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

PF-05180999 

目录号: HY-111371 纯度: 99.57%
产品使用指南

PF-05180999 是一种磷酸二酯酶 2A (PDE2A) 抑制剂,IC50 值为 1.6 nM。

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PF-05180999 Chemical Structure

PF-05180999 Chemical Structure

CAS No. : 1394033-54-5

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥880 In-stock
5 mg ¥800 In-stock
10 mg ¥1400 In-stock
25 mg ¥2900 In-stock
50 mg ¥4900 In-stock
100 mg ¥8800 In-stock
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Description

PF-05180999 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 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].

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].

Clinical Trial
Solvent & Solubility
In Vitro: 

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

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
*Please refer to the solubility information to select the appropriate solvent.
References
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
Molecular Weight

414.39

Formula

C₁₉H₁₇F₃N₈

CAS No.

1394033-54-5

SMILES

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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产品名称:
PF-05180999
目录号:
HY-111371
需求量:

PF-05180999

Cat. No.: HY-111371