MDK-5220(Orexin-2 receptor agonist)

  Cat. No.:  DC9297   Featured
Chemical Structure
1796565-52-0
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Field of application
MDK-5220(Orexin-2 receptor agonist) is the first selective nonpeptidic orexin 2 receptor (OX2R) agonist (OX2R EC50 = 0.023 μM, Emax = 98%; OX1R EC50 = 1.616 μM, Emax = 100%)
Cas No.: 1796565-52-0
Chemical Name: Orexin 2 Receptor Agonist
Synonyms: Orexin 2 Receptor Agonist;4'-methoxy-N,N-dimethyl-3'-(N-(3-((2-(3-methylbenzamido)ethyl)amino)phenyl)sulfamoyl)-[1,1'-biphenyl]-3-carboxamide;N-[2-[3-[[5-[3-(dimethylcarbamoyl)phenyl]-2-methoxyphenyl]sulfonylamino]anilino]ethyl]-3-methylbenzamide;Nag26;Nag 26;GTPL9305;BCP17168;BDBM50121214;SB19183;compound 26 [PMID: 26267383];AK547566;3-
SMILES: S(C1=C(C([H])=C([H])C(C2C([H])=C([H])C([H])=C(C(N(C([H])([H])[H])C([H])([H])[H])=O)C=2[H])=C1[H])OC([H])([H])[H])(N([H])C1=C([H])C([H])=C([H])C(=C1[H])N([H])C([H])([H])C([H])([H])N([H])C(C1=C([H])C([H])=C([H])C(C([H])([H])[H])=C1[H])=O)(=O)=O
Formula: C32H34N4O5S
M.Wt: 586.7012
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Orexin 2 Receptor Agonist is a potent (EC50 on OX2R is 23 nM) and OX2R-selective (OX1R/OX2R EC50 ratio is 70) agonist.IC50 value: 23 nM (EC50)Target: Orexin 2 ReceptorOrexin 2 Receptor Agonist shows not only potentactivity but also high selectivity for OX2R over OX1R. In CHO cells overexpressing hOX1R and HEK-293 cells overexpressing hOX2R, compound 26 displaced [125I]orexin-A in a concentration dependent manner: 26 bound to hOX2R and hOX1R with Ki of 0.14 and 0.77 μM, respectively.[1]
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC70823 TAK-925 TAK-925 (Danavorexton) is a potent, selective, and brain-penetrant Orexin 2 receptor (OX2R) agonist with EC50 of 5.5 nM, no significant inhibition on OX1R (IC50>100 uM).TAK-925 also showed good selectivity against 106 off-target enzymes and receptors.
DC11461 TCS-OX2-29 TCS-OX2-29 is a potent and selective OX2 receptor antagonist with IC50 of 40 nM. Displays >250-fold selectivity for OX2 over OX1.
DC7513 TCS 1102 TCS 1102 is a potent, dual orexin receptor antagonist (Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively).
DC5017 Suvorexant Suvorexant (MK-4305) is a potent, selective, and orally bioavailable antagonist of OX1R and OX2R currently under clinical investigation as a novel therapy for insomnia.Suvorexant is an analytical reference standard categorized as a diazepane sedative.Formulations containing suvorexant show abuse potential similar to zolpidem in recreational polydrug users with a history of sedative and psychedelic drug use.2 Suvorexant is regulated as a Schedule IV compound in the United States. This product is intended for use in analytical forensic applications.
DC9966 MK-1064 MK-1064 is a selective orexin 2 receptor antagonist (2-SORA) for the research of insomnia.
DC9297 MDK-5220(Orexin-2 receptor agonist) MDK-5220(Orexin-2 receptor agonist) is the first selective nonpeptidic orexin 2 receptor (OX2R) agonist (OX2R EC50 = 0.023 μM, Emax = 98%; OX1R EC50 = 1.616 μM, Emax = 100%)
DC8173 Lemborexant(E2006) Lemborexant (E-2006) is a dual antagonist of the orexin OX1 and OX2 receptors which is under development for treatment of insomnia.
DC7692 Almorexant HCl (Act-078573) Almorexant(ACT078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively.
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