Mirogabalin-DS5565-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMirogabalinCat. No.: HY-12650CAS No.: 1138245-13-2Synonyms: DS5565分式: CHNO分量: 209.28作靶点: Calcium Channel作通路: Membrane Transporter/Ion Channel; Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 mo

2、nth溶解性数据体外实验 Methanol : 16 mg/mL (76.45 mM; Need ultrasonic)H2O : 7.71 mg/mL (36.84 mM; Need ultrasonic)DMSO : 40% PEG300 5% Tween-80 45% salineSolubility: 0.83 mg/mL (3.97 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)1/2 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility

3、: 0.83 mg/mL (3.97 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 0.83 mg/mL (3.97 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Mirogabalin (DS-5565)种选择性的 2-1 配体，效且选择性地作于电压敏感性钙通道复合体的2-1 亚基。IC50 & Target 2-1 Calcium Channel 1体外研究 Mirogabalin (DS-5565) is a novel, preferentially select

4、ive 2-1 ligand characterized by high potency andselectivity to the 2-1 subunit of voltage-sensitive calcium-channel complexes in the central nervous system(CNS). In vitro experiments using membrane preparations from human and rat 2 subunit-expressed cellsshow that Mirogabalin had a slower dissociati

5、on rate from 2-1 than 2-2, in particular, 2-1 comparedwith Pregabalin. Additionally, Mirogabalin shows potent, sustained analgesic effects in streptozotocin-induced diabetic rats with induces pain, and the superior analgesic effects and wider CNS safety marginrelative to Pregabalin are attributed to

6、 its selectivity for and slow dissociation from 2-1 compared withPregabalin 1. Mirogabalin (DS-5565) is an 2-1 ligand being developed for pain associated with diabeticperipheral neuropathy, fibromyalgia, and postherpetic neuralgia. Mirogabalin targets 2-1, an auxiliaryprotein associated with voltage

7、-sensitive calcium channel complexes in the central nervous system. Thisbinding reduces calcium influx at nerve terminals, therefore reducing the release of several painneurotransmitters. The ED50 (on the transformed scale) for Mirogabalin is estimated to be 20.5 mg with a90% confidence interval (CI

8、) of 10.1-41.7 mg 2.体内研究 Additionally, Mirogabalin shows potent, sustained analgesic effects in streptozotocin-induced diabetic ratswith induced pain, and the superior analgesic effects and wider central nervous system (CNS) safety marginrelative to Pregabalin are attributed to its selectivity for a

9、nd slow dissociation from 2-1 compared withPregabalin 1.REFERENCES1. Vinik A, et al. Efficacy and safety of Mirogabalin (DS-5565) for the treatment of diabetic peripheral neuropathic pain: a randomized,double-blind, placebo- and active comparator-controlled, adaptive proof-of-concept phase 2 study.

10、Diabetes Care. 2014 Dec2. Hutmacher MM, et al. Exposure-response modeling of average daily pain score, and dizziness and somnolence, forMirogabalin (DS-5565) in patients with diabetic peripheral neuropathic pain. J Clin Pharmacol. 2016 Jan;56(1):67-77.McePdfHeightCaution: Product has not been fully valida