ADX-47273

Name: ADX-47273
Brand: MedChemExpress
SKU: HY-13058
Rating: 4.5 (1 reviews)

Cat. No.: HY-13058 Purity: 99.94%: FAQs
Data Sheet SDS COA Handling Instructions

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ADX-47273 is a potent, selective and brain-penetrant mGluR5 positive allosteric modulator (PAM), with an EC₅₀ of 0.17 μM for potentiation of glutamate (50 nM) response. ADX-47273 has antipsychotic and procognitive activities.

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

ADX-47273 Chemical Structure

CAS No. : 851881-60-2

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 73	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 73	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 106	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 383	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 686	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of ADX-47273:

(R)-ADX-47273 In-stock

1 Publications Citing Use of MCE ADX-47273

•Biological Sciences. 2020 Sep.

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View All mGluR Isoform Specific Products:

View All Isoforms

mGluR1 mGluR2 mGluR3 mGluR4 mGluR5 mGluR6 mGluR7 mGluR8 mGluR

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

mGluR5

0.17 μM (EC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	157 nM Compound: 7, ADX-47273	Positive allosteric modulation of human mGluR5 stably expressed in HEK293 cells assessed as Ca2+ flux by FLIPR assay Positive allosteric modulation of human mGluR5 stably expressed in HEK293 cells assessed as Ca2+ flux by FLIPR assay	[PMID: 24050755]
HEK293	EC₅₀	199 nM Compound: 2, ADX47273	Positive allosteric modulation of human mGluR5a transfected in HEK293 cells by calcium mobilization assay Positive allosteric modulation of human mGluR5a transfected in HEK293 cells by calcium mobilization assay	[PMID: 23947773]
HEK293	EC₅₀	55 nM Compound: 7, ADX-47273	Positive allosteric modulation of rat mGluR5 stably expressed in HEK293 cells assessed as Ca2+ flux by FLIPR assay Positive allosteric modulation of rat mGluR5 stably expressed in HEK293 cells assessed as Ca2+ flux by FLIPR assay	[PMID: 24050755]

In Vitro

ADX-47273 (0.1 nM-10 μM; 5 min) causes a concentration-dependent increase in the response to 50 nM glutamate in HEK 293 cells expressing rat mGlu5 without eliciting a response by itself^[1].
ADX-47273 (0.1 nM-10 μM; 5 min) causes a concentration-dependent increase in the response to 300 nM glutamate in primary astrocyte cultures, with an EC₅₀ of 0.23 μM^[1].
ADX47273 (0.01-10 μM; 60 min) inhibits [³H]MPEP binding to rat mGlu5 receptor HEK cell membranes, with a K_i of 4.3 μM^[1].

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

In Vivo

ADX47273 (1-10 mg/kg; a single i.p.) dose-dependently increases ERK and CREB phosphorylation in rat hippocampus and prefrontal cortex^[1].
ADX47273 (10-100 mg/kg; a single i.p.) decreases conditioned avoidance responding in a dose-dependent manner in rats^[1].
ADX47273 (10-300 mg/kg; i.p.) blocks apomorphine-induced climbing in mice^[1].
ADX47273 (0.1-50 mg/kg; i.p.) increases novel object recognition and reduces impulsivity in the five-choice serial reaction time test in rats^[1].
ADX47273 (15 mg/kg; i.p.) enhances reversal learning in the Morris Water Maze (MWM) in mice^[3].

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

Animal Model:	Male Long-Evans rats^[1]
Dosage:	1, 10 mg/kg
Administration:	A single i.p.
Result:	Increased ERK and CREB phosphorylation in both the prefrontal cortex and hippocampus.

Molecular Weight

369.36

Formula

C₂₀H₁₇F₂N₃O₂

CAS No.

851881-60-2

Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C(F)C=C1)N2C[C@@H](C3=NC(C4=CC=C(F)C=C4)=NO3)CCC2

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:

Methanol : 105.5 mg/mL (285.63 mM; Need ultrasonic and warming)

DMSO : ≥ 31 mg/mL (83.93 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	2.7074 mL	13.5369 mL	27.0739 mL
5 mM	0.5415 mL	2.7074 mL	5.4148 mL
10 mM	0.2707 mL	1.3537 mL	2.7074 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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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

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(per animal)

μL

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: 99.94%

Select Batch:

Data Sheet (274 KB) SDS (480 KB)

COA (245 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Liu F, et al. ADX47273 [S-(4-fluoro-phenyl)-{3-[3-(4-fluoro-phenyl)-[1,2,4]-oxadiazol-5-yl]-piperidin-1-yl}-methanone]: a novel metabotropic glutamate receptor 5-selective positive allosteric modulator with preclinical antipsychotic-like and procognitive activities. J Pharmacol Exp Ther. 2008 Dec;327(3):827-39. [Content Brief]

[2]. Schlumberger C, et, al. Effects of a positive allosteric modulator of mGluR5 ADX47273 on conditioned avoidance response and PCP-induced hyperlocomotion in the rat as models for schizophrenia. Pharmacol Biochem Behav. 2010 Mar;95(1):23-30. [Content Brief]

[3]. Xu J, et al. Potentiating mGluR5 function with a positive allosteric modulator enhances adaptive learning. Learn Mem. 2013 Jul 18;20(8):438-45. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / Methanol	1 mM	2.7074 mL	13.5369 mL	27.0739 mL	67.6846 mL
	5 mM	0.5415 mL	2.7074 mL	5.4148 mL	13.5369 mL
	10 mM	0.2707 mL	1.3537 mL	2.7074 mL	6.7685 mL
	15 mM	0.1805 mL	0.9025 mL	1.8049 mL	4.5123 mL
	20 mM	0.1354 mL	0.6768 mL	1.3537 mL	3.3842 mL
	25 mM	0.1083 mL	0.5415 mL	1.0830 mL	2.7074 mL
	30 mM	0.0902 mL	0.4512 mL	0.9025 mL	2.2562 mL
	40 mM	0.0677 mL	0.3384 mL	0.6768 mL	1.6921 mL
	50 mM	0.0541 mL	0.2707 mL	0.5415 mL	1.3537 mL
	60 mM	0.0451 mL	0.2256 mL	0.4512 mL	1.1281 mL
	80 mM	0.0338 mL	0.1692 mL	0.3384 mL	0.8461 mL
Methanol	100 mM	0.0271 mL	0.1354 mL	0.2707 mL	0.6768 mL

ADX-47273 Related Classifications

Neurological Disease

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:

ADX-47273851881-60-2ADX47273ADX 47273mGluRMetabotropic glutamate receptorsmGluR5glutamateantipsychoticprocognitiveInhibitorinhibitorinhibit

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ADX-47273

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Other Forms of ADX-47273:

ADX-47273 Related Antibodies

1 Publications Citing Use of MCE ADX-47273

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All mGluR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

ADX-47273 Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

ADX-47273 Related Classifications

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