LEO 39652 - CAS:1445656-91-6

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LEO 39652

目录号 : KM8104 CAS No. : 1445656-91-6 纯度 : 98%

Data Sheet 产品使用指南

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。

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10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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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.

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).

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.

分子式

C₂₃H₂₃N₃O₅

分子量

421.45

CAS号

1445656-91-6

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 : 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。

临床试验

纯度： 98%

Data Sheet

产品使用指南

摩尔计算器
稀释计算器

The molarity calculator equation

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

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分子量*

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

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浓度

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Other Forms of Rapamycin:

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The dilution calculator equation