ADH-503 ((Z)-Leukadherin-1 choline) 是一种具有口服活性的，变构的CD11b激动剂。ADH-503 可以导致与肿瘤相关的巨噬细胞重新极化，减少肿瘤浸润性免疫抑制骨髓细胞的数量，并增强树突状细胞的反应。
| 生物活性 | ADH-503 ((Z)-Leukadherin-1 choline) is an orally active and allostericCD11bagonist. ADH-503 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses[1]. |
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体外研究
(In Vitro) | ADH-503 ((Z)-Leukadherin-1 choline; 4 μM; 8 days) reduces the numbers of total tumor-infiltrating CD11b+cells and subsets of CD11b+monocytes, granulocytes, eosinophils, and macrophages[1].
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体内研究
(In Vivo) | ADH-503 ((Z)-Leukadherin-1 choline; oral gavage; 30, 60, or 120 mg/kg; twice a day for 60 days) delayes tumor progression, leading to a significantly decreased tumor burden in time-point analysis and improved overall survival[1].
ADH-503 (oral gavage; 30, 100 mg/kg; twice a day; on days 1 and 5) has the mean half-life of 4.68 and 3.95 hours, a maximum concentration of 1716 and 2594 ng/mL and AUC0-tin the plasma of 6950 and 13962 ng.h/mL at 30 and 100 mg/kg dosing, respectively[1].
| Animal Model: | KPC mice [p48-CRE/Lox-stop-Lox(LSL)-KrasG12D/p53flox/flox][1] | | Dosage: | 30, 60, or 120 mg/kg | | Administration: | Oral gavage; 60 days | | Result: | Delayed tumor progression, leading to a significantly decreased tumor burden in time-point analysis and improved overall survival. |
| Animal Model: | Male rats[1] | | Dosage: | 30, 100 mg/kg (Pharmacokinetic Analysis) | | Administration: | Oral gavage twice a day; on days 1 and 5 | | Result: | Had the mean half-life of 4.68 and 3.95 hours, a maximum concentration of 1716 and 2594 ng/mL and AUC0-tin the plasma of 6950 and 13962 ng.h/mL at 30 and 100 mg/kg dosing, respectively. |
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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: DMSO : 21.43 mg/mL(40.85 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.9060 mL | 9.5302 mL | 19.0603 mL | | 5 mM | 0.3812 mL | 1.9060 mL | 3.8121 mL | | 10 mM | 0.1906 mL | 0.9530 mL | 1.9060 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： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.14 mg/mL (4.08 mM); Clear solution
此方案可获得 ≥ 2.14 mg/mL (4.08 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 21.4 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。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.14 mg/mL (4.08 mM); Clear solution
此方案可获得 ≥ 2.14 mg/mL (4.08 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 21.4 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: 2.08 mg/mL (3.96 mM); Suspended solution; Need ultrasonic
此方案可获得 2.08 mg/mL (3.96 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 20.8 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。 *以上所有助溶剂都可在本网站选购。
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