1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. LEO 39652

LEO 39652 是一种 dual-soft PDE4 抑制剂,对于 PDE4AIC50 值为 1.2 nM,对于 PDE4BIC50 值为 1.2 nM,对于 PDE4CIC50 值为 3.0 nM,对于 PDE4DIC50 值为 3.8 nM。LEO 39652 还抑制 TNF-αIC50 值为 6.0 nM。LEO 39652 用于局部研究特应性皮炎。

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LEO 39652 Chemical Structure

LEO 39652 Chemical Structure

CAS No. : 1445656-91-6

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥4950
In-stock
1 mg ¥2045
In-stock
5 mg ¥4500
In-stock
10 mg ¥8000
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100 mg   询价  

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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) [1].

IC50 & Target[1]

PDE4D

3.8 nM (IC50)

PDE4A

1.2 nM (IC50)

PDE4B

1.2 nM (IC50)

PDE4C2

3.0 nM (IC50)

TNF-α

6.0 nM (IC50)

体外研究
(In Vitro)

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[2].

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

体内研究
(In Vivo)

LEO 39652 is inactivated both in blood and liver (dual-soft) while stabled in the skin[1]. 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)[1].

MCE 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[1]
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.
Clinical Trial
分子量

421.45

Formula

C23H23N3O5

CAS 号
性状

固体

颜色

Off-white to gray

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 中的溶解度 : 25 mg/mL (59.32 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

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
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3728 mL 11.8638 mL 23.7276 mL 59.3190 mL
5 mM 0.4746 mL 2.3728 mL 4.7455 mL 11.8638 mL
10 mM 0.2373 mL 1.1864 mL 2.3728 mL 5.9319 mL
15 mM 0.1582 mL 0.7909 mL 1.5818 mL 3.9546 mL
20 mM 0.1186 mL 0.5932 mL 1.1864 mL 2.9660 mL
25 mM 0.0949 mL 0.4746 mL 0.9491 mL 2.3728 mL
30 mM 0.0791 mL 0.3955 mL 0.7909 mL 1.9773 mL
40 mM 0.0593 mL 0.2966 mL 0.5932 mL 1.4830 mL
50 mM 0.0475 mL 0.2373 mL 0.4746 mL 1.1864 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
LEO 39652
目录号:
HY-131707
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