(Z)-Leukadherin-1 ADH-503 free base,98.0%

产品编号:Bellancom-15701A| CAS NO:2055362-72-4| 分子式:C22H15NO4S2| 分子量:421.49

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货号 包装 价格 库存与货期 购买量 操作
Bellancom-15701A
550.00 杭州 北京(现货)
Bellancom-15701A
900.00 杭州 北京(现货)
Bellancom-15701A
2500.00 杭州 北京(现货)
Bellancom-15701A
3500.00 杭州 北京(现货)

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(Z)-Leukadherin-1 ADH-503 free base

产品介绍 (Z)-Leukadherin-1 (ADH-503 free base) 是一种具有口服活性的,变构的 CD11b 激动剂。(Z)-Leukadherin-1 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

(Z)-Leukadherin-1 (ADH-503 free base) is an orally active and allosteric CD11b agonist. (Z)-Leukadherin-1 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

(Z)-Leukadherin-1 (ADH-503 free base; 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

(Z)-Leukadherin-1 (ADH-503 free base; 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.
(Z)-Leukadherin-1 (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-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)-KrasG12D/p53flox/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 AUC0-t in the plasma of 6950 and 13962 ng.h/ml at 30 and 100 mg/kg dosing, respectively.
体内研究

(Z)-Leukadherin-1 (ADH-503 free base; 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.
(Z)-Leukadherin-1 (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-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)-KrasG12D/p53flox/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 AUC0-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 : 4.55 mg/mL (10.80 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3725 mL 11.8627 mL 23.7254 mL
5 mM 0.4745 mL 2.3725 mL 4.7451 mL
10 mM 0.2373 mL 1.1863 mL 2.3725 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。-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。

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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