. Pharmacol Biochem Behav. 2022 Sep;219:173446. doi: 10.1016/j.pbb.2022.173446. Epub 2022 Aug 17. PMID: 35987339. 5: Volpi C, Fallarino F, Mondanelli G, Macchiarulo A, Grohmann U. Opportunities and challenges in drug discovery targeting metabotropic glutamate receptor 4. Expert Opin Drug Discov. 2018 May;13(5):411-423. doi: 10.1080/17460441.2018.1443076. Epub 2018 Feb 28. PMID: 29486616. 6: Calabrese V, Picconi B, Heck N, Campanelli F, Natale G, Marino G, Sciaccaluga M, Ghiglieri V, Tozzi A, Anceaume E, Cuoc E, Caboche J, Conquet F, Calabresi P, Charvin D. A positive allosteric modulator of mGlu4 receptors restores striatal plasticity in an animal model of l-Dopa-induced dyskinesia. Neuropharmacology. 2022 Nov 1;218:109205. doi: 10.1016/j.neuropharm.2022.109205. Epub 2022 Aug 5. PMID: 35940348. 7: Charvin D, Di Paolo T, Bezard E, Gregoire L, Takano A, Duvey G, Pioli E, Halldin C, Medori R, Conquet F. An mGlu4-Positive Allosteric Modulator Alleviates Parkinsonism in Primates. Mov Disord. 2018 Oct;33(10):1619-1631. doi: 10.1002/mds.27462. Epub 2018 Sep 14. PMID: 30216534. 8: Charvin D, Pomel V, Ortiz M, Frauli M, Scheffler S, Steinberg E, Baron L, Deshons L, Rudigier R, Thiarc D, Morice C, Manteau B, Mayer S, Graham D, Giethlen B, Brugger N, Hédou G, Conquet F, Schann S. Discovery, Structure- Activity Relationship, and Antiparkinsonian Effect of a Potent and Brain- Penetrant Chemical Series of Positive Allosteric Modulators of Metabotropic Glutamate Receptor 4. J Med Chem. 2017 Oct 26;60(20):8515-8537. doi: 10.1021/acs.jmedchem.7b00991. Epub 2017 Oct 12. PMID: 28902994. 9: Takano A, Nag S, Jia Z, Jahan M, Forsberg A, Arakawa R, Grybäck P, Duvey G, Halldin C, Charvin D. Characterization of [11C]PXT012253 as a PET Radioligand for mGlu4 Allosteric Modulators in Nonhuman Primates. Mol Imaging Biol. 2019 Jun;21(3):500-508. doi: 10.1007/s11307-018-1257-0. PMID: 30066121.