MSC-4381

SKU: orb2900974

Description

MSC-4381 (MCT4-IN-1) is an orally active and selective monocarboxylate transporter 4 (MCT4/SLC16A3) inhibitor with an IC50 of 77 nM and a Ki of 11 nM. MSC-4381 targets to the cytosolic domain of MCT4. MSC-4381 results in lactate efflux inhibition and reduction of cellular viability in MCT4 high expressing cells. MSC-4381 has the potential for MCT4 transporter inhibition research. MSC-4381 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Key Properties

• CAS Number: 2445185-57-7
• MW: 537.97
• Purity: >98% (HPLC)
• Formula: C₂₆H₂₀ClN₃O₆S
• SMILES: CCOc1ccc(c2ncccc12)S(=O)(=O)Nc1ccc(Cl)cc1C#Cc1cnc(cc1OC)C(O)=O
• Target: Monocarboxylate Transporter
• Solubility: In Vitro: DMSO : 83.33 mg/mL (154.90 mM; Ultrasonic (<60°C)

Bioactivity

• In Vivo:
  Animal model: MC38 tumor-bearing C57/BL6 mice. Dosage: 30 mg/kg. Administration: PO; single dose. Result: Only combined with MCT1/2 inhibitor exhibited a significant tumoral intracellular lactate accumulation. Animal model: Mice. Dosage: 0.2 mg/kg (Pharmacokinetic Analysis). Administration: IV. Result: Had a T1/2 of 1 hours, a CL of 0.33 L/h kg, a Cmax of 489 ng/mL and a Vss of 0.4 L/kg for mice.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Monocarboxylate Transporter