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Nerandomilast (BI 1015550) is an orally active PDE4B inhibitor with IC50 of 7.2 nM. BI 1015550 has potential applications in inflammation, allergic diseases, pulmonary fibrosis and chronic obstructive pulmonary disease (COPD) with a good safety profile.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $59 | In Stock | |
5 mg | $127 | In Stock | |
10 mg | $197 | In Stock | |
25 mg | $397 | In Stock | |
50 mg | $589 | In Stock | |
100 mg | $843 | In Stock |
Description | Nerandomilast (BI 1015550) is an orally active PDE4B inhibitor with IC50 of 7.2 nM. BI 1015550 has potential applications in inflammation, allergic diseases, pulmonary fibrosis and chronic obstructive pulmonary disease (COPD) with a good safety profile. |
Targets&IC50 | PDE4B:7.2 nM |
In vitro | METHODS: Rats were treated with Nerandomilast (BI 1015550) (0.0001-100mM) to study its effect on LPS-stimulated TNF-α release in rat whole blood. RESULTS BI 1015550 completely inhibited TNF-α release in rat whole blood with an IC50 value of 91 nM; high concentrations of BI 1015550 resulted in a concentration-dependent four-fold increase in IL-6 in rats. [1] |
In vivo | METHODS: Rats were treated with Nerandomilast (BI 1015550) (0.01, 0.1, 1, 3 mg/kg, oral) to study its effect on LPS-stimulated TNF-α release in rat whole blood. RESULTS BI 1015550 at a dose of 3 mg/kg inhibited 93% of TNF-α release. The final experimental result showed that the dose of BI 1015550 that caused half-maximal inhibition (ED50) of LPS-induced TNF-α release was 0.04 mg/kg. [1] |
Molecular Weight | 448.97 |
Formula | C20H25ClN6O2S |
Cas No. | 1423719-30-5 |
Smiles | N(C1=C2C(=NC(=N1)N3CCC(CC3)C=4N=CC(Cl)=CN4)CCS2=O)C5(CO)CCC5 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | DMSO: 4.49 mg/mL (10 mM) | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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