1. MAPK/ERK Pathway Stem Cell/Wnt Protein Tyrosine Kinase/RTK
  2. ERK FGFR
  3. MD-3-A45

MD-3-A45 is an inhibitor of fibroblast growth factor 23 (FGF-23). MD-3-A45 blocks the activation of the FGFRs/α-klotho signaling pathway by FGF-23 and inhibits FGF-23-induced ERK activation. MD-3-A45 can be used in the research of chronic kidney disease, hereditary hypophosphatemic rickets and acquired hypophosphatemic rickets.

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

MD-3-A45

MD-3-A45 Chemical Structure

CAS No. : 2314337-87-4

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Description

MD-3-A45 is an inhibitor of fibroblast growth factor 23 (FGF-23). MD-3-A45 blocks the activation of the FGFRs/α-klotho signaling pathway by FGF-23 and inhibits FGF-23-induced ERK activation. MD-3-A45 can be used in the research of chronic kidney disease, hereditary hypophosphatemic rickets and acquired hypophosphatemic rickets[1].

Cellular Effect
Cell Line Type Value Description References
HEK-293T EC50
6.9 10^2 μM
Compound: 13a
Cytotoxicity against HEK293T cells assessed as effect on LDH release measured after 5 hrs by CytoTox96 Non-Radioactive assay
Cytotoxicity against HEK293T cells assessed as effect on LDH release measured after 5 hrs by CytoTox96 Non-Radioactive assay
[PMID: 33232874]
In Vitro

MD-3-A45 completely inhibits FGF-23-induced ERK activation in HEK-293 cells expressing FGFRs/α-Klotho with an IC50 of 0.14 μM, and has a metabolic stability half-life of 9 minutes[1].

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

Molecular Weight

237.30

Formula

C16H15NO

CAS No.
Appearance

Solid

Color

Off-white to light brown

SMILES

O/N=C/C1=C(/C=C/C2=CC=C(C)C=C2)C=CC=C1

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 : 50 mg/mL (210.70 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 4.2141 mL 21.0704 mL 42.1407 mL
5 mM 0.8428 mL 4.2141 mL 8.4281 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.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 1.25 mg/mL (5.27 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
  • Protocol 2

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

    Solubility: ≥ 1.25 mg/mL (5.27 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 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 (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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 4.2141 mL 21.0704 mL 42.1407 mL 105.3519 mL
5 mM 0.8428 mL 4.2141 mL 8.4281 mL 21.0704 mL
10 mM 0.4214 mL 2.1070 mL 4.2141 mL 10.5352 mL
15 mM 0.2809 mL 1.4047 mL 2.8094 mL 7.0235 mL
20 mM 0.2107 mL 1.0535 mL 2.1070 mL 5.2676 mL
25 mM 0.1686 mL 0.8428 mL 1.6856 mL 4.2141 mL
30 mM 0.1405 mL 0.7023 mL 1.4047 mL 3.5117 mL
40 mM 0.1054 mL 0.5268 mL 1.0535 mL 2.6338 mL
50 mM 0.0843 mL 0.4214 mL 0.8428 mL 2.1070 mL
60 mM 0.0702 mL 0.3512 mL 0.7023 mL 1.7559 mL
80 mM 0.0527 mL 0.2634 mL 0.5268 mL 1.3169 mL
100 mM 0.0421 mL 0.2107 mL 0.4214 mL 1.0535 mL
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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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MD-3-A45
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