BI-1467335 HCl
BI-1467335, also known as PXS-4728A, is a SSAO/VAP inhibitor potentially for the treatment of non-alcoholic steatohepatitis. VAP-1/SSAO contributes to the migration of neutrophils during acute lung inflammation, pulmonary infection and airway hyperractivity. Selective VAP-1/SSAO inhibition by PXS-4728A diminished leukocyte rolling and adherence induced by CXCL1/KC. Inhibition of VAP-1/SSAO also dampened the migration of neutrophils to the lungs in response to LPS, Klebsiella pneumoniae lung infection and CLP induced sepsis; whilst still allowing for normal neutrophil defense function, resulting in increased survival.
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Chemical Information
| Name | BI-1467335 HCl |
|---|---|
| Iupac Chemical Name | (E)-4-((2-(aminomethyl)-3-fluoroallyl)oxy)-N-(tert-butyl)benzamide hydrochloride |
| Synonyms | PXS-4728A; PXS4728A; PXS 4728A; BI-1467335; BI 1467335; BI1467335; BI-1467335 HCl; BI-1467335 hydrochloride |
| Molecular Formula | C15H22ClFN2O2 |
| Molecular Weight | 316.80 |
| Smile | O=C(NC(C)(C)C)C1=CC=C(OC/C(CN)=C/F)C=C1.[H]Cl |
| InChiKey | AEMZEDNMNLIDSL-YGCVIUNWSA-N |
| InChi | InChI=1S/C15H21FN2O2.ClH/c1-15(2,3)18-14(19)12-4-6-13(7-5-12)20-10-11(8-16)9-17;/h4-8H,9-10,17H2,1-3H3,(H,18,19);1H/b11-8+; |
| CAS Number | 1478364-68-9 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| 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. |
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| Clinical study |
1: Schilter HC, Collison A, Russo RC, Foot JS, Yow TT, Vieira AT, Tavares LD, Mattes J, Teixeira MM, Jarolimek W. Effects of an anti-inflammatory VAP-1/SSAO inhibitor, PXS-4728A, on pulmonary neutrophil migration. Respir Res. 2015 Mar 20;16:42. doi: 10.1186/s12931-015-0200-z. PubMed PMID: 25889951; PubMed Central PMCID: PMC4389443.
2: Jarnicki AG, Schilter H, Liu G, Wheeldon K, Essilfie AT, Foot JS, Yow TT, Jarolimek W, Hansbro PM. The inhibitor of semicarbazide-sensitive amine oxidase, PXS-4728A, ameliorates key features of chronic obstructive pulmonary disease in a mouse model. Br J Pharmacol. 2016 Nov;173(22):3161-3175. doi: 10.1111/bph.13573. PubMed PMID: 27495192; PubMed Central PMCID: PMC5071557.
3: Katagiri D, Hamasaki Y, Doi K, Negishi K, Sugaya T, Nangaku M, Noiri E. Interstitial renal fibrosis due to multiple cisplatin treatments is ameliorated by semicarbazide-sensitive amine oxidase inhibition. Kidney Int. 2016 Feb;89(2):374-85. PubMed PMID: 26535996.
Chemical Structure
