Zatolmilast (Synonyms: BPN14770)

Name: Zatolmilast
Brand: MedChemExpress
SKU: HY-117571
Rating: 5.0 (2 reviews)

Cat. No.: HY-117571 Purity: 99.50%: Data Sheet
SDS

COA
Handling Instructions Technical Support

Solubility

In Vivo Dissolution Calculator

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

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	Estimated Time of Arrival: April 2
Solution
10 mM * 1 mL in DMSO	USD 308	In-stock	Estimated Time of Arrival: April 2
Solid
1 mg	USD 133	In-stock	Estimated Time of Arrival: April 2
5 mg	USD 280	In-stock	Estimated Time of Arrival: April 2
10 mg	USD 365	In-stock	Estimated Time of Arrival: April 2
25 mg	USD 535	In-stock	Estimated Time of Arrival: April 2
50 mg	USD 740	In-stock	Estimated Time of Arrival: April 2
100 mg	USD 995	In-stock	Estimated Time of Arrival: April 2
200 mg		Get quote
500 mg		Get quote

Get it April 2 by noon. Order within 20 hrs 23 mins.

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Customer Review

Based on 2 publication(s) in Google Scholar

2 Publications Citing Use of MCE Zatolmilast

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PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

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 Number	Sponsor	Condition	Start Date	Phase
NCT05163808	Tetra Discovery Partners	Fragile X Syndrome	March 29, 2022	Phase 2\|Phase 3
NCT02840279	Tetra Discovery Partners	Alzheimer´s Disease	June 2016	Phase 1
NCT05358886	Tetra Discovery Partners	Fragile X Syndrome	November 1, 2022	Phase 3
NCT03817684	Tetra Discovery Partners	Alzheimer´s Disease	April 30, 2019	Phase 2
NCT03861000	National Institute of Mental Health (NIMH)\|National Institutes of Health Clinical Center (CC)	Depression	March 12, 2019	Phase 1\|Phase 2
NCT03030105	Tetra Discovery Partners	Alzheimer Disease	January 2017	Phase 1
NCT02648672	Tetra Discovery Partners	Alzheimer´s Disease	December 2015	Phase 1
NCT03569631	Tetra Discovery Partners	Fragile X Syndrome\|FXS\|Fra(X) Syndrome	July 9, 2018	Phase 2
NCT05367960	Tetra Discovery Partners	Fragile X Syndrome	November 1, 2022	Phase 3

Molecular Weight

405.80

Formula

C₂₁H₁₅ClF₃NO₂

CAS No.

1606974-33-7

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
10 mM	0.2464 mL	1.2321 mL	2.4643 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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)

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%

Select Batch:

Data Sheet (272 KB) SDS (393 KB)

COA (245 KB)HNMR (140 KB)LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Ricciarelli R, et al. Memory-enhancing effects of GEBR-32a, a new PDE4D inhibitor holding promise for the treatment of Alzheimer's disease. Sci Rep. 2017 Apr 12;7:46320. [Content Brief]

[2]. Gurney ME, et al. Design and Synthesis of Selective Phosphodiesterase 4D (PDE4D) Allosteric Inhibitors for the Treatment of Fragile X Syndrome and Other Brain Disorders. J Med Chem. 2019 May 23;62(10):4884-4901. [Content Brief]

Complete Stock Solution Preparation Table

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

Zatolmilast Related Classifications

Neurological Disease

Keywords:

Zatolmilast1606974-33-7BPN14770BPN 14770BPN-14770Phosphodiesterase (PDE)Inhibitorinhibitorinhibit

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Zatolmilast (Synonyms: BPN14770)

Customer Review

Zatolmilast Related Antibodies

2 Publications Citing Use of MCE Zatolmilast

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

View All Phosphodiesterase (PDE) Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Zatolmilast Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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