ADH-503 (Z-Leukadherin-1 choline)|cas:2055362-74-6|西域试剂

ADH-503 (Z-Leukadherin-1 choline),98.0%

产品编号：Bellancom-15701B| CAS NO：2055362-74-6| 分子式：C₂₇H₂₈N₂O₅S₂| 分子量：524.65

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货号	价格	库存与货期
Bellancom-15701B	￥550.00	杭州北京（现货）
Bellancom-15701B	￥900.00	杭州北京（现货）
Bellancom-15701B	￥2500.00	杭州北京（现货）
Bellancom-15701B	￥3500.00	杭州北京（现货）

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ADH-503 (Z-Leukadherin-1 choline)

产品介绍

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 allosteric CD11b agonist. 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.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.
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 AUC_0-t in the plasma of 6950 and 13962 ng.h/mL at 30 and 100 mg/kg dosing, respectively.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	KPC mice [p48-CRE/Lox-stop-Lox(LSL)-Kras^G12D/p53^flox/flox]
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
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 AUC_0-t in the plasma of 6950 and 13962 ng.h/mL at 30 and 100 mg/kg dosing, respectively.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	KPC mice [p48-CRE/Lox-stop-Lox(LSL)-Kras^G12D/p53^flox/flox]
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
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 AUC_0-t in the plasma of 6950 and 13962 ng.h/mL at 30 and 100 mg/kg dosing, respectively.

性状

Solid

溶解性数据

In Vitro:

DMSO : 21.43 mg/mL (40.85 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

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-CD in 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 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
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。
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