PF-05180999 (Synonyms: PF-999)

Name: PF-05180999
Brand: MedChemExpress
SKU: HY-111371
Rating: 5.0 (1 reviews)

Cat. No.: HY-111371 Purity: 99.97%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

PF-05180999 (PF-999) is a phosphodiesterase 2A (PDE2A) inhibitor, with an IC₅₀ of 1.6 nM.

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

PF-05180999 Chemical Structure

CAS No. : 1394033-54-5

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 88	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 88	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 80	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 140	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 290	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 490	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 880	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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View All Isoforms

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

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

PF-05180999 (PF-999) is a phosphodiesterase 2A (PDE2A) inhibitor, with an IC₅₀ of 1.6 nM.

IC₅₀ & Target^[1]

PDE2A

1.6 nM (IC₅₀)

PDE10A1

2.03 μM (IC₅₀)

PDE11A4

26.969 μM (IC₅₀)

PDE7B

50.09 μM (IC₅₀)

In Vitro

PF-05180999 is a phosphodiesterase 2A (PDE2A) inhibitor, with an IC₅₀ of 1.6 nM. PF-05180999 binds to the rat, dog and monkey PDE2A, with K_is of 4.2, 8.4, and 5.5 nM and IC₅₀s of 2.6, 5.2, and 3.4 nM, respectively. PF-05180999 shows weak activity against PDE, with IC₅₀s of 2.03 μM (PDE10A1), 26.969 μM (PDE7B), 50.09 μM (PDE11A4), and >56.25 μM (PDE1B1, PDE3A1, PDE4D3, PDE5A1, PDE6 (bovine), PDE8B, PDE9A1), respectively. PF-05180999 is also a weak inducer of CYP3A4, and with no direct inhibition of human recombinant cytochrome P450 (CYP) enzymes (1A2, 2B6, 2C8, 2C9, 2C19, 2D6, and 3A) and no induction of CYP1A2^[1].

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

In Vivo

PF-05180999 (Compound 30; 0.032-0.32 mg/kg mg/kg, s.c.) dramatically reduces the working memory errors produced by ketamine in a working memory radial arm maze (RAM) model in rats. PF-05180999 causes acute and exposure-dependent elevation in the accumulation of cGMP bulk levels in the cortex, striatum, and hippocampus, but with no changes in cAMP and the associated downstream phospho-cAMP response element-binding protein (p-CREB) in mice^[1].

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

Clinical Trial

Molecular Weight

414.39

Formula

C₁₉H₁₇F₃N₈

CAS No.

1394033-54-5

Appearance

Solid

Color

White to yellow

SMILES

CC1=NC(C2=C(C3=CC=C(C(F)(F)F)C=N3)N(C)N=C2)=C4N1N=CN=C4N5CCC5

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 (120.66 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	2.4132 mL	12.0659 mL	24.1319 mL
5 mM	0.4826 mL	2.4132 mL	4.8264 mL
10 mM	0.2413 mL	1.2066 mL	2.4132 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)

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: ≥ 2.5 mg/mL (6.03 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 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% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.03 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 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.03 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)

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

Purity: 99.97%

Select Batch:

Data Sheet (279 KB) SDS (420 KB)

COA (256 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Helal CJ, et al. Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate. J Med Chem. 2018 Feb 8;61(3):1001-1018. [Content Brief]

Animal Administration
^[1]

Rats^[1]
Male Sprague-Dawley rats (weighing 250-320 g) under urethane anesthesia at 1.5 g/kg intraperitoneal (ip) are placed in a stereotaxic frame, where craniotomies are performed above the region of the medial prefrontal cortex (mPFC) and ipsilateral (CA)1/subiculum. Body temperature of the rat is maintained at 37°C with an electrical heating pad. The femoral vein is cannulated for administration of test drugs (PF-05180999, etc.). After the conclusion of the experiments animals are euthanized with an iv bolus of urethane^[1].

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

References

[1]. Helal CJ, et al. Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate. J Med Chem. 2018 Feb 8;61(3):1001-1018. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.4132 mL	12.0659 mL	24.1319 mL	60.3296 mL
	5 mM	0.4826 mL	2.4132 mL	4.8264 mL	12.0659 mL
	10 mM	0.2413 mL	1.2066 mL	2.4132 mL	6.0330 mL
	15 mM	0.1609 mL	0.8044 mL	1.6088 mL	4.0220 mL
	20 mM	0.1207 mL	0.6033 mL	1.2066 mL	3.0165 mL
	25 mM	0.0965 mL	0.4826 mL	0.9653 mL	2.4132 mL
	30 mM	0.0804 mL	0.4022 mL	0.8044 mL	2.0110 mL
	40 mM	0.0603 mL	0.3016 mL	0.6033 mL	1.5082 mL
	50 mM	0.0483 mL	0.2413 mL	0.4826 mL	1.2066 mL
	60 mM	0.0402 mL	0.2011 mL	0.4022 mL	1.0055 mL
	80 mM	0.0302 mL	0.1508 mL	0.3016 mL	0.7541 mL
	100 mM	0.0241 mL	0.1207 mL	0.2413 mL	0.6033 mL

PF-05180999 Related Classifications

Neurological Disease

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:

PF-051809991394033-54-5PF-999PF05180999PF 05180999PF999PF 999Phosphodiesterase (PDE)Inhibitorinhibitorinhibit

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PF-05180999 (Synonyms: PF-999)

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PF-05180999 Related Antibodies

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Complete Stock Solution Preparation Table

PF-05180999 Related Classifications

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