YC-001 是杆状视蛋白 (rod opsin) 的反向激动剂和拮抗剂。YC-001 可逆地结合视杆视蛋白并稳定视杆视蛋白的结构。YC-001 保护小鼠免受强光诱导的视网膜变性。YC-001 具有研究视网膜变性的潜力。
| 生物活性 | YC-001 is an inverse agonist and antagonist ofrod opsin. YC-001 reversibly binds rod opsin and stabilizes the rod opsin structure. YC-001 protects mice from bright light-induced retinal degeneration. YC-001 has the potential for the research of retinal degeneration[1]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | YC-001 (0-100 μM) shows a potency activity of 8.7 μM and an efficacy at 150–310%[1].
YC-001 (0.5, 1, 5, 10, 20, 40 μM) improves the glycosylation profile of P23H opsin mutant[1].
YC-001 (0,-1.5 μM) reversibly binds rod opsin with EC50OF 0.98 μM[1].
YC-001 (0.313, 0.625, 1.25, 2.5, 5, 10, 20, 80 μM) increases in cAMP level in a dose-dependent manner in NIH3T3 cells[1].
Western Blot Analysis[1] | Cell Line: | NIH3T3 cells | | Concentration: | 0.5, 1, 5, 10, 20, 40 μM | | Incubation Time: | | | Result: | Improved the glycosylation profile of P23H opsin. |
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体内研究
(In Vivo) | YC-001 (50, 200mg/kg; i.p.) protects Abca4–/–Rdh8–/– mice from bright light-induced retinal degeneration[1].
YC-001 (200mg/kg; i.p.) enters mouse eyes after systemic administration but is not retained for prolonged periods[1].
YC-001 (100 mg/kg, 200 mg/kg; i.p.; daily for 24 days) shows virtually no acute toxicity[1].
| Animal Model: | 6-week-old Abca4 –/–Rdh8–/– mice[1] | | Dosage: | 50, 200mg/kg | | Administration: | I.P. | | Result: | Protected Abca4–/–Rdh8–/– mice from bright light-induced retinal degeneration. |
| Animal Model: | C57BL/6 mouse[1] | | Dosage: | 200 mg/kg | | Administration: | I.P. | | Result: | Entered mouse eyes after systemic administration but is not retained for prolonged periods. |
| Animal Model: | C57BL/6 mice[1] | | Dosage: | 100 mg/kg, 200 mg/kg | | Administration: | I.p.; daily, 24 days | | Result: | Showed no acute toxicity. |
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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 : 100 mg/mL(353.64 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.5364 mL | 17.6822 mL | 35.3644 mL | | 5 mM | 0.7073 mL | 3.5364 mL | 7.0729 mL | | 10 mM | 0.3536 mL | 1.7682 mL | 3.5364 mL |
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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: ≥ 2.5 mg/mL (8.84 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.84 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。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (8.84 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.84 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。 *以上所有助溶剂都可在本网站选购。
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