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Nerandomilast (BI 1015550) is a novel, orally active phosphodiesterase 4B (PDE4B) inhibitor (IC50 = 7.2 nM) with anti-fibrotic and anti-inflammatory effects.
In vitro, Nerandomilast (BI 1015550) inhibits lipopolysaccharide (LPS)-induced tumor necrosis factor-α (TNF-α) and phytohemagglutinin-induced interleukin-2 synthesis in human peripheral blood mononuclear cells, as well as LPS-induced TNF-α synthesis in human and rat whole blood.
In vivo, oral BI 1015550 shows potent anti-inflammatory activity in mice by inhibiting LPS-induced TNF-α synthesis ex vivo and in Suncus murinus by inhibiting neutrophil influx into bronchoalveolar lavage fluid stimulated by nebulized LPS.
Nerandomilast (BI 1015550) inhibited transforming growth factor-β-stimulated myofibroblast transformation and the mRNA expression of various extracellular matrix proteins, as well as basic fibroblast growth factor plus interleukin-1β-induced cell proliferation.
| Molecular Weight | 448.97 |
| Formula | C20H25ClN6O2S |
| CAS Number | 1423719-30-5 |
| Solubility (25°C) | DMSO 6 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PDE Products |
|---|
| GSK256066
GSK256066 is a selective phosphodiesterase 4 (PDE4)inhibitor with an IC50 of 3.2 pM. *The compound is unstable in solutions, freshly prepared is recommended |
| BAY-60-7550
BAY-60-7550 is a potent PDE2 inhibitor with IC50 values of 2.0 nM (bovine) and 4.7 nM (human). |
| Roflumilast
Roflumilast (APTA-2217; BYK 20869; B9302-107) is a novel and selective, long-acting inhibitor of phosphodiesterase 4 (PDE-4). |
| Piclamilast
Piclamilast (RP 73401) is a potent and selective inhibitor of phosphodiesterase (PDE) 4. |
| Apremilast
Apremilast is a novel, orally available small molecule inhibitor of PDE4 with IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM. |
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