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5.38759

Sigma-Aldrich

MCT1 Inhibitor III

Synonym(s):

MCT1 Inhibitor III, ( E)-2-Cyano-3-(4-(diphenylamino)-2-methoxyphenyl)acrylate, Sodium, Monocarboxylate Transport 1 Inhibitor III

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About This Item

Empirical Formula (Hill Notation):
C23H17N2NaO3
Molecular Weight:
392.38
UNSPSC Code:
12352200
NACRES:
NA.77

assay

≥97% (HPLC)

Quality Level

100

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
desiccated (hygroscopic)
protect from light

color

yellow

solubility

DMSO: 50 mg/mL

storage temp.

−20°C

General description

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.: t1/2 = 3.03 h, Tmax = 0.667 h & Cmax = 17.5 mg/L; 100 mg/kg, i.p.: t1/2 = 3.19 h, Tmax = 0.5 h & Cmax = 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.: t1/2 = 3.03 h, Tmax = 0.667 h & Cmax = 17.5 mg/L; 100 mg/kg, i.p.: t1/2 = 3.19 h, Tmax = 0.5 h & Cmax = 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.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
MCT1
Reversible: yes
Target IC50: 11 nM for [¹⁴C]-lactate uptake in rat brain endothelial cell line RBE4

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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