AM-1488
AM-1488 is a potent, orally active glycine receptor (GlyR) potentiator (hGlyRα3 EC50=0.45 μM).
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- CAS No.: 2079895-60-4
- Formule: C19H17N3O4S
- Masse moléculaire:383.42
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | EC50 |
0.45 μM
Compound: 20-AM-1488
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Positive allosteric modulation of human glycine alpha3 receptor expressed in HEK293T cells assessed as potentiation of glycine-induced increase in chloride ion flux after 4 mins by membrane potential blue dye based FLIPR assay
Positive allosteric modulation of human glycine alpha3 receptor expressed in HEK293T cells assessed as potentiation of glycine-induced increase in chloride ion flux after 4 mins by membrane potential blue dye based FLIPR assay
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[PMID: 28001399] |
AM-1488 also potentiates native GlyRs in mouse spinal-cord neurons, which express mostly GlyRα1(β) and GlyRα3(β)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Mouse spinal-cord neuron
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Concentration:0.5 μM
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Incubation Time:10 min
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Result:Increased the peak current evoked by a puff of 20 µM glycine in five out of five cells, from an average of 50.8 pA to an average of 222.2 pA.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mouse model of spared nerve injury (SNI)[1]
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Dosage:20 mg/kg
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Administration:Oral gavage; 20 mg/kg; once
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Result:Produced a significant 94% reversal of tactile allodynia, and the unbound brain concentration was 2.8- and 1.6-fold higher than the mouse GlyRα1 and GlyRα3 EC50 values, respectively.
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Animal Model:Naive mice[1]
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Dosage:20 mg/kg
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Administration:Oral gavage; 20 mg/kg; once
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Result:Showed not significantly different from mice treated with vehicle.
Chemical Information
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CAS No. 2079895-60-4
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Masse moléculaire 383.42
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Formule C19H17N3O4S
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SMILES
O=C1[C@@]2([H])[C@@](CN(C2)S(=O)(C3=CC=C(OC=C4)C4=C3)=O)([H])C5=CN=CC=C5N1C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Xin Huang, et al. Crystal structures of human glycine receptor α3 bound to a novel class of analgesic potentiators. Nat Struct Mol Biol. 2017 Feb;24(2):108-113. [Content Brief]
[2]. Howard Bregman, et al. The Discovery and Hit-to-Lead Optimization of Tricyclic Sulfonamides as Potent and Efficacious Potentiators of Glycine Receptors. J Med Chem. 2017 Feb 9;60(3):1105-1125. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AM-1488 Related Classifications
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