2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. Lotamilast

Lotamilast  (Synonyms: RVT-501; E6005)

目录号: HY-12740 纯度: ≥98.0%
COA 产品使用指南

摩尔计算器

Lotamilast (RVT-501; E6005) 是选择性的磷酸二酯酶4 (PDE4) 抑制剂，IC50 值为2.8 nM。

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Lotamilast Chemical Structure

Lotamilast Chemical Structure

CAS No. : 947620-48-6

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥936
In-stock
1 mg ￥502
In-stock
5 mg ￥900
In-stock
10 mg ￥1440
In-stock
50 mg ￥4300
In-stock
100 mg ￥6000
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Lotamilast 相关抗体

Top Publications Citing Use of Products

查看 Phosphodiesterase (PDE) 亚型特异性产品:

查看所有亚型
PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Lotamilast (RVT-501; E6005) is a selective phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 2.8 nM.

IC50 & Target

IC50: 2.8 nM (human PDE4)[1]
体外研究
(In Vitro)

Lotamilast potently and selectively inhibits human PDE4 activity with an IC50 of 2.8 nM and suppresses the production of various cytokines from human lymphocytes and monocytes with IC50 values ranging from 0.49 to 3.1 nM[1].

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

Lotamilast 相关抗体:
体内研究
(In Vivo)

Lotamilast is currently in phase 2 development for patients with mild-to-moderate atopic dermatitis. In mice models, the topical application of Lotamilast produces an immediate antipruritic effect as well as an anti-inflammatory effect with reduced expression of cytokines/adhesion molecules. On the basis of these observed effects, topical RVT-501 ameliorates the appearance of atopic dermatitis-like skin lesions in two types of AD models, hapten- and mite-elicited models, exhibiting inhibitory effects comparable to that of tacrolimus[1]. A single topical application of Lotamilast significantly inhibits spontaneous scratching during 1–2 h after application in mice with chronic dermatitis; the inhibition is partial and similar between 0.01% and 0.03%. Topical application of 0.03% Lotamilast to the rostral back significantly inhibits the increased activity of the cutaneous nerve in mice with chronic dermatitis. The cutaneous concentration of cAMP is significantly decreased in mice with chronic dermatitis, and this decrease is reversed by topical Lotamilast application[2].

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

472.49

Formula

C26H24N4O5
CAS 号
性状

固体

颜色

Light yellow to yellow

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 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 25 mg/mL (52.91 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 2.1164 mL 10.5822 mL 21.1645 mL
5 mM 0.4233 mL 2.1164 mL 4.2329 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 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

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

  • 方案 一

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

    Solubility: 2.5 mg/mL (5.29 mM); 悬浊液; 超声助溶

    此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 25.0 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。

    20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
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

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献
Kinase Assay
[1]

PDE isoenzyme activities are quantified by measuring the formation of [3H]5′-AMP or [[3H]5′-GMP from [[3H]cAMP or [[3H]cGMP using an enzyme isolated from bovine brain (for PDE1), differentiated U-937 cells (for PDE2), human platelets (for PDE3 and PDE5), and U-937 cells (for PDE4). The test compounds (RVT-501), reference compounds, or vehicle (water) is added to a reaction buffer. The reaction is initialized by addition of the enzyme, and the mixture is incubated for 60 minutes at 22°C. After incubation, the reaction is stopped by heating the plate to 60°C for 3 minutes, after which time scintillation proximity assay beads are added. After 20 minutes of shaking at 22°C, the amount of [[3H]5′-AMP or [[3H]5′-GMP is quantified with a scintillation counters[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice: Lotamilast is applied to the hair-clipped rostral back. Observation of hind-paw scratching and electrophysiological recording of the cutaneous nerve branch are conducted. The effects of topical application of E6005 are evaluated 1 h after application, because topical application of the vehicle elicited hind-paw scratching for 40 min. The cutaneous concentration of cAMP is measured by enzyme immunoassay[2].

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

Lotamilast 相关分类

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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1164 mL 10.5822 mL 21.1645 mL 52.9112 mL
5 mM 0.4233 mL 2.1164 mL 4.2329 mL 10.5822 mL
10 mM 0.2116 mL 1.0582 mL 2.1164 mL 5.2911 mL
15 mM 0.1411 mL 0.7055 mL 1.4110 mL 3.5274 mL
20 mM 0.1058 mL 0.5291 mL 1.0582 mL 2.6456 mL
25 mM 0.0847 mL 0.4233 mL 0.8466 mL 2.1164 mL
30 mM 0.0705 mL 0.3527 mL 0.7055 mL 1.7637 mL
40 mM 0.0529 mL 0.2646 mL 0.5291 mL 1.3228 mL
50 mM 0.0423 mL 0.2116 mL 0.4233 mL 1.0582 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.

Keywords:

Lotamilast947620-48-6RVT-501 E6005RVT501RVT 501E6005E 6005E-6005Phosphodiesterase (PDE)Inhibitorinhibitorinhibit

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