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

Dipraglurant  (Synonyms: ADX48621)

Cat. No.: HY-14859 Purity: 99.90%
COA 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. Dipraglurant is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 350 In-stock
Solution
10 mM * 1 mL in DMSO USD 350 In-stock
Solid
1 mg USD 120 In-stock
5 mg USD 290 In-stock
10 mg USD 420 In-stock
50 mg USD 1500 In-stock
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200 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

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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]. Dipraglurant is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

265.29

Formula

C16H12FN3

CAS No.
Appearance

Solid

Color

White to off-white

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 2 years
-20°C 1 year
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.
Purity & Documentation

Purity: 99.90%

References
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Dipraglurant Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Dipraglurant
Cat. No.:
HY-14859
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