AS-2444697 (hydrochloride) - CAS:1287665-60-4

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AS-2444697 (hydrochloride) (Synonyms:AS 2444697)

目录号 : KCM10932 CAS No. : 1287665-60-4 纯度 : ≥95%

Data Sheet 产品使用指南

AS-2444697 is an inhibitor of interleukin-1 receptor-associated kinase 4 (IRAK4; IC = 21 nM). It is greater than 30-fold selective for IRAK4 over a panel of 146 kinases, but is less than 10-fold selective over PDGFRα, PDGFRβ, TrkA, TrkC, CLK1, Itk, and FLT3. AS-2444697 inhibits IL-1β-induced IL-6 production and LPS-induced TNF-α production in cellular assays (ICs = 250 and 47 nM, respectively). It is efficacious in rat models of adjuvant- and collagen-induced arthritis (EDs = 2.7 and 1.6 mg/kg, respectively). AS-2444697 (0.3-3 mg/kg, twice daily) reduces urinary protein excretion, the development of interstitial fibrosis and glomerulosclerosis, and renal mRNA expression of genes encoding IL-1β, IL-6, TNF-α, and chemokine (C-C motif) ligand 2 (CCL2) without affecting blood pressure in the 5/6 nephrectomized rat model of chronic kidney disease.

规格	价格	是否有货	数量
10 mM * 1 mL in DMSO		In-stock
5mg		In-stock
10mg		In-stock

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生物活性

AS2444697 is an orally active IRAK-4 inhibitor with an IC50 of 21 nM. AS2444697 potently inhibits human and rat IRAK-4 activity. AS2444697 exhibits renoprotective effects through anti-inflammatory action.

IC₅₀&Target

IRAK4

21 nM (IC50)

体内研究

AS2444697 is effective in both adjuvant induced arthritis (ED50 2.7 mg/kg, twice daily, orally) and collagen induced arthritis (ED50 1.6 mg/kg, twice daily, orally) disease models in rats. Good bioavailability was observed in pharmacokinetic studies of rats (F% 50) and dogs (F% 78) [1].
AS2444697 (0.3-3 mg/kg) significantly increased the levels of IL-1 β, IL-6, TNF - α, MCP-1, and aminotransferase (ALT and AST) in the plasma of LPS/GalN treated mice. A single dose of AS2444697 (0.3-3 mg/kg) dose dependently reduced plasma levels of all these parameters, and these effects were most significant at doses of 1 mg/kg or higher [2].
After oral administration of AS2444697 (3 mg/kg) to 5/6 Nx rats, the concentration of the unchanged drug in plasma and tissues (liver and kidney) reached its peak at 1 hour and gradually decreased, with a terminal half-life of 2.7-2.9 hours [2].

Animal Model:	Male 6-week-old Wistar rats and Balb/c mice
Dosage:	0.3-3 mg/kg
Administration:	Single administration; orally
Result:	The plasma levels of IL-1β, IL-6, TNF-α, MCP-1, and aminotransferases (ALT and AST) were significantly increased.

分子式

C₁₉H₂₀N₆O₄^.HCl

分子量

432.86

CAS号

1287665-60-4

中文名称

AS 2444697

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

2-8°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : ≥ 12.5 mg/mL (28.88 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3102 mL	11.5511 mL	23.1022 mL
5 mM	0.4620 mL	2.3102 mL	4.6204 mL
10 mM	0.2310 mL	1.1551 mL	2.3102 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 (sealed storage, away from moisture)。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% saline

Solubility: ≥ 1.25 mg/mL (2.89 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (2.89 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO → 90% (20% SBE-β-CD in saline)

Solubility: ≥ 1.25 mg/mL (2.89 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (2.89 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO → 90% corn oil

Solubility: ≥ 1.25 mg/mL (2.89 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (2.89 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

纯度： ≥95%

Data Sheet

产品使用指南

[1]. JohnHynesJr, et al. Chapter Nine - Advances in the Discovery of Small-Molecule IRAK4 Inhibitors. Annu Rep Med Chem. 2014 (49):117-133.

[2]. Mitsuhiro Kondo, et al. Renoprotective effects of novel interleukin-1 receptor-associated kinase 4 inhibitor AS2444697 through anti-inflammatory action in 5/6 nephrectomized rats. Naunyn Schmiedebergs Arch Pharmacol. 2014 Oct;387(10):909-19.

The molarity calculator equation

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

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

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

浓度

体积

浓度

体积

重置计算

动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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The molarity calculator equation

The dilution calculator equation

动物实验计算换算器