189511

Autotaxin Inhibitor II, HA130

• Sinonimo/i: Autotaxin Inhibitor II, HA130, ATX Inhibitor II, (Z)-3-((4-((3-(4-Fluorobenzyl)-2,4-dioxo-1,3-thiazolan-5-yliden)-methyl)phenoxy)methyl)benzeneboronic acid
• Formula empirica (notazione di Hill): C₂₄H₁₉BFNO₅S
• Peso molecolare: 463.29
• Codice UNSPSC: 51111800
• NACRES: NA.77

Proprietà

• Saggio: ≥97% (HPLC)
• Livello qualitativo: 100
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; desiccated (hygroscopic); protect from light
• Colore: off-white
• Solubilità: DMSO: 50 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: −20°C

Descrizione

Descrizione generale

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. 189510).

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.189510).

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Regulatory Review (Z)

Ricostituzione

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Altre note

Albers, H.M.H.G. et al. 2010. J. Med. Chem.53, 4958.
Albers, H.M.H.G. et al. 2010. Proc. Natl. Acad. Sci. USA107, 7257.

Note legali

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable