Lotamilast - CAS:947620-48-6

您当前的位置：

Lotamilast (Synonyms:RVT-501; E6005)

目录号 : KM7049 CAS No. : 947620-48-6 纯度 : ≥98%

Data Sheet 产品使用指南

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。

规格	价格	是否有货
2mg		In-stock
5mg		In-stock
10mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

查看所有商品（2）

加入购物车大包装询价

Other Forms of Rapamycin:

Kgp-IN-1 hydrochloride In-stock
Ginkgolide A In-stock
Ginkgetin In-stock
VKGILS-NH2 In-stock
7,3',4'-Tri-O-methylluteolin In-stock

KKL Med 的所有产品和服务仅用于科学研究，不能被用于人体，兽医，我们也不向个人提供产品和服务。

生物活性

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

体外研究

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.

体内研究

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. 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.

分子式

C₂₆H₂₄N₄O₅

分子量

472.49

CAS号

947620-48-6

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 (52.91 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1164 mL	10.5822 mL	21.1645 mL
5 mM	0.4233 mL	2.1164 mL	4.2329 mL
10 mM	0.2116 mL	1.0582 mL	2.1164 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。

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 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (5.29 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (5.29 mM) 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。

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)

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

Other Forms of Rapamycin:

KKL 顾客使用本产品发表的 0 篇科研文献

The molarity calculator equation

The dilution calculator equation