1. Membrane Transporter/Ion Channel
  2. Monocarboxylate Transporter
  3. MSC-4381

MSC-4381  (Synonyms: MCT4-IN-1)

Cat. No.: HY-132301 Purity: 98.11%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

MSC-4381 Chemical Structure

MSC-4381 Chemical Structure

CAS No. : 2445185-57-7

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 561 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 561 In-stock
Solid
5 mg USD 510 In-stock
10 mg USD 820 In-stock
25 mg USD 1680 In-stock
50 mg USD 2650 In-stock
100 mg USD 4200 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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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[1].

IC50 & Target

MCT4

77 nM (IC50)

MCT4

11 nM (Ki)

In Vitro

MSC-4381 (compound 18n) inhibits lactate efflux in the MDA-MB-231 cell line with an IC50 of 1 nM. The on-target activity is confirmed with a Ki of 11 nM by fluorescence cross-correlation spectroscopy (FCCS)[1].
MSC-4381 does not inhibit lactate efflux to a similar extent in SNU-398 and MiaPaca2, and only 600-fold less in RT-4 cell lines[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

MSC-4381 (compound 18n; 30 mg/kg; PO; single dose) only combined with MCT1/2 inhibitor exhibits a significant tumoral intracellular lactate accumulation[1].
MSC-4381 (30 mg/kg/day; for 15 days) shows no significant antitumor activity[1].
MSC-4381 (0.2 mg/kg; iv) has 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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MC38 tumor-bearing C57/BL6 mice[1]
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[1]
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.
Molecular Weight

537.97

Appearance

Solid

Formula

C26H20ClN3O6S

CAS No.
SMILES

O=C(C1=NC=C(C#CC2=CC(Cl)=CC=C2NS(=O)(C3=C4N=CC=CC4=C(OCC)C=C3)=O)C(OC)=C1)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 83.33 mg/mL (154.90 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8588 mL 9.2942 mL 18.5884 mL
5 mM 0.3718 mL 1.8588 mL 3.7177 mL
10 mM 0.1859 mL 0.9294 mL 1.8588 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.87 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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MSC-4381
Cat. No.:
HY-132301
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