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

Nerandomilast dihydrate  (Synonyms: BI 1015550 dihydrate)

Cat. No.: HY-153192A
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Nerandomilast (BI 1015550) dihydrate is an orally active inhibitor of PDE4B with an IC50 value of 7.2 nM. Nerandomilast (dihydrate) has good safety and potential applications in inflammation, allergic diseases, pulmonary fibrosis, and chronic obstructive pulmonary disease (COPD).

For research use only. We do not sell to patients.

Nerandomilast dihydrate Chemical Structure

Nerandomilast dihydrate Chemical Structure

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Description

Nerandomilast (BI 1015550) dihydrate is an orally active inhibitor of PDE4B with an IC50 value of 7.2 nM. Nerandomilast (dihydrate) has good safety and potential applications in inflammation, allergic diseases, pulmonary fibrosis, and chronic obstructive pulmonary disease (COPD)[1][2].

In Vitro

Nerandomilast (dihydrate) inhibits Lipopolysaccharides (HY-D1056) induced TNF-α release and Phytohemagglutinin P (HY-N7038A) induced IL-2 release in human PBMCs with IC50 values of 35 nM and 9 nM, respectively[2].
Nerandomilast (dihydrate) inhibits TNF-α release in rat whole blood with an IC50 value of 91 nM[2].

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

In Vivo

Nerandomilast (dihydrate) (Example 2) (0, 0.3, 1.0 and 3.0 mg/kg; p.o.; single dose) weakens intestinal transport in rats at 1.0 mg/kg without significantly affecting body weight[1].
Nerandomilast (dihydrate) prevents inflammation in rat lung tissue with an ED50 value of 0.1 mg/kg[1].
Nerandomilast (dihydrate) (0.01, 0.1 and 1.0 mg/kg; p.o.; single dose) reduces the Lipopolysaccharides (HY-D1056) induced TNF-α release with dose-dependent manner in mice plasma[2].
Nerandomilast (dihydrate) (0.1, 0.3 and 1.0 mg/kg; p.o.; single dose) inhibits lipopolysaccharides induced neutrophil entry into bronchoalveolar lavage fluid of male Suncus Murinus and Wistar rats[2].
Nerandomilast (dihydrate) (2.5 mg/kg and 12.5 mg/kg; p.o.; twice daily for 6 d) effectively improves the damage of Bleomycin (HY-108345) to mice[2].

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

Animal Model: Rats[1].
Dosage: 0, 0.3, 1.0 and 3.0 mg/kg.
Administration: Oral gavage; single dose.
Result: Had minimal toxic and side effects on the intestines and stomach of rats, demonstrating biosafety.
Animal Model: Male Suncus Murinus and Wistar rats; mice[2].
Dosage: 0.01, 0.1, 0.3, 1.0, 2.5 or 12.5 mg/kg.
Administration: Oral gavage; single dose or twice daily for 6 d.
Result: Effectively improved inflammation in lung tissue and reduced the pro-inflammatory factor TNF-α release.
Clinical Trial
Molecular Weight

485.00

Formula

C20H29ClN6O4S

SMILES

O=[S@]1C2=C(CC1)N=C(N3CCC(CC3)C4=NC=C(C=N4)Cl)N=C2NC5(CO)CCC5.O.O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Nerandomilast dihydrate Related Classifications

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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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Product Name:
Nerandomilast dihydrate
Cat. No.:
HY-153192A
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