2. Membrane Transporter/Ion Channel
  3. Ferroportin
  4. DMT1 blocker 2

DMT1 blocker 2 is a direct inhibitor of divalent metal transporter 1 (DMT1), with an IC50 of 0.83 μM. DMT1 blocker 2 can block iron uptake by enterocytes in vivo.

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DMT1 blocker 2 Chemical Structure

DMT1 blocker 2 Chemical Structure

CAS No. : 1062648-63-8

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Based on 2 publication(s) in Google Scholar

DMT1 blocker 2 Related Antibodies

Top Publications Citing Use of Products

2 Publications Citing Use of MCE DMT1 blocker 2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

DMT1 blocker 2 is a direct inhibitor of divalent metal transporter 1 (DMT1), with an IC50 of 0.83 μM. DMT1 blocker 2 can block iron uptake by enterocytes in vivo[1].

IC50 & Target

IC50: 0.83 μM (divalent metal transporter 1)[1]
Cellular Effect
Cell Line Type Value Description References
CHO IC50
0.83 μM
Compound: 12f
Inhibition of human DMT1 expressed in CHO cells assessed as blockage of ferrous influx after 20 mins by calcein fluorescence quenching method
Inhibition of human DMT1 expressed in CHO cells assessed as blockage of ferrous influx after 20 mins by calcein fluorescence quenching method
[PMID: 22154351]
In Vitro

DMT1 blocker 2 (Compound 12f) (10 μM; 24 h) has no cytotoxic to HepG2 cells[1].
DMT1 blocker 2 (10 μM) inhibits 44% of CYP3A4 activity[1].

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

DMT1 blocker 2 Related Antibodies
In Vivo

DMT1 blocker 2 (50 mg/kg; p.o.) blocks iron uptake by enterocytes in an acute rat model of iron hyperabsorption[1].

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

Animal Model: Weanling (3-4 weeks) rats were placed on a low iron diet for four weeks[1]
Dosage: 50 mg/kg
Administration: Oral gavage followed 1 h later by an iron challenge
Result: Attenuated the post-challenge serum iron increase.
Molecular Weight

263.29

Formula

C16H13N3O
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

OC1=C2C3=C(C=CC=C3)CCC2=NN1C4=NC=CC=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (189.90 mM; Need ultrasonic; 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 3.7981 mL 18.9905 mL 37.9809 mL
5 mM 0.7596 mL 3.7981 mL 7.5962 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (9.50 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (9.50 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.7981 mL 18.9905 mL 37.9809 mL 94.9523 mL
5 mM 0.7596 mL 3.7981 mL 7.5962 mL 18.9905 mL
10 mM 0.3798 mL 1.8990 mL 3.7981 mL 9.4952 mL
15 mM 0.2532 mL 1.2660 mL 2.5321 mL 6.3302 mL
20 mM 0.1899 mL 0.9495 mL 1.8990 mL 4.7476 mL
25 mM 0.1519 mL 0.7596 mL 1.5192 mL 3.7981 mL
30 mM 0.1266 mL 0.6330 mL 1.2660 mL 3.1651 mL
40 mM 0.0950 mL 0.4748 mL 0.9495 mL 2.3738 mL
50 mM 0.0760 mL 0.3798 mL 0.7596 mL 1.8990 mL
60 mM 0.0633 mL 0.3165 mL 0.6330 mL 1.5825 mL
80 mM 0.0475 mL 0.2374 mL 0.4748 mL 1.1869 mL
100 mM 0.0380 mL 0.1899 mL 0.3798 mL 0.9495 mL
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DMT1 blocker 2 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:

DMT1 blocker 21062648-63-8FerroportinIron-regulated Transporter 1directdivalentmetaltransporterDMT1ironuptakeenterocytesInhibitorinhibitorinhibit

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