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TCS OX2 29

Catalog No.GC10549

TCS OX2 29는 IC50 값이 40nM이고 pKI 값이 7.5인 강력하고 친화도가 높은 선택적 오렉신-2 수용체(OX2R) 길항제입니다.

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TCS OX2 29 Chemical Structure

Cas No.: 372523-75-6

Size 가격 재고 수량
10mM (in 1mL DMSO)
US$79.00
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5mg
US$72.00
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10mg
US$108.00
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25mg
US$207.00
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50mg
US$306.00
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100mg
US$504.00
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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents Related Products

TCS-OX2-29 is a potent, high affinities and selective orexin-2 receptor (OX2R) antagonist with an IC50 value of 40 nM and a pKI value of 7.5. TCS-OX2-29 displays ~250-fold selectivity for OX2 over OX1[1][2].

TCS-OX2-29 inhibits orexin A induced IP3 accumulation and ERK1/2 phosphorylation in CHO cells transfected with the OX2 receptor[2].

TCS-OX2-29 (5-10 mg/kg; intraperitoneal injection; adult male NMRI mice) treatment suppresses conditioned place preference (CPP) acquisition and expression in both naïve and dependent mice significantly[3].

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]. Tabaeizadeh M, et al. The differential effects of OX1R and OX2R selective antagonists on morphine conditioned place preference in naïve versus morphine-dependent mice. Behav Brain Res. 2013 Jan 15;237:41-8.
[3]. R Mould et al. Binding kinetics differentiates functional antagonism of orexin-2 receptor ligands. Br J Pharmacol. 2014 Jan; 171(2): 351-363.

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