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PF-05180999 (Synonyms: PF-999)

Catalog No.GC30828

A PDE2A inhibitor

Products are for research use only. Not for human use. We do not sell to patients.

PF-05180999 Chemical Structure

Cas No.: 1394033-54-5

Size Price Stock Qty
10mM (in 1mL DMSO)
$81.00
In stock
5mg
$73.00
In stock
10mg
$129.00
In stock
25mg
$267.00
In stock
50mg
$450.00
In stock
100mg
$809.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Animal experiment:

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].

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.

Background

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

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 Kis 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].

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].

[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.

Chemical Properties

Cas No. 1394033-54-5 SDF
Synonyms PF-999
Canonical SMILES CC1=NC(C2=C(C3=CC=C(C(F)(F)F)C=N3)N(C)N=C2)=C4N1N=CN=C4N5CCC5
Formula C19H17F3N8 M.Wt 414.39
Solubility DMSO : 50 mg/mL (120.66 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Average Rating: 5 ★★★★★ (Based on Reviews and 1 reference(s) in Google Scholar.)

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