AM-1488

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AM-1488 is a potent, orally active glycine receptor (GlyR) potentiator (hGlyRα3 EC₅₀=0.45 μM).

For research use only. We do not sell to patients.

AM-1488 Chemical Structure

CAS No. : 2079895-60-4

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Description

AM-1488 is a potent, orally active glycine receptor (GlyR) potentiator (hGlyRα3 EC₅₀=0.45 μM)^[1]^[2].

Cellular Effect

Cell Line	Type	Value	Description	References
HEK-293T	EC₅₀	0.45 μM Compound: 20-AM-1488	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	[PMID: 28001399]

In Vitro

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.

Cell Viability Assay^[1]

Cell Line:	Mouse spinal-cord neuron
Concentration:	0.5 μM
Incubation Time:	10 min
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.

In Vivo

AM-1488 (oral gavage; 20 mg/kg; once) treatment significantly reverse mechanical allodynia induced by nerve injury in a mouse model of neuropathic pain, without being confounded by sedation or motor side effects^[1].

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

Animal Model:	Mouse model of spared nerve injury (SNI)^[1]
Dosage:	20 mg/kg
Administration:	Oral gavage; 20 mg/kg; once
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.

Animal Model:	Naive mice^[1]
Dosage:	20 mg/kg
Administration:	Oral gavage; 20 mg/kg; once
Result:	Showed not significantly different from mice treated with vehicle.

Molecular Weight

383.42

Formula

C₁₉H₁₇N₃O₄S

CAS No.

2079895-60-4

SMILES

O=C1[C@@]2([H])[C@@](CN(C2)S(=O)(C3=CC=C(OC=C4)C4=C3)=O)([H])C5=CN=CC=C5N1C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]

AM-1488 Related Classifications

Neurological Disease

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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:

AM-14882079895-60-4AM1488AM 1488Othersoral activityglycine receptormouse spinal-cord neuronInhibitorinhibitorinhibit

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