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ALX 5407 hydrochloride

Catalog No.GC15467

GlyT1 inhibitor,selective non-transportable

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ALX 5407 hydrochloride Chemical Structure

Cas No.: 200006-08-2

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10mg
$329.00
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Sample solution is provided at 25 µL, 10mM.

Description of ALX 5407 hydrochloride

ALX 5407 is a potent and selective inhibitor of the hGlyT1 glycine transporter. It completely inhibited glycine transport in the GlyT1 cells with an IC50 value of 3 nM [1].

GlyT1 is a family of glycine transporters. Transporters terminate the actions of both glycine and glutamate. There are at least three splice variants in the GlyT1 family, called 1A, 1B, and 1C. GlyT1 is distributed widely throughout the CNS, and that distribution correlates better with the localization of N-methyl-D-aspartate (NMDA) receptors than with the strychnine-sensitive glycine receptor [1].

QT6-1C cells were treated with 50 nM ALX 5407, and then were washed four times with HBS. After washing, 90 ?l of HBS was added. The rate at which ALX 5407 dissociated from the GlyT1C transporter was then measured. A long half-time was found. This indicates the binding of ALX 5407 to the GlyT1C transporter is essentially irreversible [1].

Using microdialysis, it was found that in vivo in rat prefrontal cortex (PFC), administration of ALX 5407 at a dose of 10 mg/kg, p.o., resulted in an increase of 40% in PFC glycine levels measured 60 to 90 min after drug administration, whereas the lower dose at 1 mg/kg elicited a slight, nonsignificant elevation [1].

Reference:
[1].  Atkinson BN, Bell SC, De Vivo M, et al. ALX 5407: a potent, selective inhibitor of the hGlyT1 glycine transporter. Mol Pharmacol, 2001, 60(6):1414-20.

Chemical Properties of ALX 5407 hydrochloride

Cas No. 200006-08-2 SDF
Chemical Name (S)-2-((3-([1,1'-biphenyl]-4-yloxy)-3-(4-fluorophenyl)propyl)(methyl)amino)acetic acid hydrochloride
Canonical SMILES FC1=CC=C(C=C1)[C@H](CCN(C)CC(O)=O)OC2=CC=C(C3=CC=CC=C3)C=C2.Cl
Formula C24H24FNO3.HCl M.Wt 429.92
Solubility <42.99mg/ml in DMSO; <21.5mg/ml in ethanol 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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of ALX 5407 hydrochloride

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1 mg 5 mg 10 mg
1 mM 2.326 mL 11.6301 mL 23.2601 mL
5 mM 0.4652 mL 2.326 mL 4.652 mL
10 mM 0.2326 mL 1.163 mL 2.326 mL
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