SB-674042 是非肽类食欲肽OX1受体拮抗剂 (Kd=5.03 nM),对OX1受体的结合能力约是对OX2受体 100 倍,IC50分别为 3.76 nM 和 531 nM。
生物活性 | SB-674042 is a potent and selective non-peptide orexinOX1receptor antagonist (Kd=5.03 nM), exhibits 100-fold selectivity forOX1overOX2receptors withIC50values of 3.76 nM and 531 nM, respectively[1][4]. |
IC50& Target[1][4] | OX1Receptor 3.76 nM (IC50) | OX2Receptor 531 nM (IC50) | OX1Receptor 1.1 nM (Ki) | OX2Receptor 129 nM (Ki) |
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体外研究 (In Vitro) | SB-674042 ([3H]) (0.2-24 nM; 2 h) shows high-affinity and serves as a radio ligand suitable for labelling human OX1 receptors stably expressed in CHO cells[1]. SB-674042 (5 μM; 4 ℃ for 30 min, and 37 ℃ for 3 h) reduces the potency of CB1 receptor agonist (Rimonabant Hydrochloride, HY-14137) to phosphorylate ERK1/2 in HEK293 cells co-expressing the orexin-1 and CB1 receptors[2]. SB-674042 (1 μM; 24 h) eradicates the increase in mTOR phosphorylation in response toOrexin-A(HY-106224) (1 nM-1 μM; 24 h) in INS-1 cells, indicating activation of the mTOR pathway induced by orexin-A was dependent on the activated OX1 receptor[3].
Western Blot Analysis[3] Cell Line: | INS-1 cells | Concentration: | 1 μM | Incubation Time: | 24 hours; accompanied with 1 μMOrexin-Afor 24 hour | Result: | Decreased the phosphorylation level of mTOR induced by Orexin-A. |
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体内研究 (In Vivo) | SB-674042 (0.3 nM/0.3 μL; icv; single dose) reduces contextual and cues fear freezing responses in Stay animals in Stress Alternatives Model (SMA) in mice[4].
Animal Model: | Stress-induced mice model (male C57BL/6NHsd mice, 22-26 g)[4] | Dosage: | 0.3 nM/0.3 μL | Administration: | Intracerebroventricular injection; subjected mice to 4 days of social aggression (days 1-4) | Result: | Resulted 39.4% Escape and 60.6% Stay phenotypes among mice. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 25 mg/mL(55.74 mM;Need ultrasonic) 配制储备液 1 mM | 2.2296 mL | 11.1480 mL | 22.2960 mL | 5 mM | 0.4459 mL | 2.2296 mL | 4.4592 mL | 10 mM | 0.2230 mL | 1.1148 mL | 2.2296 mL |
*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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 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: ≥ 1.43 mg/mL (3.19 mM); Clear solution
此方案可获得 ≥ 1.43 mg/mL (3.19 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 14.3 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。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 1.43 mg/mL (3.19 mM); Clear solution
此方案可获得 ≥ 1.43 mg/mL (3.19 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 14.3 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 1.43 mg/mL (3.19 mM); Clear solution
此方案可获得 ≥ 1.43 mg/mL (3.19 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 14.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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