ChemicalBook > CAS DataBase List > PF 04447943

PF 04447943

Product Name
PF 04447943
CAS No.
1082744-20-4
Chemical Name
PF 04447943
Synonyms
EOS-62041;PF 4447943;PF-04447943;PF 04447943;PF 4447943;PF-4447943;PF04447943; PF 04447943;PF 04447943 - PF 4447943;PF-04447943 >=98% (HPLC);PF-04447943, 10 mM in DMSO;PDE9 Inhibitor, PF-04447943
CBNumber
CB82645148
Molecular Formula
C20H25N7O2
Formula Weight
395.46
MOL File
1082744-20-4.mol
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PF 04447943 Property

Boiling point:
599.8±60.0 °C(Predicted)
Density 
1.52±0.1 g/cm3(Predicted)
storage temp. 
-20C
solubility 
Soluble in DMSO
form 
Off-white solid
pka
7.22±0.60(Predicted)
color 
Light yellow to yellow
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P321Specific treatment (see … on this label).

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
PZ0380
Product name
PF-04447943
Purity
≥98% (HPLC)
Packaging
5 mg
Price
$99.75
Updated
2025/07/31
Sigma-Aldrich
Product number
PZ0380
Product name
PF-04447943
Purity
≥98% (HPLC)
Packaging
25 mg
Price
$423
Updated
2025/07/31
Sigma-Aldrich
Product number
5.38337
Product name
PDE9 Inhibitor, PF-04447943 - CAS 1082744-20-4 - Calbiochem
Packaging
10mg
Price
$253
Updated
2025/07/31
Cayman Chemical
Product number
24299
Product name
PF-04447943
Purity
≥98%
Packaging
1mg
Price
$36
Updated
2024/03/01
Cayman Chemical
Product number
24299
Product name
PF-04447943
Purity
≥98%
Packaging
5mg
Price
$95
Updated
2024/03/01
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PF 04447943 Chemical Properties,Usage,Production

Uses

Edelinontrine (PF-04447943) is a potent inhibitor of human recombinant PDE9A (IC50=12 nM) with >78-fold selectivity, respectively, over other PDE family members (IC50>1000 nM).

Biological Activity

pf-04447943 is a potent and selective inhibitor of pde9 [1].phosphodiesterase 9 (pde9) selectively degrades cgmp and limits the cgmp-mediated signal transduction which occurs following glutamate binding to nmda receptors. pde9 in cortex and hippocampus of rodents and humans play an important role in memory and learning [1].pf-04447943 have high affinity with ki of 2.8, 4.5 and 18 nm for human, rhesus and rat recombinant pde9 respectively and high selectivity for pde9 versus pdes1- 8 and 10 -11. in cultured hippocampal neurons, pf-04447943 (30-100 nm) significantly increased neurite outgrowth and synapse formation. also, pf-04447943 (100 nm) significantly facilitated hippocampal slice ltp evoked by a weak tetanic stimulus [1].in mice model, pf-04447943 (1 mg/kg) significantly reduced the time spent interacting with the female mouse during the second encounter 24 h later compared to the first encounter, which suggested that pf-04447943 enhanced recognition memory. while, pf-04447943 (3 or 10 mg/kg) didn’t change the interaction times for each encounter. these results suggested that pf-04447943 enhanced memory with an inverted u-shaped dose-response efficacy curve [1].

in vivo

Based on i.v. and p.o. dosing, pharmacokinetic studies with Edelinontrine in the rat indicates a Tmax of 0.3 h, T1/2 of 4.9 h, Cl of 21.7 mL/min/kg and an oral bioavailability of 47%. Thirty minutes following oral administration in rats (1-30 mg/kg), Edelinontrine concentrations dose-dependently increase in blood, brain and cerebrospinal fluid (CSF). The brain:plasma exposure ratios 30 min after dosing range from 0.13 at the 1 mg/kg dose to 0.33 at the 30 mg/kg dose. CSF levels are approximately 50% of brain levels. In mice, Edelinontrine (3, 10, 30 mg/kg p.o.) dose-dependently increases plasma and brain concentrations of Edelinontrine while the brain to plasma ratio ranged from 0.26 to 0.7 although this is not entirely dose dependent. CSF cGMP levels increase in a dose-dependent manner from a basal level of 3 pmol/mL to 13.3 pmol/mL (3.5-fold) at the 30 mg/kg dose. CSF cGMP levels also increase in a dose-dependent manner from a basal level of 3 pmol/mL in vehicle treated animals to 13.3 pmol/mL (3.5-fold) at the 30 mg/kg dose. CSF cGMP levels are elevated at all doses tested with a maximal effect of 3.5 fold increase above controls at 30 mg/kg[2].

IC 50

PDE9

References

[1]hutson ph, finger en, magliaro bc, et al. the selective phosphodiesterase 9 (pde9) inhibitor pf-04447943(6-[(3s,4s)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2h-pyran-4-yl)-1,5-dihydro-4h-pyrazolo[3,4-d]pyrimidin-4-one) enhances synaptic plasticity and cognitive function in rodents. neuropharmacology, 2011, 61(4): 665-676.

PF 04447943 Preparation Products And Raw materials

Raw materials

Preparation Products

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PF 04447943 Suppliers

China 61 The Netherlands 1 United States 9 Global 71
Shanghai Boyle Chemical Co., Ltd.
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Dalian Meilun Biotech Co., Ltd.
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0411-62910999 13889544652
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Haoyuan Chemexpress Co., Ltd.
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021-58950125
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(86) 21-58955996
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info@chemexpress.com
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MedChemexpress LLC
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021-58955995
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sales@medchemexpress.cn
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United States
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AdooQ Bioscience CHINA
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025-68650336
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LETOPHARM LIMITED
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+86-21-5106 2861
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sales@letopharm.com
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Shanghai Zhongjun Pharma Co., Ltd.
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Mob.:17717392686
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SPIRO PHARMA
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Codow Chemical Co.,Ltd.
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18620099427
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+86-20-62619665
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amy@howeipharm.com
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Shanghai EFE Biological Technology Co., Ltd.
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021-65675885 18964387627
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1082744-20-4, PF 04447943Related Search:

3-(5-fluoro-indol-3-yl)-pyrrolidine-2,5-dione PF-06882961 PF-06650833 PF-06873600 PF-06700841 tosylate

  • PF 04447943
  • PF-04447943
  • 1,5-Dihydro-6-[(3S,4S)-4-methyl-1-(2-pyrimidinylmethyl)-3-pyrrolidinyl]-1-(tetrahydro-2H-pyran-4-yl)-4H-pyrazolo[3,4-d]pyrimidin-4-one
  • PF 4447943
  • 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(oxan-4-yl)-2H-pyrazolo[3,4-d]pyrimidin-4-one
  • EOS-62041
  • 6-((3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl)-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
  • PF 4447943;PF-4447943
  • PF04447943; PF 04447943
  • PDE9 Inhibitor, PF-04447943 - CAS 1082744-20-4 - Calbiochem
  • PF 04447943 - PF 4447943
  • 4H-Pyrazolo[3,4-d]pyrimidin-4-one, 1,5-dihydro-6-[(3S,4S)-4-methyl-1-(2-pyrimidinylmethyl)-3-pyrrolidinyl]-1-(tetrahydro-2H-pyran-4-yl)-
  • PF-04447943 >=98% (HPLC)
  • (tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-one
  • PF-04447943, 10 mM in DMSO
  • PDE9 Inhibitor, PF-04447943
  • 1082744-20-4