A PDE4B inhibitor
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Nerandomilast

Item No. 44975

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[[(5R)-2-[4-(5-chloro-2-pyrimidinyl)-1-piperidinyl]-6,7-dihydro-5-oxidothieno[3,2-d]pyrimidin-4-yl]amino]-cyclobutanemethanol
CAS Number
1423719-30-5
Synonyms
  • BI-1015550
Molecular Formula
C20H25ClN6O2S
Formula Weight
449.0
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile:Water (1:1): Sparingly soluble: 1-10 mg/ml
SMILES
O=[S@@]1CCC2=NC(N3CCC(CC3)C4=NC=C(C=N4)Cl)=NC(NC5(CO)CCC5)=C21
InChi Code
InChI=1S/C20H25ClN6O2S/c21-14-10-22-17(23-11-14)13-2-7-27(8-3-13)19-24-15-4-9-30(29)16(15)18(25-19)26-20(12-28)5-1-6-20/h10-11,13,28H,1-9,12H2,(H,24,25,26)/t30-/m1/s1
InChi Key
UHYCLWAANUGUMN-SSEXGKCCSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $67

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    10 mg

    $121

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    25 mg

    $251

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    50 mg

    $469

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    Cayman Chemical
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    Product Description

    Nerandomilast is an inhibitor of phosphodiesterase 4B (PDE4B; IC50 = 0.01 µM).1 It is selective for PDE4B over PDE4A, PDE4C, and PDE4D (IC50s = 0.248, 8.7, and 0.091 µM, respectively), PDE7A, PDE3A, PDE1C, and PDE9A (IC50s = 14, 120, 46, and >100 µM, respectively), and does not inhibit PDE2A, PDE5, or PDE6. Nerandomilast inhibits LPS-induced TNF-α release and phytohemagglutinin P-induced IL-2 release in isolated human peripheral blood mononuclear cells (PBMCs; IC50s = 0.035 and 0.009 µM, respectively). It exhibits a lower emetic potential than roflumilast (Item No. 15141) in Asian house shrews. Nerandomilast (12.5 mg/kg) reduces decreases in forced vital capacity and static lung volume in a mouse model of pulmonary fibrosis bleomycin-induced. Formulations containing nerandomilast have been used in the treatment of idiopathic pulmonary fibrosis.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Herrmann, F.E., Hesslinger, C., Wollin, L., et al. BI 1015550 is a PDE4B inhibitor and a clinical drug candidate for the oral treatment of idiopathic pulmonary fibrosis. Front. Pharmacol. 13, 838449 (2022).