Identification | Back Directory | [Name]
MK 0657-CIS-(-)-ISOMER | [CAS]
808732-98-1 | [Synonyms]
MK-0657 CERC301 CERC-301 CERC 301 Rislenemdaz MK 0657-CIS-(-)-ISOMER 1-Piperidinecarboxylic acid, 3-fluoro-4-[(2-pyrimidinylamino)methyl]-, (4-methylphenyl)methyl ester, (3S,4R)- | [Molecular Formula]
C19H23FN4O2 | [MDL Number]
MFCD14635204 | [MOL File]
808732-98-1.mol | [Molecular Weight]
358.41 |
Chemical Properties | Back Directory | [Boiling point ]
527.4±60.0 °C(Predicted) | [density ]
1.24±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 150 mg/mL (418.52 mM) | [form ]
Solid | [pka]
3.75±0.10(Predicted) | [color ]
White to off-white |
Hazard Information | Back Directory | [Uses]
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. | [in vivo]
Rislenemdaz (CERC-301) (1, 3, 10, and 30 mg/kg) significantly decreases immobility frequency (P<0.001) and significantly increases swimming behavior (P<0.01 for 1, 3, and 30 mg/kg; P<0.05 for 10 mg/kg) compare to the vehicle control. Rislenemdaz plasma levels are approximately 15, 120, 390, 1420, 4700, and 14,110 nM (0.015, 0.120, 0.390, 1.42, 4.7, and 14.11 uM) at the time of sampling, corresponding to approximately 5, 29, 56, 83, 94, and 98% RO, respectively, in rats. The ED50 for increaing 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 total distance traveling (P<0.01 for 1 mg/kg; P<0.001 for 3, 10, and 30 mg/kg) compare to vehicle control over the 60 min test[1]. | [storage]
Store at -20°C | [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. DOI:10.1002/prp2.198 |
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Novachemistry
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