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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemERislenemdazCat. No.: HY-106441ACAS No.: 808732-98-1Synonyms: MK-0657; CERC-301分式: CHFNO分量: 358.41作靶点: iGluR作通路: Membrane Transporter/Ion Channel; Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1

2、 month溶解性数据体外实验 DMSO : 150 mg/mL (418.52 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.7901 mL 13.9505 mL 27.9010 mL5 mM 0.5580 mL 2.7901 mL 5.5802 mL10 mM 0.2790 mL 1.3951 mL 2.7901 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Rislenemd

3、az （CERC-301），个服有活性且有选择性的 N-methyl-D-aspartate (NMDA) receptorsubunit 2B (GluN2B) 拮抗剂，K i 和 IC 50 分别为 8.1 nM 和 3.6 nM。IC50 & Target IC50: 3.6 nM (GluN2B) 1Ki: 8.1 nM (GluN2B) 11/2 Master of Small Molecules 您边的抑制剂师www.MedChemE体外研究 Rislenemdaz (CERC-301) inhibits calcium influx into agonist-stimulatin

4、g NMDA-GluN1a/GluN2B L(tk-) cellswith an IC50 of 3.6 nM. Rislenemdaz exhibits at least 1000 selectivity for the GluN2B receptor versus alltargets tested, including the hERG potassium channel. Rislenemdaz also exhibits minimal activity againstsigma-type receptors at 10 uM 1.体内研究 Rislenemdaz (CERC-301

5、) (1, 3, 10, and 30 mg/kg) significantly decreases immobility frequency (P50 forincreaing in frequency of swimming and decreasing in immobility are 0.3 and 0.7 mg/kg, respectively,corresponding to RO of 30 and 50%. Rislenemdaz (1, 3, 10, and 30 mg/kg) significantly increases totaldistance traveling

6、(P 1.PROTOCOLCell Assay 1 Rat, dog, rhesus monkey, and human plasma samples (3 mL, N=3) are incubated with 2 and 20 uM 14CRislenemdaz at 37C for 30 min in a shaking water bath. Following incubation, standard ultracentrifugationmethodology is used to determine the percentage of drug unbind 1.MCE has

7、not independently confirmed the accuracy of these methods. They are for reference only.Animal Four groups of 24 rats (12/sex) are given single doses of vehicle (0.5% methylcellulose MC and 0.02%Administration 1 sodium lauryl sulfate SLS in deionized water) or Rislenemdaz at 10, 30 or 100 mg/kg by or

8、al gavage at adose volume of 10 mL/kg. Three additional groups of rats (four males and three females per group) are orallydosed in the same manner with Rislenemdaz, and 24h serial blood samples are obtained and analyzed forRislenemdaz plasma concentrations and evaluated for systemic exposure. Young,

9、 adult, male rats arerandomly assigned across the treatment groups and are administered vehicle (0.5% MC/0.02% SLS), thereference compound desipramine (20 mg/kg; a tricyclic antidepressant) dissolving in sterile water, orRislenemdaz (0.1, 0.3, 1, 3, 10, and 30 mg/kg) suspending in 0.5% MC/0.02% SLS,

10、 twice on Day 1 (afterhabituation; 24 h prior to test, and prior to dark cycle) and once on Day 2 (30 min pretest for desipramineand 45 min pretest for Rislenemdaz and vehicle) 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Rachel Garner

11、, et al. Preclinical pharmacology and pharmacokinetics of CERC301, a GluN2Bselective Nm ethylDaspartate receptorantagonist. Pharm acol Res Perspect. 2015 Dec; 3(6): e00198.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-3792;Fax:E-mail: techMedChemE2/2 Master of Small Molecules 您边的抑制剂师