WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H208429
CAS#: 2409963-83-1 (free base)
Description: PXS-5505 is a Pan-Lysyl Oxidase Inhibitor that has been found to ameliorate multiple-organ fibrosis by inhibiting collagen crosslinks in rodent models in systemic sclerosis. PXS-5505 inhibited lysyl oxidase activity in the skin and LOXL2 activity in the lung. PXS-5505 exhibited anti-fibrotic effects in the SSc skin mouse model, reducing dermal thickness and α-smooth muscle actin. Similarly, in the bleomycin-induced mouse lung model, PXS-5505 reduced pulmonary fibrosis toward normal levels, mediated by its ability to normalise collagen/elastin crosslink formation. PXS-5505 also reduced fibrotic extent in models of the ischaemia-reperfusion heart, the unilateral ureteral obstruction kidney, and the CCl4-induced fibrotic liver.
Hodoodo Cat#: H208429
Name: PXS-5505 free base
CAS#: 2409963-83-1 (free base)
Chemical Formula: C13H13FN2O2S
Exact Mass: 280.07
Molecular Weight: 280.320
Elemental Analysis: Elemental Analysis: C, 55.70; H, 4.67; F, 6.78; N, 9.99; O, 11.41; S, 11.44
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Related CAS #: 2409963-83-1 (free base) 2409964-23-2 (HCl)
Synonym: PXS5505, PXS 5505, PXS-5505; LOX-IN-3
IUPAC/Chemical Name: (Z)-3-Fluoro-4-quinolin-8-ylsulfonylbut-2-en-1-amine
InChi Key: DHXXLGDTPFPYRH-WDZFZDKYSA-N
InChi Code: InChI=1S/C13H13FN2O2S/c14-11(6-7-15)9-19(17,18)12-5-1-3-10-4-2-8-16-13(10)12/h1-6,8H,7,9,15H2/b11-6-
SMILES Code: NC/C=C(F)/CS(=O)(C1=C2N=CC=CC2=CC=C1)=O
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:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 280.32 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.
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 |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Xu Q, Streuer A, Jann JC, Altrock E, Schmitt N, Flach J, Sens-Albert C, Rapp F, Wolf J, Nowak V, Weimer N, Obländer J, Palme I, Kuzina M, Jawhar A, Darwich A, Weis CA, Marx A, Wuchter P, Costina V, Jäger E, Sperk E, Neumaier M, Fabarius A, Metzgeroth G, Nolte F, Steiner L, Levkin PA, Jawhar M, Hofmann WK, Riabov V, Nowak D. Inhibition of lysyl oxidases synergizes with 5-azacytidine to restore erythropoiesis in myelodysplastic and myeloid malignancies. Nat Commun. 2023 Mar 17;14(1):1497. doi: 10.1038/s41467-023-37175-8. PMID: 36932114; PMCID: PMC10023686.
2: Yao Y, Findlay A, Stolp J, Rayner B, Ask K, Jarolimek W. Pan-Lysyl Oxidase Inhibitor PXS-5505 Ameliorates Multiple-Organ Fibrosis by Inhibiting Collagen Crosslinks in Rodent Models of Systemic Sclerosis. Int J Mol Sci. 2022 May 16;23(10):5533. doi: 10.3390/ijms23105533. PMID: 35628342; PMCID: PMC9146019.
3: Perryman L, Gray SG. Fibrosis in Mesothelioma: Potential Role of Lysyl Oxidases. Cancers (Basel). 2022 Feb 15;14(4):981. doi: 10.3390/cancers14040981. PMID: 35205728; PMCID: PMC8870010.
4: Nguyen LT, Saad S, Shi Y, Wang R, Chou ASY, Gill A, Yao Y, Jarolimek W, Pollock CA. Lysyl oxidase inhibitors attenuate cyclosporin A-induced nephropathy in mouse. Sci Rep. 2021 Jun 14;11(1):12437. doi: 10.1038/s41598-021-91772-5. PMID: 34127702; PMCID: PMC8203624.