1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. Zatolmilast

Zatolmilast (BPN14770) is a selective phosphodiesterase 4D (PDE4D) allosteric inhibitor with IC50s of 7.8 nM and 7.4 nM for PDE4D7 and PDE4D3, respectively.

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

Zatolmilast Chemical Structure

Zatolmilast Chemical Structure

CAS No. : 1606974-33-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 293 In-stock
Solution
10 mM * 1 mL in DMSO USD 308 In-stock
Solid
1 mg USD 133 In-stock
5 mg USD 280 In-stock
10 mg USD 365 In-stock
25 mg USD 535 In-stock
50 mg USD 740 In-stock
100 mg USD 995 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Zatolmilast (BPN14770) is a selective phosphodiesterase 4D (PDE4D) allosteric inhibitor with IC50s of 7.8 nM and 7.4 nM for PDE4D7 and PDE4D3, respectively[1].

IC50 & Target[1]

PDE4D3

7.4 nM (IC50)

PDE4D7

7.8 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
Sf9 IC50
1018 nM
Compound: 28; BPN14770
Inhibition of recombinant human wild-type His6-tagged PDE4D7 UCR1 domain (S129 residues) expressed in baculovirus infected Sf9 insect cells using cAMP as substrate preincubated for 5 to 10 mins followed by substrate addition and measured for 10 mins by ye
Inhibition of recombinant human wild-type His6-tagged PDE4D7 UCR1 domain (S129 residues) expressed in baculovirus infected Sf9 insect cells using cAMP as substrate preincubated for 5 to 10 mins followed by substrate addition and measured for 10 mins by ye
[PMID: 31013090]
Sf9 IC50
127 nM
Compound: 28; BPN14770
Inhibition of recombinant human His6-tagged PDE4D2 expressed in baculovirus infected Sf9 insect cells using cAMP as substrate preincubated for 5 to 10 mins followed by substrate addition and measured for 10 mins by yeast myokinase/pyruvate kinase/lactate
Inhibition of recombinant human His6-tagged PDE4D2 expressed in baculovirus infected Sf9 insect cells using cAMP as substrate preincubated for 5 to 10 mins followed by substrate addition and measured for 10 mins by yeast myokinase/pyruvate kinase/lactate
[PMID: 31013090]
Sf9 IC50
2013 nM
Compound: 28; BPN14770
Inhibition of recombinant human His6-tagged PDE4B1 UCR1 S133D mutant expressed in baculovirus infected Sf9 insect cells using cAMP as substrate preincubated for 5 to 10 mins followed by substrate addition and measured for 10 mins by yeast myokinase/pyruva
Inhibition of recombinant human His6-tagged PDE4B1 UCR1 S133D mutant expressed in baculovirus infected Sf9 insect cells using cAMP as substrate preincubated for 5 to 10 mins followed by substrate addition and measured for 10 mins by yeast myokinase/pyruva
[PMID: 31013090]
Sf9 IC50
6561 nM
Compound: 28; BPN14770
Inhibition of recombinant human His6-tagged PDE4D UCR2 deletion mutant catalytic domain expressed in baculovirus infected Sf9 insect cells using cAMP as substrate preincubated for 5 to 10 mins followed by substrate addition and measured for 10 mins by yea
Inhibition of recombinant human His6-tagged PDE4D UCR2 deletion mutant catalytic domain expressed in baculovirus infected Sf9 insect cells using cAMP as substrate preincubated for 5 to 10 mins followed by substrate addition and measured for 10 mins by yea
[PMID: 31013090]
Sf9 IC50
7.4 nM
Compound: 28; BPN14770
Inhibition of recombinant human His6-tagged PDE4D3 UCR1 S54D mutant expressed in baculovirus infected Sf9 insect cells using cAMP as substrate preincubated for 5 to 10 mins followed by substrate addition and measured for 10 mins by yeast myokinase/pyruvat
Inhibition of recombinant human His6-tagged PDE4D3 UCR1 S54D mutant expressed in baculovirus infected Sf9 insect cells using cAMP as substrate preincubated for 5 to 10 mins followed by substrate addition and measured for 10 mins by yeast myokinase/pyruvat
[PMID: 31013090]
Sf9 IC50
7.8 nM
Compound: 28; BPN14770
Inhibition of recombinant human His6-tagged PDE4D7 UCR1 S129D mutant expressed in baculovirus infected Sf9 insect cells using cAMP as substrate preincubated for 5 to 10 mins followed by substrate addition and measured for 10 mins by yeast myokinase/pyruva
Inhibition of recombinant human His6-tagged PDE4D7 UCR1 S129D mutant expressed in baculovirus infected Sf9 insect cells using cAMP as substrate preincubated for 5 to 10 mins followed by substrate addition and measured for 10 mins by yeast myokinase/pyruva
[PMID: 31013090]
In Vivo

Zatolmilast increases brain cAMP, increases phosphorylation of CREB and increases production of brain-derived neurotrophic factor (BDNF) in hippocampus[1].
? Zatolmilast (0.1-30 mg/kg; p.o.; 24 hours) provides cognitive benefit in the mouse novel object recognition (NOR) at doses above 0.3 mg/kg[2].

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

Animal Model: C57Bl6 mice[2]
Dosage: 0.1, 0.3, 1, 3, 10, 30 mg/kg
Administration: p.o.; 24 hours
Result: Significantly improved novel object discrimination at doses above 0.3 mg/kg.
Clinical Trial
NCT NumberSponsorConditionStart DatePhase
NCT05163808Tetra Discovery Partners
Fragile X Syndrome
March 29, 2022Phase 2|Phase 3
NCT02840279Tetra Discovery Partners
Alzheimer´s Disease
June 2016Phase 1
NCT05358886Tetra Discovery Partners
Fragile X Syndrome
November 1, 2022Phase 3
Molecular Weight

405.80

Formula

C21H15ClF3NO2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)CC1=CC=C(CC2=CC(C3=CC=CC(Cl)=C3)=NC(C(F)(F)F)=C2)C=C1

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 : ≥ 100 mg/mL (246.43 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4643 mL 12.3213 mL 24.6427 mL
5 mM 0.4929 mL 2.4643 mL 4.9285 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
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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

=
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C2

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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: ≥ 2.17 mg/mL (5.35 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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: ≥ 2.17 mg/mL (5.35 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.17 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 (21.7 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, PEG300/PEG400, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.50%

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 2.4643 mL 12.3213 mL 24.6427 mL 61.6067 mL
5 mM 0.4929 mL 2.4643 mL 4.9285 mL 12.3213 mL
10 mM 0.2464 mL 1.2321 mL 2.4643 mL 6.1607 mL
15 mM 0.1643 mL 0.8214 mL 1.6428 mL 4.1071 mL
20 mM 0.1232 mL 0.6161 mL 1.2321 mL 3.0803 mL
25 mM 0.0986 mL 0.4929 mL 0.9857 mL 2.4643 mL
30 mM 0.0821 mL 0.4107 mL 0.8214 mL 2.0536 mL
40 mM 0.0616 mL 0.3080 mL 0.6161 mL 1.5402 mL
50 mM 0.0493 mL 0.2464 mL 0.4929 mL 1.2321 mL
60 mM 0.0411 mL 0.2054 mL 0.4107 mL 1.0268 mL
80 mM 0.0308 mL 0.1540 mL 0.3080 mL 0.7701 mL
100 mM 0.0246 mL 0.1232 mL 0.2464 mL 0.6161 mL
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Zatolmilast
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