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Product Information:

HA130

A thiazolidinedione that is designed to target the ATX active site thr210 with a boronic moiety and shown to potently inhibit ATX lysoPLD activity (IC50 ~28 nM using recombinant human ATX or human plasma) in a reversible manner with a mixed-type Lineweaver-Burk kinetics. Reported to exhibit low cytotoxicity (TD50 = 83, 105, and 2056 µM in HEK293T, A2058, and HepG2 cultures) and no activity toward NPP1, PDE, AP, or proteasomal chymotryptic/tryptic/caspase-like activities even at concentrations as high as 10 µM. Although HA130 quickly and effectively reduces circulating LPA level when injected in mice (463 µg/kg, i.v.) in vivo, the effect appears short-lived as is the case with S32826

Cat. No.: EX-A1545    Purity: >98%
HA130
For research only, Do not use for Human!

SizeUnit Price (US$)StockQuantityOrder
50mg430In-stock
100mg650In-stock


SynonymsATX Inhibitor II, (Z)-3-((4-((3-(4-Fluorobenzyl)-2,4-dioxo-1,3-thiazolan-5-yliden)-methyl)phenoxy)methyl)benzeneboronic acid
CAS No.1229652-21-4
Purity>98%
FormulaC24H19BFNO5S
Mol Weight463.286
AppearanceOff-white solid
SolubilitySoluble in DMSO, not in water
Shelf Life>2 years if stored properly
StoragePowder -20℃ 2 years; In solvent -20℃ 1 month;
ShippingShipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
 
 
Reference:  [1]. Albers, H.M.H.G. et al. 2010. J. Med. Chem. 53, 4958.

[2]. Albers, H.M.H.G. et al. 2010. Proc. Natl. Acad. Sci. USA 107, 7257.
CoACoA of HA130
Smiles:OB(O)C1=CC=CC(COC2=CC=C(\C=C3/SC(=O)N(CC4=CC=C(F)C=C4)C3=O)C=C2)=C1

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