ADX-47273

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

Cat. No.: HY-13058 Purity: 98.77%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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.

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ADX-47273 화학구조

CAS No. : 851881-60-2

사이즈	재고	수량

무료 샘플 (0.1 - 0.2 mg)	지금 신청하기
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

or 대량구매 문의

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

고객리뷰

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

•CUNY Hunter College. 2020 Sep.

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•Related Screening Libraries:

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View All mGluR Isoform Specific Products:

View All Isoforms

mGluR1 mGluR2 mGluR3 mGluR4 mGluR5 mGluR6 mGluR7 mGluR8 mGluR

Biological Activity
순도&문서
References
고객리뷰

제품 설명

IC₅₀ & Target^[1]

mGluR5

0.17 μM (EC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HCCLM3	IC₅₀	66.4 μM Compound: ADX-47273	Antiproliferative activity against human HCCLM3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human HCCLM3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 38905539]
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.

분자량

369.36

화학식

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

선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

용액&용해도

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.

몰농도 계산기
농도 희석 계산기

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:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.77 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

순도&문서

Purity: 99.34%

Select Batch:

Data Sheet (274 KB) SDS (480 KB)

COA (245 KB) HNMR (210 KB) LCMS (484 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

고객리뷰

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

순도&문서

References

고객리뷰

ADX-47273 Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

ADX-47273 Related Classifications

Keywords:

최근 본 상품:

고객리뷰

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report