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

MSC-4381  (Synonyms: MCT4-IN-1)

Cat. No.: HY-132301 Purity: 98.11%
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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.

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
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 561 In-stock
Solution
10 mM * 1 mL in DMSO 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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Based on 1 publication(s) in Google Scholar

MSC-4381 Related Antibodies

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  • Purity & Documentation

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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]. 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.

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].

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

MSC-4381 Related Antibodies
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].

MedChemExpress (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

Formula

C26H20ClN3O6S
CAS No.
Appearance

Solid

Color

White to yellow

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8588 mL 9.2942 mL 18.5884 mL 46.4710 mL
5 mM 0.3718 mL 1.8588 mL 3.7177 mL 9.2942 mL
10 mM 0.1859 mL 0.9294 mL 1.8588 mL 4.6471 mL
15 mM 0.1239 mL 0.6196 mL 1.2392 mL 3.0981 mL
20 mM 0.0929 mL 0.4647 mL 0.9294 mL 2.3235 mL
25 mM 0.0744 mL 0.3718 mL 0.7435 mL 1.8588 mL
30 mM 0.0620 mL 0.3098 mL 0.6196 mL 1.5490 mL
40 mM 0.0465 mL 0.2324 mL 0.4647 mL 1.1618 mL
50 mM 0.0372 mL 0.1859 mL 0.3718 mL 0.9294 mL
60 mM 0.0310 mL 0.1549 mL 0.3098 mL 0.7745 mL
80 mM 0.0232 mL 0.1162 mL 0.2324 mL 0.5809 mL
100 mM 0.0186 mL 0.0929 mL 0.1859 mL 0.4647 mL
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MSC-4381 Related Classifications

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.

Keywords:

MSC-43812445185-57-7MCT4-IN-1MSC4381MSC 4381Monocarboxylate TransporterorallyMCT4SLC16A3cytosoliclactateeffluxMDA-MB-231SNU-398MiaPaca2Inhibitorinhibitorinhibit

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