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MedKoo Cat#: 130443 | Name: Nerandomilast
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Nerandomilast, also known as BI-1015550, is a potent PDE4 inhibitor that displays anti-inflammatory activity. BI 1015550 shows a preferential enzymatic inhibition of PDE4B. In vitro, 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.

Chemical Structure

Nerandomilast
Nerandomilast
CAS#1423719-30-5

Theoretical Analysis

MedKoo Cat#: 130443

Name: Nerandomilast

CAS#: 1423719-30-5

Chemical Formula: C20H25ClN6O2S

Exact Mass: 448.1448

Molecular Weight: 448.97

Elemental Analysis: C, 53.50; H, 5.61; Cl, 7.90; N, 18.72; O, 7.13; S, 7.14

Price and Availability

Size Price Availability Quantity
10mg USD 250.00 2 Weeks
25mg USD 450.00 2 Weeks
50mg USD 750.00 2 Weeks
100mg USD 1,250.00 2 Weeks
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Related CAS #
No Data
Synonym
BI-1015550; BI1015550; BI 1015550; I5DGT51IB8, nerandomilast
IUPAC/Chemical Name
(R)-2-(4-(5-chloropyrimidin-2-yl)piperidin-1-yl)-4-((1-(hydroxymethyl)cyclobutyl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide
InChi Key
UHYCLWAANUGUMN-SSEXGKCCSA-N
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
SMILES Code
OCC1(NC2=C3C(CC[S@]3=O)=NC(N4CCC(C5=NC=C(Cl)C=N5)CC4)=N2)CCC1
Appearance
To be determined
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
The anti-inflammatory and immunomodulatory abilities of oral selective phosphodiesterase 4 (PDE4) inhibitors enabled the approval of roflumilast and apremilast for use in chronic obstructive pulmonary disease and psoriasis/psoriatic arthritis, respectively.

Preparing Stock Solutions

The following data is based on the product molecular weight 448.97 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Sofia C, Comes A, Sgalla G, Richeldi L. An update on emerging drugs for the treatment of idiopathic pulmonary fibrosis: a look towards 2023 and beyond. Expert Opin Emerg Drugs. 2023 Dec;28(4):283-296. doi: 10.1080/14728214.2023.2281416. Epub 2023 Dec 26. PMID: 37953604. 2: Maher TM, Assassi S, Azuma A, Cottin V, Hoffmann-Vold AM, Kreuter M, Oldham JM, Richeldi L, Valenzuela C, Wijsenbeek MS, Coeck C, Schlecker C, Voss F, Wachtlin D, Martinez FJ. Design of a phase III, double-blind, randomised, placebo-controlled trial of BI 1015550 in patients with progressive pulmonary fibrosis (FIBRONEER-ILD). BMJ Open Respir Res. 2023 Sep;10(1):e001580. doi: 10.1136/bmjresp-2022-001580. PMID: 37709661; PMCID: PMC10503394. 3: Richeldi L, Azuma A, Cottin V, Kreuter M, Maher TM, Martinez FJ, Oldham JM, Valenzuela C, Gordat M, Liu Y, Stowasser S, Zoz DF, Wijsenbeek MS. Design of a phase III, double-blind, randomised, placebo-controlled trial of BI 1015550 in patients with idiopathic pulmonary fibrosis (FIBRONEER-IPF). BMJ Open Respir Res. 2023 Aug;10(1):e001563. doi: 10.1136/bmjresp-2022-001563. PMID: 37597969; PMCID: PMC10441083. 4: Herrmann FE, Hesslinger C, Wollin L, Nickolaus P. Corrigendum: BI 1015550 is a PDE4B inhibitor and a clinical drug candidate for the oral treatment of idiopathic pulmonary fibrosis. Front Pharmacol. 2023 May 30;14:1219760. doi: 10.3389/fphar.2023.1219760. Erratum for: Front Pharmacol. 2022 Apr 20;13:838449. PMID: 37324497; PMCID: PMC10263364. 5: Sgalla G, Simonetti J, Cortese S, Richeldi L. BI 1015550: an investigational phosphodiesterase 4B (PDE4B) inhibitor for lung function decline in idiopathic pulmonary fibrosis (IPF). Expert Opin Investig Drugs. 2023 Jan;32(1):17-23. doi: 10.1080/13543784.2023.2173061. Epub 2023 Feb 3. PMID: 36693635. 6: Richeldi L, Azuma A, Cottin V, Hesslinger C, Stowasser S, Valenzuela C, Wijsenbeek MS, Zoz DF, Voss F, Maher TM. Plain language summary: Clinical study of BI 1015550 as a potential treatment for idiopathic pulmonary fibrosis. J Comp Eff Res. 2022 Dec 20;12(1):e220142. doi: 10.2217/cer-2022-0142. Epub ahead of print. PMID: 36537726; PMCID: PMC10288937. 7: Maher TM, Schlecker C, Luedtke D, Bossert S, Zoz DF, Schultz A. Phase I studies of BI 1015550, a preferential phosphodiesterase 4B inhibitor, in healthy males and patients with idiopathic pulmonary fibrosis. ERJ Open Res. 2022 Oct 24;8(4):00240-2022. doi: 10.1183/23120541.00240-2022. PMID: 36299369; PMCID: PMC9589333. 8: Richeldi L, Azuma A, Cottin V, Hesslinger C, Stowasser S, Valenzuela C, Wijsenbeek MS, Zoz DF, Voss F, Maher TM; 1305-0013 Trial Investigators. Trial of a Preferential Phosphodiesterase 4B Inhibitor for Idiopathic Pulmonary Fibrosis. N Engl J Med. 2022 Jun 9;386(23):2178-2187. doi: 10.1056/NEJMoa2201737. Epub 2022 May 15. PMID: 35569036. 9: Herrmann FE, Hesslinger C, Wollin L, Nickolaus P. BI 1015550 is a PDE4B Inhibitor and a Clinical Drug Candidate for the Oral Treatment of Idiopathic Pulmonary Fibrosis. Front Pharmacol. 2022 Apr 20;13:838449. doi: 10.3389/fphar.2022.838449. Erratum in: Front Pharmacol. 2023 May 30;14:1219760. PMID: 35517783; PMCID: PMC9065678.