(Z)-Leukadherin-1

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(Z)-Leukadherin-1

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2055362-72-4

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

产品名称

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 allostericCD11bagonist. (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^[1].

IC₅₀& Target

CD11b^[1]

体外研究
(In Vitro)

(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^[1].

体内研究
(In Vivo)

(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^[1].
(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^[1].

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

分子量

421.49

性状

Solid

Formula

C₂₂H₁₅NO₄S₂

CAS 号

2055362-72-4

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

溶解性数据

In Vitro:

DMSO : 4.55 mg/mL(10.80 mM;ultrasonic and warming and heat to 60℃)

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℃, 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。