2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. ADX-47273

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 Chemical Structure

ADX-47273 Chemical Structure

CAS No. : 851881-60-2

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of ADX-47273:

ADX-47273 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE ADX-47273

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mGluR1 mGluR2 mGluR3 mGluR4 mGluR5 mGluR6 mGluR7 mGluR8 mGluR

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  • Purity & Documentation

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Description

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[1][2].

IC50 & Target[1]

mGluR5

0.17 μM (EC50)

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 Ki of 4.3 μM[1].

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

ADX-47273 Related Antibodies
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.
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
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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

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

Purity: 99.34%

COA (245 KB) HNMR (210 KB) LCMS (484 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 / 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
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ADX-47273 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:

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

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