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

Dipraglurant  (Synonyms: ADX48621)

Cat. No.: HY-14859 Purity: 99.90%
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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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Based on 1 publication(s) in Google Scholar

Dipraglurant Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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.

Dipraglurant Related Antibodies
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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

g

Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.90%

COA (248 KB) RP-HPLC (204 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.7695 mL 18.8473 mL 37.6946 mL 94.2365 mL
5 mM 0.7539 mL 3.7695 mL 7.5389 mL 18.8473 mL
10 mM 0.3769 mL 1.8847 mL 3.7695 mL 9.4236 mL
15 mM 0.2513 mL 1.2565 mL 2.5130 mL 6.2824 mL
20 mM 0.1885 mL 0.9424 mL 1.8847 mL 4.7118 mL
25 mM 0.1508 mL 0.7539 mL 1.5078 mL 3.7695 mL
30 mM 0.1256 mL 0.6282 mL 1.2565 mL 3.1412 mL
40 mM 0.0942 mL 0.4712 mL 0.9424 mL 2.3559 mL
50 mM 0.0754 mL 0.3769 mL 0.7539 mL 1.8847 mL
60 mM 0.0628 mL 0.3141 mL 0.6282 mL 1.5706 mL
80 mM 0.0471 mL 0.2356 mL 0.4712 mL 1.1780 mL
100 mM 0.0377 mL 0.1885 mL 0.3769 mL 0.9424 mL
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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.

Keywords:

Dipraglurant872363-17-2ADX48621ADX 48621ADX-48621mGluRMetabotropic glutamate receptorsmGluR5LevodopainduceddyskinesiaLIDInhibitorinhibitorinhibit

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