Rislenemdaz (MK-0657) (Synonyms: MK-0657; CERC-301) |
رقم الكتالوجGC30835
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Rislenemdaz (MK-0657) (CERC-301) هو أحد مضادات مستقبلات N-methyl-D-aspartate (NMDA) 2B (GluN2B) المتوفر بيولوجيًا عن طريق الفم والانتقائية مع Ki و IC 50 من 8.1 نانومتر و 3.6 نانومتر ، على التوالي.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 808732-98-1
Sample solution is provided at 25 µL, 10mM.
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Rislenemdaz (CERC-301) is an orally bioavailable and selective N-methyl-D-aspartate (NMDA) receptor subunit 2B (GluN2B) antagonist with Ki and IC 50 of 8.1 nM and 3.6 nM, respectively.
Rislenemdaz (CERC-301) inhibits calcium influx into agonist-stimulating NMDA-GluN1a/GluN2B L(tk-) cells with an IC50 of 3.6 nM. Rislenemdaz exhibits at least 1000× selectivity for the GluN2B receptor versus all targets tested, including the hERG potassium channel. Rislenemdaz also exhibits minimal activity against sigma-type receptors at 10 uM[1].
Rislenemdaz (CERC-301) (1, 3, 10, and 30 mg/kg) significantly decreases immobility frequency (P
[1]. Rachel Garner, et al. Preclinical pharmacology and pharmacokinetics of CERC‐301, a GluN2B‐selective N‐methyl‐D‐aspartate receptor antagonist. Pharmacol Res Perspect. 2015 Dec; 3(6): e00198.
Cell experiment: | Rat, dog, rhesus monkey, and human plasma samples (3 mL, N=3) are incubated with 2 and 20 uM [14C] Rislenemdaz at 37°C for 30 min in a shaking water bath. Following incubation, standard ultracentrifugation methodology is used to determine the percentage of drug unbind[1]. |
Animal experiment: | Four groups of 24 rats (12/sex) are given single doses of vehicle (0.5% methylcellulose [MC] and 0.02% sodium lauryl sulfate [SLS] in deionized water) or Rislenemdaz at 10, 30 or 100 mg/kg by oral gavage at a dose volume of 10 mL/kg. Three additional groups of rats (four males and three females per group) are orally dosed in the same manner with Rislenemdaz, and 24h serial blood samples are obtained and analyzed for Rislenemdaz plasma concentrations and evaluated for systemic exposure. Young, adult, male rats are randomly assigned across the treatment groups and are administered vehicle (0.5% MC/0.02% SLS), the reference compound desipramine (20 mg/kg; a tricyclic antidepressant) dissolving in sterile water, or Rislenemdaz (0.1, 0.3, 1, 3, 10, and 30 mg/kg) suspending in 0.5% MC/0.02% SLS, twice on Day 1 (after habituation; ~24 h prior to test, and prior to dark cycle) and once on Day 2 (30 min pretest for desipramine and 45 min pretest for Rislenemdaz and vehicle)[1]. |
References: [1]. Rachel Garner, et al. Preclinical pharmacology and pharmacokinetics of CERC‐301, a GluN2B‐selective N‐methyl‐D‐aspartate receptor antagonist. Pharmacol Res Perspect. 2015 Dec; 3(6): e00198. | |
| Cas No. | 808732-98-1 | SDF | |
| المرادفات | MK-0657; CERC-301 | ||
| Canonical SMILES | O=C(N1C[C@@H](F)[C@@H](CNC2=NC=CC=N2)CC1)OCC3=CC=C(C)C=C3 | ||
| Formula | C19H23FN4O2 | M.Wt | 358.41 |
| الذوبان | DMSO : 150 mg/mL (418.52 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7901 mL | 13.9505 mL | 27.901 mL |
| 5 mM | 558 μL | 2.7901 mL | 5.5802 mL |
| 10 mM | 279 μL | 1.3951 mL | 2.7901 mL |
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Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)