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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 |
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| MR-L2
MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4), activates representative PDE4 long-isoform variants (PDE4A4, PDE4B1, PDE4C3, PDE4D5). MR-L2 suppresses PGE2-induced MDCK cell cyst formation with an EC50 of 1.2 μM. |
| MMPX
MMPX is a potent PDE1 inhibitor. |
| T-0156
T-0156 is a potent and selective phosphodiesterase type 5 (PDE5) inhibitor. |
| TPN171
TPN171 is a potent, selective and oral bioavailable inhibitor of phosphodiesterase type 5 (PDE5) with an IC50 of 0.62 nM, being developed for the treatment of pulmonary arterial hypertension (PAH). |
| Mesopram
Mesopram (Daxalipram) is an orally active phosphodiesterase (PDE) 4 inhibitor. |
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