WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H319676
CAS#: 872363-17-2 (free base)
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.
Hodoodo Cat#: H319676
Name: Dipraglurant
CAS#: 872363-17-2 (free base)
Chemical Formula: C16H12FN3
Exact Mass: 265.10
Molecular Weight: 265.291
Elemental Analysis: C, 72.44; H, 4.56; F, 7.16; N, 15.84
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:
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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 |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
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.
