Dipraglurant | ADX-48621 | CAS#872363-17-2 | mGlu5 receptor modulator

MedKoo Cat#: 319676 | Name: Dipraglurant

Description:

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

Dipraglurant, aslo known as ADX-48621, is a negative allosteric modulator of the mGlu5 receptor which is under development by Addex Therapeutics for the treatment of Parkinson's disease levodopa-induced dyskinesia (PD-LID). Blocking metabotropic glutamate receptor type 5 (mGluR5) has been proposed as a target for levodopa-induced dyskinesias (LID) in Parkinson's disease (PD). Acute challenges of dipraglurant were efficacious on choreic and dystonic LID in the MPTP-macaque model.

Chemical Structure

Dipraglurant

CAS#872363-17-2 (free base)

Theoretical Analysis

MedKoo Cat#: 319676

Name: Dipraglurant

CAS#: 872363-17-2 (free base)

Chemical Formula: C16H12FN3

Exact Mass: 265.1015

Molecular Weight: 265.29

Elemental Analysis: C, 72.44; H, 4.56; F, 7.16; N, 15.84

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

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Related CAS #

872363-17-2 (free base) 1687740-45-9 (phosphate)

Synonym

ADX-48621; ADX48621; ADX 48621; Dipraglurant

IUPAC/Chemical Name

6-Fluoro-2-[4-(2-pyridinyl)-3-butyn-1-yl]imidazo[1,2-a]pyridine

InChi Key

LZXMUJCJAWVHPZ-UHFFFAOYSA-N

InChi Code

InChI=1S/C16H12FN3/c17-13-8-9-16-19-15(12-20(16)11-13)7-2-1-5-14-6-3-4-10-18-14/h3-4,6,8-12H,2,7H2

SMILES Code

FC1=CN2C(C=C1)=NC(CCC#CC3=NC=CC=C3)=C2

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

Soluble in DMSO, not in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

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 265.29 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: Sciamanna G, Ponterio G, Tassone A, Maltese M, Madeo G, Martella G, Poli S, Schirinzi T, Bonsi P, Pisani A. Negative allosteric modulation of mGlu5 receptor rescues striatal D2 dopamine receptor dysfunction in rodent models of DYT1 dystonia. Neuropharmacology. 2014 Oct;85:440-50. doi: 10.1016/j.neuropharm.2014.06.013. Epub 2014 Jun 19. PubMed PMID: 24951854. 2: Rascol O, Fox S, Gasparini F, Kenney C, Di Paolo T, Gomez-Mancilla B. Use of metabotropic glutamate 5-receptor antagonists for treatment of levodopa-induced dyskinesias. Parkinsonism Relat Disord. 2014 Sep;20(9):947-56. doi: 10.1016/j.parkreldis.2014.05.003. Epub 2014 May 14. Review. PubMed PMID: 24951359. 3: Bezard E, Pioli EY, Li Q, Girard F, Mutel V, Keywood C, Tison F, Rascol O, Poli SM. The mGluR5 negative allosteric modulator dipraglurant reduces dyskinesia in the MPTP macaque model. Mov Disord. 2014 Jul;29(8):1074-9. doi: 10.1002/mds.25920. Epub 2014 May 27. PubMed PMID: 24865335.