AMN 082 dihydrochloride |
カタログ番号GC11287
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AMN 082 二塩酸塩は、選択的、経口活性、および脳浸透性の mGluR7 アゴニストであり、膜貫通ドメインのアロステリック部位を介して受容体シグナル伝達を直接活性化します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 97075-46-2
Sample solution is provided at 25 µL, 10mM.
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AMN 082 dihydrochloride is an specific allosteric agonist of mGluR7 [1]. In the absence of orthosteric agonist, AMN 082 activated the human mGlu7 receptor with an EC50 of 64 nM in vitro [2].
MGlu receptors belong to the family 3 G-protein coupled receptors (GPCRs) [2]. The GPCR metabotropic glutamate receptor 7 (mGluR7) is widely expressed in the nervous system. MGluR7 is implicated in many physiological processes such as synaptic plasticity and neuroprotection [1].
Dissociated hippocampal cultured neurons had been transfected with N-terminally myc-tagged mGluR7a were used in the assay. In these neurons, treatment with AMN082 at concentrations ranging from 0.5-1 µM strikingly caused robust mGluR7 internalization. The receptor internalization was increased to 291 ± 30% of control levels. The binding site of AMN082 on mGluR7 is distinct from the glutamate binding pocket on the receptor, conventional competitive antagonists are not able to prevent the activation of the allosteric agonist to the receptor [1].
In vivo, treatment with AMN082 was shown to penetrate into the brain and hence it modulated the level of stress hormones (ACTH and cortisol) in wild type animal. But these effects were not found in the mGluR7 ko mouse [2].
References:
[1]. Pelkey KA, Yuan X, Lavezzari G, et al. mGluR7 undergoes rapid internalization in response to activation by the allosteric agonist AMN082. Neuropharmacology, 2007, 52(1): 108-117.
[2]. Gasparini F, Spooren W. Allosteric modulators for mGlu receptors. Current neuropharmacology, 2007, 5(3): 187-194.
| Cas No. | 97075-46-2 | SDF | |
| Chemical Name | N1,N2-dibenzhydrylethane-1,2-diamine dihydrochloride | ||
| Canonical SMILES | C(C1=CC=CC=C1)(C2=CC=CC=C2)NCCNC(C3=CC=CC=C3)C4=CC=CC=C4.Cl.Cl | ||
| Formula | C28H28N2.2HCl | M.Wt | 465.45 |
| 溶解度 | <46.55mg/ml in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1485 mL | 10.7423 mL | 21.4846 mL |
| 5 mM | 429.7 μL | 2.1485 mL | 4.2969 mL |
| 10 mM | 214.8 μL | 1.0742 mL | 2.1485 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)