Dipraglurant phosphate

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MedKoo CAT#: 125980

CAS#: 1687740-45-9 (phosphate)

Description: 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

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Dipraglurant phosphate
CAS# 1687740-45-9 (phosphate)
Instruction

Theoretical Analysis

MedKoo Cat#: 125980
Name: Dipraglurant phosphate
CAS#: 1687740-45-9 (phosphate)
Chemical Formula: C16H15FN3O4P
Exact Mass: 363.08
Molecular Weight: 363.285
Elemental Analysis: C, 52.90; H, 4.16; F, 5.23; N, 11.57; O, 17.62; P, 8.53

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Related CAS #: 872363-17-2 (free base)   1687740-45-9 (phosphate)  

Synonym: Dipraglurant phosphate; ADX-48621; ADX48621; ADX 48621;

IUPAC/Chemical Name: 6-fluoro-2-(4-(pyridin-2-yl)but-3-yn-1-yl)imidazo[1,2-a]pyridine phosphate

InChi Key: ZNJYWIJANUVJSR-UHFFFAOYSA-N

InChi Code: InChI=1S/C16H12FN3.H3O4P/c17-13-8-9-16-19-15(12-20(16)11-13)7-2-1-5-14-6-3-4-10-18-14;1-5(2,3)4/h3-4,6,8-12H,2,7H2;(H3,1,2,3,4)

SMILES Code: OP(O)(O)=O.FC1=CN2C=C(CCC#CC3=NC=CC=C3)N=C2C=C1

Appearance: To be determined

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:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 363.29 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.

Recalculate based on batch purity %
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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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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.