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

433.97

C₂₃H₃₂ClN₃O₃

1610882-30-8

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Hirose M, et al. N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: the first orexin-2 receptor selective non-peptidic antagonist. 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]. Mould R, et al. Binding kinetics differentiates functional antagonism of orexin-2 receptor ligands. Br J Pharmacol. 2014 Jan;171(2):351-63.

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

IC50: 40 nM (OX₂R)^[1]; pKi: 7.5 (OX₂R)^[2]

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

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

397.51

C₂₃H₃₁N₃O₃

372523-75-6

Room temperature in continental US; may vary elsewhere.

DMSO : 25 mg/mL (62.89 mM; Need ultrasonic)

Ethanol : 25 mg/mL (62.89 mM; Need ultrasonic)

H₂O : 0.67 mg/mL (1.69 mM; Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.5 mg/mL (6.29 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (6.29 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.5 mg/mL (6.29 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (6.29 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.5 mg/mL (6.29 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (6.29 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [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.