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PF-05180999

Catalog No. T16484 CAS 1394033-54-5

PF-05180999 is an inhibitor of phosphodiesterase 2A (IC50: 1.6 nM).

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PF-05180999, CAS 1394033-54-5

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	PF-05180999 is an inhibitor of phosphodiesterase 2A (IC50: 1.6 nM).
Targets&IC50	PDE11A4:26.969 μM, PDE7B:50.09 μM, PDE2A:1.6 nM, PDE10A1:2.03 μM
In vitro	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. PF-05180999 binds to the rat, dog and monkey PDE2A (Kis: 4.2, 8.4, and 5.5 nM and IC50s: 2.6, 5.2, and 3.4 nM, respectively). PF-05180999 displays 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 [1].
In vivo	PF-05180999 induces 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. PF-05180999 (0.032-0.32 mg/kg mg/kg, s.c.) dramatically decreases the working memory errors produced by ketamine in a working memory radial arm maze (RAM) model in rats [1].

Molecular Weight	414.39
Formula	C19H17F3N8
CAS No.	1394033-54-5

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 50 mg/mL (120.66 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

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.

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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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

PF-05180999 1394033-54-5 Metabolism PDE PF 05180999 PF05180999 Inhibitor inhibitor inhibit

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