1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. Lirimilast

Lirimilast  (Synonyms: BAY 19-8004)

製品番号: HY-19672 純度: 98.69%
COA 取扱説明書 Technical Support

Lirimilast (BAY 19-8004) is a potent, selective and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 value of 49 nM. Lirimilast can be used for the treatment of asthma or chronic obstructive pulmonary disease (COPD). Lirimilast has potently anti-inflammatory properties.

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Lirimilast

Lirimilast 構造式

CAS 番号 : 329306-27-6

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 616 在庫あり
Solution
10 mM * 1 mL in DMSO USD 616 在庫あり
Solid
1 mg $224 在庫あり
5 mg $560 在庫あり
10 mg $950 在庫あり
25 mg $1710 在庫あり
50 mg $2565 在庫あり
100 mg $3848 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Phosphodiesterase (PDE) アイソフォーム固有の製品をすべて表示:

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  • 純度とドキュメンテーション

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製品説明

Lirimilast (BAY 19-8004) is a potent, selective and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 value of 49 nM. Lirimilast can be used for the treatment of asthma or chronic obstructive pulmonary disease (COPD). Lirimilast has potently anti-inflammatory properties[1][2].

IC50 & Target[2]

PDE4

42 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
Sf21 IC50
>10 μM
Compound: BAY-198004
Inhibition of His-tagged catalytic domain Trypanosoma brucei brucei PDEB1 expressed in baculovirus infected insect Sf21 cells
Inhibition of His-tagged catalytic domain Trypanosoma brucei brucei PDEB1 expressed in baculovirus infected insect Sf21 cells
[PMID: 22023548]
Sf21 IC50
>10 μM
Compound: BAY-198004
Inhibition of His-tagged catalytic domain Trypanosoma brucei brucei PDEB2 expressed in baculovirus infected insect Sf21 cells
Inhibition of His-tagged catalytic domain Trypanosoma brucei brucei PDEB2 expressed in baculovirus infected insect Sf21 cells
[PMID: 22023548]
体外実験

In PDE4 assays Lirimilast (BAY 19-8004) is reported to be 5-fold more potent than Cilomilast and equipotent with CDP-840 using freshly prepared PDE4 from human PMNL[1].

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

体内実験

Since Lirimilast (BAY 19-8004) is orally active in the guinea-pig at 3 mg/kg and, more critically, in primates at 0.1 mg/kg/day it appears to have a good therapeutic ratio. In addition Lirimilast is found to be 3-fold more potent than Cilomilast when compared in a rat model of lung neutrophilic inflammation[2].

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

分子量

443.26

分子式

C17H12Cl2N2O6S

CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(N)NC1=C(C(C2=CC=C(Cl)C=C2Cl)=O)OC3=CC(OS(=O)(C)=O)=CC=C13

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (225.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2560 mL 11.2801 mL 22.5601 mL
5 mM 0.4512 mL 2.2560 mL 4.5120 mL
10 mM 0.2256 mL 1.1280 mL 2.2560 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始)

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In Vivo Dissolution Calculator
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純度とドキュメンテーション

純度: 98.69%

参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2560 mL 11.2801 mL 22.5601 mL 56.4003 mL
5 mM 0.4512 mL 2.2560 mL 4.5120 mL 11.2801 mL
10 mM 0.2256 mL 1.1280 mL 2.2560 mL 5.6400 mL
15 mM 0.1504 mL 0.7520 mL 1.5040 mL 3.7600 mL
20 mM 0.1128 mL 0.5640 mL 1.1280 mL 2.8200 mL
25 mM 0.0902 mL 0.4512 mL 0.9024 mL 2.2560 mL
30 mM 0.0752 mL 0.3760 mL 0.7520 mL 1.8800 mL
40 mM 0.0564 mL 0.2820 mL 0.5640 mL 1.4100 mL
50 mM 0.0451 mL 0.2256 mL 0.4512 mL 1.1280 mL
60 mM 0.0376 mL 0.1880 mL 0.3760 mL 0.9400 mL
80 mM 0.0282 mL 0.1410 mL 0.2820 mL 0.7050 mL
100 mM 0.0226 mL 0.1128 mL 0.2256 mL 0.5640 mL
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  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
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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Inquiry Information

製品名:
Lirimilast
製品番号:
HY-19672
数量:
MCE 日本正規代理店: