TCS-OX2-29|TCS-OX229

Cas No.:	372523-75-6
Chemical Name:	(2S)-1-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)-3,3-dimethyl-2-[(4-pyridinylmethyl)amino]-1-butanone, monohydrochloride
SMILES:	COC1=C(OC)C=C(CN(C([C@H](C(C)(C)C)NCC2=CC=NC=C2)=O)CC3)C3=C1.Cl
Formula:	C₁₁H₅F₂NO₄S
M.Wt:	285.22
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

TCS-OX2-29 is a potent and selective OX2 receptor antagonist with IC50 of 40 nM. Displays >250-fold selectivity for OX2 over OX1.target: OX2 IC 50: 40 nMIn vitro:TCS-OX2-29 shows selectivity for ion channels, and transporters (<30% inhibition at 10 μM), which includes G-protein coupled receptors associated with food intake including galanin and neuripeptide Y. [1]TCS-OX2-29 Inhibits orexin A induced IP3 accumulation and ERK1/2 phosphorylation in CHO cells transfected with the OX2 receptor. [2]

References:

[1]. Hirose M et al. N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: the first orexin-2 receptor selective non-peptidicantagonist. Bioorg Med Chem Lett, 2003 Dec 15, 13(24):4497-9. [2]. R Mould et al. Binding kinetics differentiates functional antagonism of orexin-2 receptor ligands. Br J Pharmacol. 2014 Jan; 171(2): 351-363.

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.