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AMN082 free base

Cat No.:V70619 Purity: ≥98%
AMN082 free base is a selective, orally bioactive, BBB (blood-brain barrier) permeable (penetrable) mGluR7 agonist that directly activates receptor signaling through the allosteric site in the transmembrane region.
AMN082 free base
AMN082 free base Chemical Structure CAS No.: 83027-13-8
Product category: mGluR
This product is for research use only, not for human use. We do not sell to patients.
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5mg
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Other Forms of AMN082 free base:

  • AMN082
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
AMN082 free base is a selective, orally bioactive, BBB (blood-brain barrier) permeable (penetrable) mGluR7 agonist that directly activates receptor signaling through the allosteric site in the transmembrane region. AMN082 free base effectively inhibits cAMP accumulation and stimulates GTPγS binding (EC50, 64-290 nM) in transfected mammalian cells expressing mGluR7. AMN082 free base is selective for other mGluR subtypes and selective ionotropic glutamate receptors. Has antidepressant effects.
Biological Activity I Assay Protocols (From Reference)
Targets
mGluR7[1]
ln Vitro
Without affecting the basal release of glutamate, preincubation of the synaptosomes with AMN082 (1 μM) for 10 min prior to 4-aminopyridine treatment effectively suppresses the glutamate release triggered by 4-aminopyridine[2].
ln Vivo
mGluR7+/+ mice (C57BL/6 genetic background) exhibit stress hormone increases in response to AMN082 (6 mg/kg; po) in a mGluR7-dependent manner[1]. AMN082 (1.25-5.0 mg/kg, ip; 30 min before each injection of cocaine during recurrent drug administration or prior to a cocaine challenge) attenuates the expression and development of cocaine locomotor sensitization in a dose-dependent manner[3].
References

[1]. A selective metabotropic glutamate receptor 7 agonist: activation of receptor signaling via an allosteric site modulates stress parameters in vivo. Proc Natl Acad Sci U S A. 2005;102(51):18712-18717.

[2]. Metabotropic glutamate 7 receptor agonist AMN082 inhibits glutamate release in rat cerebral cortex nerve terminal. Eur J Pharmacol. 2018;823:11-18.

Additional Infomation
AMN082 dihydrochloride is a hydrochloride obtained by combining N,N'-bis(diphenylmethyl)ethane-1,2-diamine with two molar equivalent of hydrochloric acid. It has a role as a metabotropic glutamate receptor agonist, a geroprotector and a neuroprotective agent. It contains a N,N'-bis(diphenylmethyl)ethane-1,2-diamine(2+).
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C28H28N2
Molecular Weight
392.54
Exact Mass
464.179
CAS #
83027-13-8
Related CAS #
AMN082;97075-46-2
PubChem CID
11698390
Appearance
White to off-white solid powder
Boiling Point
533.7ºC at 760 mmHg
Flash Point
321.5ºC
LogP
8.13
Hydrogen Bond Donor Count
4
Hydrogen Bond Acceptor Count
2
Rotatable Bond Count
9
Heavy Atom Count
32
Complexity
362
Defined Atom Stereocenter Count
0
InChi Key
YRQCDCNQANSUPB-UHFFFAOYSA-N
InChi Code
InChI=1S/C28H28N2.2ClH/c1-5-13-23(14-6-1)27(24-15-7-2-8-16-24)29-21-22-30-28(25-17-9-3-10-18-25)26-19-11-4-12-20-26;;/h1-20,27-30H,21-22H2;2*1H
Chemical Name
N,N'-dibenzhydrylethane-1,2-diamine;dihydrochloride
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: This product requires protection from light (avoid light exposure) during transportation and storage.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 12.5 mg/mL (31.84 mM)
Solubility (In Vivo)
Solubility in Formulation 1: 1.25 mg/mL (3.18 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

Solubility in Formulation 2: ≥ 1.25 mg/mL (3.18 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.5475 mL 12.7376 mL 25.4751 mL
5 mM 0.5095 mL 2.5475 mL 5.0950 mL
10 mM 0.2548 mL 1.2738 mL 2.5475 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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