1. GPCR/G Protein
    Neuronal Signaling
  2. mGluR
  3. Dipraglurant

Dipraglurant (Synonyms: ADX48621)

Cat. No.: HY-14859 Purity: 99.99%
Handling Instructions

Dipraglurant (ADX48621) is a potent, selective, orally active and brain penetrant mGluR5 negative allosteric modulator (NAM), with an IC50 of 21 nM. Dipraglurant can reduce Levodopa-induced dyskinesia (LID) in vivo.

For research use only. We do not sell to patients.

Dipraglurant Chemical Structure

Dipraglurant Chemical Structure

CAS No. : 872363-17-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 490 In-stock
Estimated Time of Arrival: December 31
1 mg USD 168 In-stock
Estimated Time of Arrival: December 31
5 mg USD 383 In-stock
Estimated Time of Arrival: December 31
10 mg USD 528 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1980 In-stock
Estimated Time of Arrival: December 31
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Description

Dipraglurant (ADX48621) is a potent, selective, orally active and brain penetrant mGluR5 negative allosteric modulator (NAM), with an IC50 of 21 nM. Dipraglurant can reduce Levodopa-induced dyskinesia (LID) in vivo[1][2].

IC50 & Target[1]

mGluR5

21 nM (IC50)

In Vitro

Dipraglurant (1-10 μM; 15 min) counteracts the abnormal membrane responses and calcium rise induced either by the D2R agonist quinpirole or by caged dopamine (NPEC-Dopamine)[3].

In Vivo

Dipraglurant (3-30 mg/kg; a single p.o.) reduces L-dopa-induced chorea and dystonia and does not interfere with the efficacy of L-dopa in treating parkinsonian disability macaque[1].
Dipraglurant exhibits Cmax (1.040, 1.380, 5.310 ng/mL) Tmax (1.0, 0.5, 1.0 h) and AUCinf (2.230, 2.860, 15.700) following p.o. administration (3, 10, 30 mg/kg) in macaque[1].

Clinical Trial
Molecular Weight

265.29

Formula

C₁₆H₁₂FN₃

CAS No.

872363-17-2

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 40 mg/mL (150.78 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7695 mL 18.8473 mL 37.6946 mL
5 mM 0.7539 mL 3.7695 mL 7.5389 mL
10 mM 0.3769 mL 1.8847 mL 3.7695 mL
*Please refer to the solubility information to select the appropriate solvent.
References

Purity: 99.99%

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Keywords:

DipraglurantADX48621ADX 48621ADX-48621mGluRMetabotropic glutamate receptorsmGluR5LevodopainduceddyskinesiaLIDInhibitorinhibitorinhibit

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Dipraglurant
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