产品说明书

Dexpramipexole 2HCl

Print
Chemical Structure| 104632-27-1 同义名 : 普拉克索杂质D ;(R)-Pramipexole dihydrochloride;R-(+)-Pramipexole dihydrochloride;SND 919CL2X;(+)-Pramipexole;KNS 760704;Dexpramipexole;(R)-Pramipexole (hydrochloride);KNS-760704 dihydrochloride;Dexpramipexole dihydrochloride
CAS号 : 104632-27-1
货号 : A111766
分子式 : C10H19Cl2N3S
纯度 : 99+%
分子量 : 284.249
MDL号 : MFCD13186799
存储条件:

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(369.39 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 100 mg/mL(351.8 mM),配合低频超声助溶

动物实验配方:
生物活性
描述 Dexpramipexole (Dihydrochloride), an orally bioavailable synthetic aminobenzothiazole, showed an excellent safety profile and was coincidentally noted to significantly decrease absolute eosinophil counts (AECs) in a phase 3 trial for amyotrophic lateral sclerosis. Dexpramipexole appears promising as a GC-sparing (glucocorticoid) agent without apparent toxicity in a subset of subjects with GC-responsive HESs (Hypereosinophilic syndromes)[3]. Dexpramipexole increased mitochondrial ATP production in cultured neurons or glia and reduces energy failure, prevents intracellular Ca2+ overload and affords cytoprotection when cultures are exposed to OGD (oxygen-glucose deprivation). Post-ischaemic treatment with dexpramipexole, at doses consistent with those already used in ALS (amyotrophic lateral sclerosis) patients, reduced brain infarct size and ameliorated neuroscore in mice subjected to transient or permanent MCAo (middle cerebral artery occlusion)[4]. Moreover, patch-clamp recordings in rat hippocampal neurons revealed that Dexpramipexole dose-dependently inhibited (IC50 of 814 nM) the IA current, a rapidly-inactivating K+ current that negatively regulates neuronal excitability as well as cognition and memory processes. Dexpramipexole counteracted both scopolamine-induced spatial memory loss in rats challenged in Morris Water Maze test and memory retention in rats undergoing Novel Object Recognition[5]. Dexpramipexole treatment produced profound eosinophil-lowering in peripheral blood and nasal polyp tissue[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.52mL

0.70mL

0.35mL

17.59mL

3.52mL

1.76mL

35.18mL

7.04mL

3.52mL

参考文献

[1]Rudnicki SA, Berry JD, et al. Dexpramipexole effects on functional decline and survival in subjects with amyotrophic lateral sclerosis in a Phase II study: subgroup analysis of demographic and clinical characteristics. Amyotroph Lateral Scler Frontotemporal Degener. 2013 Jan;14(1):44-51.

[2]Alavian KN, Dworetzky SI, et al. Effects of dexpramipexole on brain mitochondrial conductances and cellular bioenergetic efficiency. Brain Res. 2012 Mar 29;1446:1-11.

[3]Panch SR, Bozik ME, Brown T, et al. Dexpramipexole as an oral steroid-sparing agent in hypereosinophilic syndromes [published correction appears in Blood. 2018 Sep 27;132(13):1461]. Blood. 2018;132(5):501‐509

[4]Muzzi M, Gerace E, Buonvicino D, et al. Dexpramipexole improves bioenergetics and outcome in experimental stroke. Br J Pharmacol. 2018;175(2):272‐283

[5]Coppi E, Lana D, Cherchi F, et al. Dexpramipexole enhances hippocampal synaptic plasticity and memory in the rat. Neuropharmacology. 2018;143:306‐316

[6]Laidlaw TM, Prussin C, Panettieri RA, et al. Dexpramipexole depletes blood and tissue eosinophils in nasal polyps with no change in polyp size. Laryngoscope. 2019;129(2):E61‐E66