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ALX 5407 hydrochloride Sale

(Synonyms: N-[(3R)-3-([1,1'-联苯]-4-基氧)-3-(4-氟苯基)丙基]-N-甲基甘氨酸盐酸盐) 目录号 : GC15467

An inhibitor of GlyT1

ALX 5407 hydrochloride Chemical Structure

Cas No.:200006-08-2

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10mg
¥3,293.00
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产品描述

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

Cas No. 200006-08-2 SDF
别名 N-[(3R)-3-([1,1'-联苯]-4-基氧)-3-(4-氟苯基)丙基]-N-甲基甘氨酸盐酸盐
化学名 (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
分子式 C24H24FNO3.HCl 分子量 429.92
溶解度 <42.99mg/ml in DMSO; <21.5mg/ml in ethanol 储存条件 Store at -20°C
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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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