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  2. Immunology/Inflammation
  3. FLAP
  4. AM103

AM 103 是具有選擇性的，有效的 FLAP 抑制劑，IC50 值為 4.2 nM。

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AM103 Chemical Structure

AM103 Chemical Structure

CAS No. : 1147872-22-7

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥6115
In-stock
1 mg ￥2000
In-stock
5 mg ￥4400
In-stock
10 mg 現(xiàn)貨 詢價
25 mg 現(xiàn)貨 詢價
50 mg 現(xiàn)貨 詢價
100 mg 現(xiàn)貨 詢價
200 mg   詢價  
500 mg   詢價  

* Please select Quantity before adding items.

Other Forms of AM103:

  • 生物活性

  • 實驗參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

AM 103 is a potent and selective FLAP inhibitor, with an IC50 value of 4.2 nM.

IC50 & Target

IC50: 4.2 nM (FLAP)[1]
體外研究
(In Vitro)

AM 103 has an IC50 value of 349 nM in the human blood LTB4 inhibition assay. AM 103 has an excellent CYP profile against the 5 most common CYP isoforms with IC50 values greater than 30 μM for CYP2D6 and >50 μM for CYPs 3A4, 2C9 2C19, and 1A2[1]. AM103 is a novel, potent, and selective FLAP inhibitor with IC50 values of 350, 113, and 117 nM against human, rat, and mouse whole-blood ionophore-stimulated LTB4 production, respectively[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

AM 103 has high bioavailability (64%), low clearance (2.9 mL/min/kg), low volume of distribution (0.41 L/kg), and a long i.v. half-life (5.2 h) in dogs. AM 103 (10 mg/kg q.i.d.) inhibits the increase in CysLTs and EPO by approximately 60%, and IL-5 levels are reduced to the concentrations obtained following saline treatment alone in mice[1]. AM103 (1 mg/kg, p.o.) displays >50% inhibition for up to 6 h with a calculated EC50 of appr 60 nM, in a rat ex vivo whole-blood calcium ionophore-induced LTB4 assay. AM 103 inhibits LTB4 and cysteinyl leukotriene (CysLT) production with ED50 values of 0.8 and 1 mg/kg, respectively, when rat lung is challenged in vivo with calcium ionophore. In this model, the EC50 derived from plasma AM103 is appr 330 nM for inhibition of both LTB4 and CysLT. In a model of chronic lung inflammation using ovalbumin-primed and challenged BALB/c mice, AM103 reduces the concentrations of eosinophil peroxidase, CysLTs, and interleukin-5 in the bronchoalveolar lavage fluid. Finally, AM 103 increases survival time in mice exposed to a lethal intravenous injection of platelet-activating factor[2].

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

631.76

Formula

C36H38N3NaO4S
CAS 號
性狀

固體

顏色

Off-white to light yellow

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式

4°C, sealed storage, away from moisture and light

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

溶解性數(shù)據(jù)
細胞實驗： 

DMSO 中的溶解度 : 200 mg/mL (316.58 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 1.5829 mL 7.9144 mL 15.8288 mL
5 mM 0.3166 mL 1.5829 mL 3.1658 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物實驗：

請根據(jù)您的 實驗動物和給藥方式 選擇適當?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 5 mg/mL (7.91 mM); 懸濁液; 超聲助溶

    此方案可獲得 5 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

    以 1 mL 工作液為例，取 100 μL 50.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
  • 方案 二

    請依序添加每種溶劑： 10% DMSO    90% Corn Oil

    Solubility: ≥ 5 mg/mL (7.91 mM); 澄清溶液

    此方案可獲得 ≥ 5 mg/mL（飽和度未知）的澄清溶液，此方案實驗周期在半個月以上的動物實驗酌情使用。

    以 1 mL 工作液為例，取 100 μL 50.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中，混合均勻。

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
計算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。

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

您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上，請謹慎選擇該方案。
請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料
參考文獻
Kinase Assay
[1]

Packed human polymorphonuclear cell pellets (1.8×109 cells) are resuspended, lysed, and 75,000g membranes. The 75,000g pelleted membranes are resuspended in a Tris buffer (50 mM Tris HCl, pH 7.4, 1 mM EDTA, 1 mM DTT, and 30% glycerol) to yield a protein concentration of appr 4 mg/mL. Then, 2.5 μg of membrane protein per well is added to 96-well deep well plates containing Tris-Tween buffer (100 mM Tris HCl, pH 7.4, 100 mM NaCl, 1 mM EDTA, 0.5 mM DTT, 5% glycerol, and 0.05% Tween-20) and appr 30,000 cpm of [3H]-3-[5-(pyrid-2-ylmethoxy)-3-tert-butylthio-1-benzyl-indol-2-yl]-2,2-dimethylpropionic acid and test compound in a total volume of 100 μL and incubated for 60 min at room temperature. The reactions are then harvested onto GF/B filter plates using a Brandel 96-tip harvester and washed 3× with 1 mL of ice-cold Tris-Tween buffer. The filter plates are dried, the bottoms sealed, and 100 μL of scintillant added. The plates are incubated for 1 h before reading on Perkin-Elmer TopCount. Specific binding is defined as total radioactive binding minus nonspecific binding in the presence of 10 μM MK886. IC50 values are determined using Graphpad prism analysis of drug titration curves.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Compounds are administered intravenously (i.v.) (2 mg/kg) to two or three male rats (fasted overnight) as a solution in PEG400/ethanol/water (40/10/50, v/v/v) via a bolus injection into the jugular vein (2 mg/mL; 1 mL/kg) and orally (p.o.) (10 mg/kg) to two or three male rats as a suspension in 0.5% methylcellulose via an oral gavage to the stomach (3.33 mg/mL; 3 mL/kg). Blood samples (approximately 300 μL) are taken from each rat via the jugular vein cannula at time intervals up to 24 h postdose (8?9 samples per animal). After each sample, the cannula is flushed with an equivalent volume of heparinized saline (0.1 mL at 40 units/mL). Plasma samples, prepared by centrifugation of whole blood, are stored frozen (?80°C) prior to analysis.

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

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C儲存時，請在6個月內(nèi)使用，-20°C儲存時，請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5829 mL 7.9144 mL 15.8288 mL 39.5720 mL
5 mM 0.3166 mL 1.5829 mL 3.1658 mL 7.9144 mL
10 mM 0.1583 mL 0.7914 mL 1.5829 mL 3.9572 mL
15 mM 0.1055 mL 0.5276 mL 1.0553 mL 2.6381 mL
20 mM 0.0791 mL 0.3957 mL 0.7914 mL 1.9786 mL
25 mM 0.0633 mL 0.3166 mL 0.6332 mL 1.5829 mL
30 mM 0.0528 mL 0.2638 mL 0.5276 mL 1.3191 mL
40 mM 0.0396 mL 0.1979 mL 0.3957 mL 0.9893 mL
50 mM 0.0317 mL 0.1583 mL 0.3166 mL 0.7914 mL
60 mM 0.0264 mL 0.1319 mL 0.2638 mL 0.6595 mL
80 mM 0.0198 mL 0.0989 mL 0.1979 mL 0.4946 mL
100 mM 0.0158 mL 0.0791 mL 0.1583 mL 0.3957 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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產(chǎn)品名稱：
AM103
目錄號：
HY-14163
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