DipraglurantCAS# 872363-17-2 |
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Quality Control & MSDS
3D structure
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| Cas No. | 872363-17-2 | SDF | Download SDF |
| PubChem ID | 44557636 | Appearance | Powder |
| Formula | C16H12FN3 | M.Wt | 265.29 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | ADX48621 | ||
| Solubility | DMSO : ≥ 40 mg/mL (150.78 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 6-fluoro-2-(4-pyridin-2-ylbut-3-ynyl)imidazo[1,2-a]pyridine | ||
| SMILES | C1=CC=NC(=C1)C#CCCC2=CN3C=C(C=CC3=N2)F | ||
| Standard InChIKey | LZXMUJCJAWVHPZ-UHFFFAOYSA-N | ||
| Standard InChI | 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 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Dipraglurant (ADX 48621) is a mGluR5 antagonists with IC50 of 0.021 μM.
IC50 Value: 0.021 μM [1]
Target: mGluR
Dipraglurant (ADX-48621) from Addex Therapeutics showed in vivo activity in different anxiety models in rat50 and is currently in phase II for the treatment of dyskinesia in Parkinson's disease. References: | |||||
Dipraglurant Dilution Calculator
Dipraglurant Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.7695 mL | 18.8473 mL | 37.6946 mL | 75.3892 mL | 94.2365 mL |
| 5 mM | 0.7539 mL | 3.7695 mL | 7.5389 mL | 15.0778 mL | 18.8473 mL |
| 10 mM | 0.3769 mL | 1.8847 mL | 3.7695 mL | 7.5389 mL | 9.4236 mL |
| 50 mM | 0.0754 mL | 0.3769 mL | 0.7539 mL | 1.5078 mL | 1.8847 mL |
| 100 mM | 0.0377 mL | 0.1885 mL | 0.3769 mL | 0.7539 mL | 0.9424 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Dipraglurant (ADX 48621) is mGlu5 receptor negative allosteric modulator.
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A Phase 2A Trial of the Novel mGluR5-Negative Allosteric Modulator Dipraglurant for Levodopa-Induced Dyskinesia in Parkinson's Disease.[Pubmed:27214664]
Mov Disord. 2016 Sep;31(9):1373-80.
BACKGROUND: The metabotropic glutamate receptor 5-negative allosteric modulator Dipraglurant reduces levodopa-induced dyskinesia in the MPTP-macaque model. The objective of this study was to assess the safety, tolerability (primary objective), and efficacy (secondary objective) of Dipraglurant on levodopa-induced dyskinesia in Parkinson's disease (PD). METHODS: The study was a phase 2A double-blind, placebo-controlled, randomized (2:1), 4-week, parallel-group, multicenter dose-escalation (from 50 mg once daily to 100 mg 3 times daily) clinical trial involving 76 PD subjects with moderate to severe levodopa-induced dyskinesia. Safety and tolerability were assessed based on clinical and biological examination and adverse events recording. Secondary efficacy outcome measures included the modified Abnormal Involuntary Movement Scale, UPDRS, and diaries. Pharmacokinetics were measured at 3 visits following a single dose. RESULTS: Fifty-two patients were exposed to Dipraglurant and 24 to placebo. There were no major safety concerns. Two subjects did not complete the study because of adverse events. Most frequent adverse events included dyskinesia, dizziness, nausea, and fatigue. Dipraglurant significantly reduced peak dose dyskinesia (modified Abnormal Involuntary Movement Scale) on day 1 (50 mg, 20%; P = 0.04) and on day 14 (100 mg, 32%; P =0 .04) and across a 3-hour postdose period on day 14 (P = 0.04). There was no evidence of worsening of parkinsonism. Dipraglurant was rapidly absorbed (tmax = 1 hour). The 100-mg dose led to a mean Cmax of 1844 ng/mL on day 28. CONCLUSIONS: Dipraglurant proved to be safe and well tolerated in its first administration to PD patients. Its efficacy in reversing levodopa-induced dyskinesia warrants further investigations in a larger number of patients. (c) 2016 International Parkinson and Movement Disorder Society.
The mGluR5 negative allosteric modulator dipraglurant reduces dyskinesia in the MPTP macaque model.[Pubmed:24865335]
Mov Disord. 2014 Jul;29(8):1074-9.
BACKGROUND: Blocking metabotropic glutamate receptor type 5 (mGluR5) has been proposed as a target for levodopa-induced dyskinesias (LID) in Parkinson's disease (PD). We assessed the effect on LID of Dipraglurant, a potent selective mGluR5 receptor negative allosteric modulator in the gold-standard LID macaque model. METHODS: Dipraglurant (3, 10, and 30 mg/kg, by mouth) was tested in the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) macaque model of LID in a four-way crossover, single-dose, controlled study (n = 8). RESULTS: Dipraglurant inhibited dyskinesias in the LID macaque model, with best effect reached at 30 mg/kg dose with no alteration of levodopa efficacy. CONCLUSION: Acute challenges of Dipraglurant were efficacious on choreic and dystonic LID in the MPTP-macaque model. Dipraglurant pharmacokinetic variables were similar to those of levodopa, suggesting that both drugs can be co-administered simultaneously in further studies.
