MedKoo Cat#: 555681 | Name: PXS-5153A

Description:

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

PXS-5153A is a novel mechanism based, fast-acting, dual LOXL2/LOXL3 inhibitor, which was used to interrogate the role of these enzymes in models of collagen crosslinking and fibrosis. PXS-5153A dose-dependently reduced LOXL2-mediated collagen oxidation and collagen crosslinking in vitro. In two liver fibrosis models, carbon tetrachloride or streptozotocin/high fat diet-induced, PXS-5153A reduced disease severity and improved liver function by diminishing collagen content and collagen crosslinks. In myocardial infarction, PXS-5153A improved cardiac output.

Chemical Structure

PXS-5153A
PXS-5153A
CAS#2125956-82-1 (HCl)

Theoretical Analysis

MedKoo Cat#: 555681

Name: PXS-5153A

CAS#: 2125956-82-1 (HCl)

Chemical Formula: C20H25Cl2FN4O2S

Exact Mass:

Molecular Weight: 475.40

Elemental Analysis: C, 50.53; H, 5.30; Cl, 14.91; F, 4.00; N, 11.79; O, 6.73; S, 6.74

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
2125956-82-1 (HCl) 2125956-81-0 (free base)
Synonym
PXS-5153A; PXS 5153A; PXS5153A; PXS-5153; PXS 5153; PXS5153;
IUPAC/Chemical Name
(Z)-3-(1-(4-amino-2-fluorobut-2-en-1-yl)-2-methyl-1H-pyrrolo[3,2-b]pyridin-3-yl)-N,N-dimethylbenzenesulfonamide dihydrochloride
InChi Key
INSNGJNTNAUITD-ULPVBNQHSA-N
InChi Code
InChI=1S/C20H23FN4O2S.2ClH/c1-14-19(15-6-4-7-17(12-15)28(26,27)24(2)3)20-18(8-5-11-23-20)25(14)13-16(21)9-10-22;;/h4-9,11-12H,10,13,22H2,1-3H3;2*1H/b16-9-;;
SMILES Code
O=S(C1=CC=CC(C2=C(C)N(C/C(F)=C/CN)C3=CC=CN=C32)=C1)(N(C)C)=O.[H]Cl.[H]Cl
Appearance
Solid powder
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
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
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

Preparing Stock Solutions

The following data is based on the product molecular weight 475.40 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: Schilter H, Findlay AD, Perryman L, Yow TT, Moses J, Zahoor A, Turner CI, Deodhar M, Foot JS, Zhou W, Greco A, Joshi A, Rayner B, Townsend S, Buson A, Jarolimek W. The lysyl oxidase like 2/3 enzymatic inhibitor, PXS-5153A, reduces crosslinks and ameliorates fibrosis. J Cell Mol Med. 2019 Mar;23(3):1759-1770. doi: 10.1111/jcmm.14074. Epub 2018 Dec 9. PubMed PMID: 30536539; PubMed Central PMCID: PMC6378217.