BD-1047 二氢溴酸盐是一种选择性的sigma-1 receptor受体拮抗剂，作用于精神分裂症动物模型，具有抗精神病活性。
| 生物活性 | BD-1047 (dihydrobromide) is a selective functional antagonist ofsigma-1 receptor, shows antipsychotic activity in animal models predictive of efficacy in schizophrenia[1]. |
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体外研究
(In Vitro) | BD-1047 (dihydrobromide) prevents that Cutamesine reduces the cell death rate induced by light exposure in murine photoreceptor-derived 661w cells[2].
BD-1047 (dihydrobromide) attenuates that Cutamesine reduces the mitochondrial damage and the elevated level of caspase 3/7 activity[2].
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体内研究
(In Vivo) | BD-1047 (dihydrobromide) (1-10 mg/kg; i.p.) decreases the Apomorphine (APO)-induced climbing behavior at the dose of 10 mg/kg in mice[1].
BD-1047 (dihydrobromide) counteracts the antidepressant-like effect induced by co-administration of pramipexole and sertraline (but not pramipexole and fluoxetine)[3].
BD-1047 (dihydrobromide) reduces the increasing expression of pNR1, and reverses the Sig-1 R agonists potentiated NMDA-induced pain behaviour and pNR1 immunoreactivity[4].
| Animal Model: | Male Albino Swiss mice (50 days old, 25–28 g)[1] | | Dosage: | 1 mg/kg, 3 mg/kg, 10 mg/kg | | Administration: | Intraperitoneal injection | | Result: | Decreased the APO-induced climbing at the dose of 10 mg/kg in mice. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: H2O : 25 mg/mL(57.20 mM;Need ultrasonic) DMSO : 25 mg/mL(57.20 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.2881 mL | 11.4406 mL | 22.8812 mL | | 5 mM | 0.4576 mL | 2.2881 mL | 4.5762 mL | | 10 mM | 0.2288 mL | 1.1441 mL | 2.2881 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 (sealed storage, away from moisture)。-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： PBS Solubility: 33.33 mg/mL (76.26 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (5.72 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.72 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。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (5.72 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.72 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 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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