Dantrolene-13C3(Synonyms: F 368-13C3)

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Dantrolene-13C3 (Synonyms: F 368-13C3)

Dantrolene-13C3 是 13C3 标记的 Dantrolene。Dantrolene (F368) 是一种肌肉松弛剂，非竞争性地抑制人红细胞谷胱甘肽还原酶 (glutathione reductase)，K_i 和 IC₅₀ 值分别为 111.6 μM 和 52.3 μM。 Dantrolene 是一种兰尼碱受体拮抗剂和 Ca²⁺ 信号稳定剂。Dantrolene 可用于肌肉痉挛、恶性高热

Dantrolene-13C3 Chemical Structure

CAS No. : 1185234-99-4

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生物活性	Dantrolene-13C3 is the 13C3 labeled Dantrolene. Dantrolene (F368), a muscle relaxant, non-competitively inhibits human erythrocyte glutathione reductase. Ki and IC50 values are 111.6 μM and 52.3 μM, respectively. Dantrolene is a ryanodine receptor antagonist and Ca2+ signaling stabilizer. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington’s disease and other neuroleptic malignant syndrome.
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	317.23
Formula	C₁₁¹³C₃H₁₀N₄O₅
CAS 号	1185234-99-4
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):211-223. [2]. W J Meyler, et al. The effect of dantrolene sodium on rat skeletal muscle in relation to the plasma concentration. Eur J Pharmacol. 1979 Feb 1;53(4):335-42. [3]. F Zhao, et al. Dantrolene inhibition of ryanodine receptor Ca2+ release channels. Molecular mechanism and isoform selectivity. J Biol Chem. 2001 Apr 27;276(17):13810-6. [4]. Murat Sentürk, et al. Dantrolene inhibits human erythrocyte glutathione reductase. Biol Pharm Bull. 2008 Nov;31(11):2036-9. [5]. Shigeki Kobayashi, et al. Dantrolene, a therapeutic agent for malignant hyperthermia, markedly improves the function of failing cardiomyocytes by stabilizing interdomain interactions within the ryanodine receptor. J Am Coll Cardiol. 2009 May 26;53(21):1993-2005. [6]. Xi Chen, et al. Dantrolene is neuroprotective in Huntington’s disease transgenic mouse model. Mol Neurodegener. 2011 Nov 25;6:81.

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