AZD7986

Catalog No: 20648

CAS Number: 1802148-05-5

Purity: 98% Min.

Brensocatib, also known as AZD7986, INS 1007, is an oral reversible inhibitor of dipeptidyl peptidase 1 (DPP-1), an enzyme responsible for the activation of neutrophil serine proteases. AZD 7986 inhibits activation of the DPP-1 targets neutrophil elastase, proteinase 3, and cathepsin G in human bone marrow-derived CD34+ neutrophil progenitor cells (IC50s = 61.7, 208.9, and 114.8 nM, respectively). AZD7986 inhibits whole blood NE activity in an exposure-dependent, indirect manner-consistent with in vitro and preclinical predictions.

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Chemical Information

Name	AZD7986
Iupac Chemical Name	(S)-N-((S)-1-cyano-2-(4-(3-methyl-2-oxo-2,3-dihydrobenzo[d]oxazol-5-yl)phenyl)ethyl)-1,4-oxazepane-2-carboxamide
Synonyms	AZD7986; AZD-7986; AZD 7986; INS 1007; INS-1007; INS1007, Brensocatib
Molecular Formula	C23H24N4O4
Molecular Weight	420.46
Smile	N#C[C@H](CC1=CC=C(C2=CC=C(OC(N3C)=O)C3=C2)C=C1)NC([C@H]4OCCCNC4)=O
InChiKey	AEXFXNFMSAAELR-RXVVDRJESA-N
InChi	InChI=1S/C23H24N4O4/c1-27-19-12-17(7-8-20(19)31-23(27)29)16-5-3-15(4-6-16)11-18(13-24)26-22(28)21-14-25-9-2-10-30-21/h3-8,12,18,21,25H,2,9-11,14H2,1H3,(H,26,28)/t18-,21-/m0/s1
CAS Number	1802148-05-5
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Formulation	Solid powder
Purity	98% Min.
Storage	Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility	Soluble in DMSO
Handling
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.
HS Code

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Targets
Mechanism
Cell study
Animal study
Clinical study

1: Sun L, Han X, Egeblad M. Isolation of mouse mammary carcinoma-derived macrophages and cancer cells for co-culture assays. STAR Protoc. 2022 Nov 10;3(4):101833. doi: 10.1016/j.xpro.2022.101833. PMID: 36386879; PMCID: PMC9664409.

2: Keir HR, Long MB, Abo-Leyah H, Giam YH, Vadiveloo T, Pembridge T, Hull RC, Delgado L, Band M, McLaren-Neil F, Adamson S, Lahnsteiner E, Gilmour A, Hughes C, New BJ, Connell D, Dowey R, Turton H, Richardson H, Cassidy D, Cooper J, Suntharalingam J, Diwakar L, Russell P, Underwood J, Hicks A, Dosanjh DP, Sage B, Dhasmana D, Spears M, Thompson AR, Brightling C, Smith A, Patel M, George J, Condliffe AM, Shoemark A, MacLennan G, Chalmers JD; STOP-COVID19 Investigators. Dipeptidyl peptidase-1 inhibition in patients hospitalised with COVID-19: a multicentre, double-blind, randomised, parallel-group, placebo-controlled trial. Lancet Respir Med. 2022 Dec;10(12):1119-1128. doi: 10.1016/S2213-2600(22)00261-2. Epub 2022 Sep 5. PMID: 36075243; PMCID: PMC9442496.

3: Chalmers JD, Usansky H, Rubino CM, Teper A, Fernandez C, Zou J, Mange KC. Pharmacokinetic/Pharmacodynamic Evaluation of the Dipeptidyl Peptidase 1 Inhibitor Brensocatib for Non-cystic Fibrosis Bronchiectasis. Clin Pharmacokinet. 2022 Oct;61(10):1457-1469. doi: 10.1007/s40262-022-01147-w. Epub 2022 Jul 25. PMID: 35976570; PMCID: PMC9553789.

4: Song D, Adrover JM, Felice C, Christensen LN, He XY, Merrill JR, Wilkinson JE, Janowitz T, Lyons SK, Egeblad M, Tonks NK. PTP1B inhibitors protect against acute lung injury and regulate CXCR4 signaling in neutrophils. JCI Insight. 2022 Jul 22;7(14):e158199. doi: 10.1172/jci.insight.158199. PMID: 35866483; PMCID: PMC9431713.

5: Wu XS, He XY, Ipsaro JJ, Huang YH, Preall JB, Ng D, Shue YT, Sage J, Egeblad M, Joshua-Tor L, Vakoc CR. OCA-T1 and OCA-T2 are coactivators of POU2F3 in the tuft cell lineage. Nature. 2022 Jul;607(7917):169-175. doi: 10.1038/s41586-022-04842-7. Epub 2022 May 16. PMID: 35576971; PMCID: PMC9419707.

6: Quail DF, Amulic B, Aziz M, Barnes BJ, Eruslanov E, Fridlender ZG, Goodridge HS, Granot Z, Hidalgo A, Huttenlocher A, Kaplan MJ, Malanchi I, Merghoub T, Meylan E, Mittal V, Pittet MJ, Rubio-Ponce A, Udalova IA, van den Berg TK, Wagner DD, Wang P, Zychlinsky A, de Visser KE, Egeblad M, Kubes P. Neutrophil phenotypes and functions in cancer: A consensus statement. J Exp Med. 2022 Jun 6;219(6):e20220011. doi: 10.1084/jem.20220011. Epub 2022 May 6. PMID: 35522219; PMCID: PMC9086501.

7: Usansky H, Yoon E, Teper A, Zou J, Fernandez C. Safety, Tolerability, and Pharmacokinetic Evaluation of Single and Multiple Doses of the Dipeptidyl Peptidase 1 Inhibitor Brensocatib in Healthy Japanese and White Adults. Clin Pharmacol Drug Dev. 2022 Jul;11(7):832-842. doi: 10.1002/cpdd.1094. Epub 2022 Apr 11. PMID: 35411669; PMCID: PMC9322451.

8: Adrover JM, Carrau L, Daßler-Plenker J, Bram Y, Chandar V, Houghton S, Redmond D, Merrill JR, Shevik M, tenOever BR, Lyons SK, Schwartz RE, Egeblad M. Disulfiram inhibits neutrophil extracellular trap formation and protects rodents from acute lung injury and SARS-CoV-2 infection. JCI Insight. 2022 Mar 8;7(5):e157342. doi: 10.1172/jci.insight.157342. PMID: 35133984; PMCID: PMC8983145.

9: Maiorino L, Shevik M, Adrover JM, Han X, Georgas E, Wilkinson JE, Seidner H, Foerschner L, Tuveson DA, Qin YX, Egeblad M. Longitudinal Intravital Imaging Through Clear Silicone Windows. J Vis Exp. 2022 Jan 5;(179):10.3791/62757. doi: 10.3791/62757. PMID: 35068483; PMCID: PMC9286001.

10: Korkmaz B, Lamort AS, Domain R, Beauvillain C, Gieldon A, Yildirim AÖ, Stathopoulos GT, Rhimi M, Jenne DE, Kettritz R. Cathepsin C inhibition as a potential treatment strategy in cancer. Biochem Pharmacol. 2021 Dec;194:114803. doi: 10.1016/j.bcp.2021.114803. Epub 2021 Oct 20. PMID: 34678221.

11: Shen XB, Chen X, Zhang ZY, Wu FF, Liu XH. Cathepsin C inhibitors as anti- inflammatory drug discovery: Challenges and opportunities. Eur J Med Chem. 2021 Dec 5;225:113818. doi: 10.1016/j.ejmech.2021.113818. Epub 2021 Sep 3. PMID: 34492551.

12: Sun L, Kees T, Almeida AS, Liu B, He XY, Ng D, Han X, Spector DL, McNeish IA, Gimotty P, Adams S, Egeblad M. Activating a collaborative innate-adaptive immune response to control metastasis. Cancer Cell. 2021 Oct 11;39(10):1361-1374.e9. doi: 10.1016/j.ccell.2021.08.005. Epub 2021 Sep 2. PMID: 34478639; PMCID: PMC8981964.

13: Fujii T, Rehman H, Chung SY, Shen J, Newman J, Wu V, Hines A, Azimi-Nekoo E, Fayyaz F, Lee M, Raptis G, Egeblad M, Zhu X. Treatment with Granulocyte-colony Stimulating Factor (G-CSF) is not associated with Increased Risk of Brain Metastasis in Patients with De Novo Stage IV Breast Cancer. J Cancer. 2021 Jul 25;12(18):5687-5692. doi: 10.7150/jca.63159. PMID: 34405029; PMCID: PMC8364654.

14: Xiao Y, Cong M, Li J, He D, Wu Q, Tian P, Wang Y, Yang S, Liang C, Liang Y, Wen J, Liu Y, Luo W, Lv X, He Y, Cheng DD, Zhou T, Zhao W, Zhang P, Zhang X, Xiao Y, Qian Y, Wang H, Gao Q, Yang QC, Yang Q, Hu G. Cathepsin C promotes breast cancer lung metastasis by modulating neutrophil infiltration and neutrophil extracellular trap formation. Cancer Cell. 2021 Mar 8;39(3):423-437.e7. doi: 10.1016/j.ccell.2020.12.012. Epub 2021 Jan 14. PMID: 33450198.

15: Kingston L, Gu C, Guo J, Swallow S, Elmore CS. The impact of radiochemistry in drug projects: The use of C-14 label in the AZD8529, AZD7325, and AZD6280 projects. J Labelled Comp Radiopharm. 2021 Feb;64(2):65-72. doi: 10.1002/jlcr.3902. Epub 2021 Jan 7. PMID: 33326121.

16: Chalmers JD, Haworth CS, Metersky ML, Loebinger MR, Blasi F, Sibila O, O'Donnell AE, Sullivan EJ, Mange KC, Fernandez C, Zou J, Daley CL; WILLOW Investigators. Phase 2 Trial of the DPP-1 Inhibitor Brensocatib in Bronchiectasis. N Engl J Med. 2020 Nov 26;383(22):2127-2137. doi: 10.1056/NEJMoa2021713. Epub 2020 Sep 7. PMID: 32897034.

17: Ludvigsson JW, Wikström H, Andersson T, Norrby PO. Degradation caused by incompatibility between sodium stearyl fumarate (PRUV) and AZD7986 in the drug product. J Pharm Biomed Anal. 2018 Sep 5;158:82-87. doi: 10.1016/j.jpba.2018.05.036. Epub 2018 May 22. PMID: 29860182.

18: Palmér R, Mäenpää J, Jauhiainen A, Larsson B, Mo J, Russell M, Root J, Prothon S, Chialda L, Forte P, Egelrud T, Stenvall K, Gardiner P. Dipeptidyl Peptidase 1 Inhibitor AZD7986 Induces a Sustained, Exposure-Dependent Reduction in Neutrophil Elastase Activity in Healthy Subjects. Clin Pharmacol Ther. 2018 Dec;104(6):1155-1164. doi: 10.1002/cpt.1053. Epub 2018 Apr 16. PMID: 29484635; PMCID: PMC6282495.

19: Doyle K, Lönn H, Käck H, Van de Poël A, Swallow S, Gardiner P, Connolly S, Root J, Wikell C, Dahl G, Stenvall K, Johannesson P. Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986). J Med Chem. 2016 Oct 27;59(20):9457-9472. doi: 10.1021/acs.jmedchem.6b01127. Epub 2016 Oct 11. PMID: 27690432.

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AZD7986

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