TCS OX2 29 |
カタログ番号GC10549 |
TCS OX2 29 は、40 nM の IC50 値と 7.5 の pKI 値を持つ強力で高親和性かつ選択的なオレキシン 2 受容体 (OX2R) アンタゴニストです。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 372523-75-6
Sample solution is provided at 25 µL, 10mM.
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.
Cas No. | 372523-75-6 | SDF | |
Chemical Name | (S)-1-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-3,3-dimethyl-2-((pyridin-4-ylmethyl)amino)butan-1-one hydrochloride | ||
Canonical SMILES | O=C([C@H](C(C)(C)C)NCC1=CC=NC=C1)N(CC2=C3)CCC2=CC(OC)=C3OC.Cl | ||
Formula | C23H31N3O3 | M.Wt | 397.51 |
溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,PBS (pH 7.2): 10 mg/ml | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
1 mM | 2.5157 mL | 12.5783 mL | 25.1566 mL |
5 mM | 0.5031 mL | 2.5157 mL | 5.0313 mL |
10 mM | 0.2516 mL | 1.2578 mL | 2.5157 mL |
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Quality Control & SDS
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- Purity: >99.50%
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Average Rating: 5
(Based on Reviews and 7 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
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