LEO 39652|cas:1445656-91-6|西域试剂

LEO 39652,99.11%

产品编号：Bellancom-131707| CAS NO：1445656-91-6| 分子式：C₂₃H₂₃N₃O₅| 分子量：421.45

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-131707	￥4500.00	杭州北京（现货）
Bellancom-131707	￥8000.00	杭州北京（现货）
Bellancom-131707	￥16500.00	杭州北京（现货）
Bellancom-131707	￥25500.00	杭州北京（现货）
Bellancom-131707	￥38000.00	杭州北京（现货）

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LEO 39652

产品介绍

LEO 39652 是一种 dual-soft PDE4 抑制剂，对于 PDE4A 的 IC₅₀ 值为 1.2 nM，对于 PDE4B 的 IC₅₀ 值为 1.2 nM，对于 PDE4C 的 IC₅₀ 值为 3.0 nM，对于 PDE4D 的 IC₅₀ 值为 3.8 nM。LEO 39652 还抑制 TNF-α，IC₅₀ 值为 6.0 nM。LEO 39652 用于局部研究特应性皮炎。

生物活性

LEO 39652 is a dual-soft PDE4 inhibitor with IC₅₀s of 1.2 nM, 1.2 nM, 3.0 nM and 3.8 nM for PDE4A, PDE4B, PDE4C and PDE4D, respectively. LEO 39652 also inhibits TNF-α with an IC₅₀ value of 6.0 nM. LEO 39652 is used for topical research of Atopic dermatitis (AD) .

体外研究

LEO 39652 shows unbound in vitro potency when measured as LPS induced TNF-α release in human peripheral blood mononuclear cells (PBMC), incubated in serum free medium. LEO 39652 shows a relatively high binding to human serum albumin.

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

体内研究

LEO 39652 is inactivated both in blood and liver (dual-soft) while stabled in the skin. Pharmacokinetic Analysis
LEO 39652 exhibits total clearance (rats 930, minipigs 200 and monkey 300 mL/min/kg) and ratio to total AUC (rats 4, minipigs 6 and monkey 6 %) following intravenous administration (rats 0.075, minipigs 0.5 and monkeys 2.0 mg/kg).

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

Animal Model:	3 male Sprague Dawley rats, 2 female Göttingen minipigs, 2 male Göttingen minipigs, 2 female cynomolgus monkeys and 2 male cynomolgus monkeys
Dosage:	Rats 0.075, minipigs 0.5 and monkeys 2.0 mg/kg
Administration:	Intravenous injection
Result:	Total clearance of 930, 200 and 300 mL/min/kg for rats, minipigs and monkeys, respectively.

体内研究

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

Animal Model:	3 male Sprague Dawley rats, 2 female Göttingen minipigs, 2 male Göttingen minipigs, 2 female cynomolgus monkeys and 2 male cynomolgus monkeys
Dosage:	Rats 0.075, minipigs 0.5 and monkeys 2.0 mg/kg
Administration:	Intravenous injection
Result:	Total clearance of 930, 200 and 300 mL/min/kg for rats, minipigs and monkeys, respectively.

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (59.32 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3728 mL	11.8638 mL	23.7276 mL
5 mM	0.4746 mL	2.3728 mL	4.7455 mL
10 mM	0.2373 mL	1.1864 mL	2.3728 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