5.38759

MCT1 Inhibitor III

• Sinonimo/i: MCT1 Inhibitor III, ( E)-2-Cyano-3-(4-(diphenylamino)-2-methoxyphenyl)acrylate, Sodium, Monocarboxylate Transport 1 Inhibitor III
• Formula empirica (notazione di Hill): C₂₃H₁₇N₂NaO₃
• Peso molecolare: 392.38
• Codice UNSPSC: 12352200
• 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: yellow
• Solubilità: DMSO: 50 mg/mL
• Temperatura di conservazione: −20°C

Descrizione

Descrizione generale

A cell-permeable, orally bioavailable, water-soluble (~1 mg/ml), non-toxic α-cyanocinnamate analog that acts as a potent and reversible inhibitor of MCT1 activity (IC₅₀ = 11 nM for [¹⁴C]-lactate uptake in rat brain endothelial cell line RBE4). Shown to suppress colorectal adenocarcinoma (WiDr cell line) tumor growth in female BALB/c nude mice (% inhibition at the end of 3-weeks = 29, 45, 45 & 56 administered at 10 mg/kg, b.i.d., i.p., 50 mg/kg, b.i.d., p.o., 50 mg/kg, b.i.d., i.p. and 100 mg/kg, q.i.d., p.o., respectively). Displays favorable PK profile in mice (100 mg/kg, p.o.: t_1/2 = 3.03 h, T_max = 0.667 h & C_max = 17.5 mg/L; 100 mg/kg, i.p.: t_1/2 = 3.19 h, T_max = 0.5 h & C_max = 61.333 mg/L).

A cell-permeable, orally bioavailable, water-soluble (~1 mg/ml), non-toxic α-cyanocinnamate analog that acts as a potent and reversible inhibitor of MCT1 activity (IC₅₀ = 11 nM for [¹⁴C]-lactate uptake in rat brain endothelial cell line RBE4). Shown to suppress colorectal adenocarcinoma (WiDr cell line) tumor growth in female BALB/c nude mice (% inhibition at the end of 3-weeks = 29, 45, 45 & 56 administered at 10 mg/kg, b.i.d., i.p., 50 mg/kg, b.i.d., p.o., 50 mg/kg, b.i.d., i.p. and 100 mg/kg, q.i.d., p.o., respectively). Displays favorable PK profile in mice (100 mg/kg, p.o.: t_1/2 = 3.03 h, T_max = 0.667 h & C_max = 17.5 mg/L; 100 mg/kg, i.p.: t_1/2 = 3.19 h, T_max = 0.5 h & C_max = 61.333 mg/L).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Azioni biochim/fisiol

Cell permeable: yes

Primary Target
MCT1

Reversible: yes

Target IC₅₀: 11 nM for [¹⁴C]-lactate uptake in rat brain endothelial cell line RBE4

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Altre note

Gurrapu, S., et al. 2015. ACS Med. Chem. Lett.6, 558.

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