MedKoo Cat#: 207207 | Name: PXS-5505 HCl
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Description:

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

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.

Chemical Structure

PXS-5505 HCl
PXS-5505 HCl
CAS#2409964-23-2 (HCl)

Theoretical Analysis

MedKoo Cat#: 207207

Name: PXS-5505 HCl

CAS#: 2409964-23-2 (HCl)

Chemical Formula: C13H15Cl2FN2O2S

Exact Mass: 0.0000

Molecular Weight: 353.23

Elemental Analysis: C, 44.20; H, 4.28; Cl, 20.07; F, 5.38; N, 7.93; O, 9.06; S, 9.08

Price and Availability

Size Price Availability Quantity
5mg USD 150.00 Ready to ship
10mg USD 250.00 Ready to ship
25mg USD 450.00 Ready to ship
50mg USD 750.00 Ready to ship
100mg USD 1,250.00 Ready to ship
200mg USD 1,950.00 Ready to ship
500mg USD 3,650.00 Ready to ship
1g USD 5,250.00 Ready to ship
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Synonym
PXS-5505 HCl; PXS-5505 2HCl; PXS-5505 dihydrochloride; PXS-5505; PXS 5505; PXS5505;
IUPAC/Chemical Name
(Z)-3-Fluoro-4-quinolin-8-ylsulfonylbut-2-en-1-amine dihyrochloride
InChi Key
YYYHSAUHJBNINZ-LEOXJOGCSA-N
InChi Code
InChI=1S/C13H13FN2O2S.2ClH/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;2*1H/b11-6-;;
SMILES Code
NC/C=C(F)/CS(=O)(C1=C2N=CC=CC2=CC=C1)=O.[H]Cl.[H]Cl
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:
PXS-5505 HCl is a LOX inhibitor.
In vitro activity:
To be determined
In vivo activity:
PXS-5505 shows strong anti-fibrotic potential in various organ fibrosis models, including those relevant to systemic sclerosis. It may offer a novel treatment for SSc. When taken orally, PXS-5505 inhibits skin and lung enzyme activity, reducing fibrosis in mouse models of systemic sclerosis. It also reduces fibrosis in heart, kidney, and liver models. Reference: Int J Mol Sci. 2022 May 16;23(10):5533. https://pubmed.ncbi.nlm.nih.gov/35628342/

Preparing Stock Solutions

The following data is based on the product molecular weight 353.23 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
Formulation 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.
In vitro protocol:
To be determined
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.
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.