| Bioactivity | 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]. | ||||||||||||
| Invitro | TCS-OX2-29 inhibits orexin A induced IP3 accumulation and ERK1/2 phosphorylation in CHO cells transfected with the OX2 receptor[2]. | ||||||||||||
| In Vivo | 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[2]. Animal Model: | ||||||||||||
| Name | TCS-OX2-29 | ||||||||||||
| CAS | 372523-75-6 | ||||||||||||
| Formula | C23H31N3O3 | ||||||||||||
| Molar Mass | 397.51 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |
TCS-OX2-29
CAS: 372523-75-6 F: C23H31N3O3 W: 397.51
TCS-OX2-29 is a potent, high affinities and selective orexin-2 receptor (OX2R) antagonist with an IC50 value of 40 nM an
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