LIRIMILAST
- Product Name
- LIRIMILAST
- CAS No.
- 329306-27-6
- Chemical Name
- LIRIMILAST
- Synonyms
- LIRIMILAST;BAY 19-8004;Lirimilast/BAY 19-8004;BAY 19-8004 - Lirimilast;2-(2,4-Dichlorobenzoyl)-3-ureidobenzofuran-6-yl methanesulfonate;Urea,[2-(2,4-dichlorobenzoyl)-6-[(methylsulfonyl)oxy]-3-benzofuranyl]-;UREA, N-[2-(2,4-DICHLOROBENZOYL)-6-[(METHYLSULFONYL)OXY]-3-BENZOFURANYL]-;METHANESULFONIC ACID 2-(2,4-DICHLORO-BENZOYL)-3-UREIDO-BENZOFURAN-6-YL ESTER
- CBNumber
- CB02451336
- Molecular Formula
- C17H12Cl2N2O6S
- Formula Weight
- 443.26
- MOL File
- 329306-27-6.mol
LIRIMILAST Property
- Boiling point:
- 663.2±55.0 °C(Predicted)
- Density
- 1.619±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- pka
- 12.33±0.30(Predicted)
- form
- Solid
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- Axon1178
- Product name
- BAY19-8004-Lirimilast
- Purity
- 98%
- Packaging
- 5mg
- Price
- $148.5
- Updated
- 2021/12/16
- Product number
- API0004703
- Product name
- BAY 19-8004
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $320.1
- Updated
- 2021/12/16
LIRIMILAST Chemical Properties,Usage,Production
Uses
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].
in vivo
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].
IC 50
PDE4: 42 nM (IC50)
References
[1] Grootendorst DC, et al. Efficacy of the novel phosphodiesterase-4 inhibitor BAY 19-8004 on lung function and airway inflammation in asthma and chronic obstructive pulmonary disease (COPD). Pulm Pharmacol Ther. 2003;16(6):341-7. DOI:10.1016/S1094-5539(03)00090-7
[2] Peter Norman. PDE4 inhibitors: sustained patenting activity as leading drugs near the market. Exp. Opin. Ther. Patents (2000) 10(9):1415-1427.