LY487379-d3 hydrochloride

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LY487379-d3 hydrochloride 

LY487379-d3 hydrochloride 是 LY487379 hydrochloride 的氘代物。LY487379 hydrochloride 是一种选择性人 mGluR2 正变构调节剂 (PAM)。LY487379 hydrochloride 增强谷氨酸刺激[35S]GTPγS 与 EC50 值分别为 1.7 μM 和 >10 μM 的 mGlu2 和 mGlu3 受体的结合。LY487379 hydrochlorid

LY487379-d3 hydrochloride

LY487379-d3 hydrochloride Chemical Structure

CAS No. : 2732982-35-1

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生物活性

LY487379-d3 hydrochloride is the deuterium labeled LY487379 hydrochloride. LY487379 hydrochloride is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 hydrochloride potentiates glutamate-stimulated [35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 hydrochloride promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 hydrochloride can be used for schizophrenia research[2].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

491.93

Formula

C21H17D3ClF3N2O4S

CAS 号

2732982-35-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献
  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Agnieszka Nikiforuk, et al. Effects of a positive allosteric modulator of group II metabotropic glutamate receptors, LY487379, on cognitive flexibility and impulsive-like responding in rats. J Pharmacol Exp Ther. 2010 Dec;335(3):665-73.

    [3]. Hervé Schaffhauser, et al. Pharmacological characterization and identification of amino acids involved in the positive modulation of metabotropic glutamate receptor subtype 2. Mol Pharmacol. 2003 Oct;64(4):798-810.

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