MDL-28170-Calpain-Inhibitor-III-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMDL-28170Cat. No.: HY-18236CAS No.: 88191-84-8Synonyms: Calpain Inhibitor III分式: CHNO分量: 382.45作靶點(diǎn): Proteasome作通路: Metabolic Enzyme/Protease儲(chǔ)存式: Powder -20C 3 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 30 mg/mL (7

2、8.44 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.6147 mL 13.0736 mL 26.1472 mL5 mM 0.5229 mL 2.6147 mL 5.2294 mL10 mM 0.2615 mL 1.3074 mL 2.6147 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍福渲魄罢?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作

3、液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.25 mg/mL (5.88 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.25 mg/mL (5.88 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOL

4、OGICAL ACTIVITY物活性 MDL-28170 (Calpain Inhibitor III)種有效的、選擇性的、具有膜滲透性的半胱氨酸蛋酶 (calpain)抑制劑，可在全給藥后迅速穿過腦屏障。MDL-28170 還能阻斷-secretase。IC50 & Target Calpain 1.體外研究 MDL-28170 significantly and time-dependently improves the recovery of synaptic responses in hippocampalslices following prolonged, moderate hyp

5、oxia without hypoxic depolarization 1.MDL-28170 dose-dependently inhibits brain cysteine proteinase activity (in vitro Ki= 0.01 M) 2.體內(nèi)研究 Treatment with MDL-28170 (50 mg/kg, i.p.) completely prevents the striatal damage in four animals in eachof the two treatment groups. The numbers of necrotic neur

6、ons are reduced by 85% and 68% in animals inwhich MDL-28170 injections are initiated at 0.5 and 3 h of recirculation, respectively 2.MDL-28170 (30 mg/kg, i.p.) reduces the functional and structural deterioration of corpus callosum followingfluid percussion injury 3.MDL-28170 (10 mg/kg, i.p.) signifi

7、cantly improves nerve function parameters in diabetic rats. MDL-28170 (3and 10 mg/kg, i.p.) improves nociceptive behavior in diabetic rats 5.REFERENCES1. Chen ZF, et al. Neuronal recovery after moderate hypoxia is improved by the calpain inhibitor MDL28170. Brain Res. 1997 Sep19;769(1):188-92.2. Li

8、PA, et al. Postischemic treatment with calpain inhibitor MDL 28170 ameliorates brain damage in a gerbil model of global ischemia.Neurosci Lett. 1998 May 8;247(1):17-20.3. Ai J, et al. Calpain inhibitor MDL-28170 reduces the functional and structural deterioration of corpus callosum following fluid p

9、ercussioninjury. J Neurotrauma. 2007 Jun;24(6):960-78.4. De Strooper B, et al. A presenilin-1-dependent gamma-secretase-like protease mediates release of Notch intracellular domain. Nature.1999 Apr 8;398(6727):518-22.5. Kharatmal SB, et al. Calpain inhibitor, MDL 28170 confer electrophysiological, nociceptive and biochemical improvement in diabeticneuropathy. Neuropharmacology. 2015 Oct;97:113-21.McePdfHeightCaution: Product has not been fully validated for