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MedKoo Cat#: 462312 | Name: PF-04449613
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

PF-04449613 is a phosphodiesterase 9A (PDE9A) inhibitor. Subcutaneous administration of PF-04449613 (10 mg/kg) increases the rate of dendritic spine formation and elimination in mouse primary motor cortex pyramidal neurons in vivo.

Chemical Structure

PF-04449613
CAS#1236858-52-8

Theoretical Analysis

MedKoo Cat#: 462312

Name: PF-04449613

CAS#: 1236858-52-8

Chemical Formula: C21H25N5O3

Exact Mass: 395.1957

Molecular Weight: 395.46

Elemental Analysis: C, 63.78; H, 6.37; N, 17.71; O, 12.14

Price and Availability

Size Price Availability Quantity
5mg USD 500.00 2 Weeks
10mg USD 915.00 2 Weeks
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Related CAS #
No Data
Synonym
PF-04449613; PF 04449613; PF04449613
IUPAC/Chemical Name
1,5-dihydro-6-[(1R)-1-(3-phenoxy-1-azetidinyl)ethyl]-1-(tetrahydro-2H-pyran-4-yl)-4H-pyrazolo[3,4-d]pyrimidin-4-one
InChi Key
FHBANDDJQJAZOQ-CQSZACIVSA-N
InChi Code
InChI=1S/C21H25N5O3/c1-14(25-12-17(13-25)29-16-5-3-2-4-6-16)19-23-20-18(21(27)24-19)11-22-26(20)15-7-9-28-10-8-15/h2-6,11,14-15,17H,7-10,12-13H2,1H3,(H,23,24,27)/t14-/m1/s1
SMILES Code
O=C1N=C([C@@H](C)N2CC(OC3=CC=CC=C3)C2)NC4=C1C=NN4C5CCOCC5
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
PF-04449613 is a selective PDE9A inhibitor with an IC50 of 22 nM.
In vitro activity:
TBD
In vivo activity:
This study found that administration of PF-04449613 increased calcium activity of dendrites and dendritic spines of layer V pyramidal neurons in mice under resting and running conditions. Chronic treatment of PF-04449613 over weeks increased dendritic spine formation and elimination under basal conditions. Furthermore, PF-04449613 treatment over 1-7 days increased the formation and survival of new spines as well as performance improvement after rotarod motor training. Reference: Dev Neurobiol. 2018 Sep;78(9):859-872. https://pubmed.ncbi.nlm.nih.gov/30022611/
Solvent mg/mL mM comments
Solubility
DMSO 24.8 62.65
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 395.46 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Zhu XJ, Wang YW, Zhang WH, Gao L, Xiao YJ, Gao QW, Wang RR, Chen L. [Positive inotropic effect of phosphodiesterase type 9 inhibitor PF-04449613 in rats and its underlying mechanism]. Sheng Li Xue Bao. 2021 Apr 25;73(2):275-285. Chinese. PMID: 33903889. 2. Lai B, Li M, Hu W, Li W, Gan WB. The Phosphodiesterase 9 Inhibitor PF-04449613 Promotes Dendritic Spine Formation and Performance Improvement after Motor Learning. Dev Neurobiol. 2018 Sep;78(9):859-872. doi: 10.1002/dneu.22623. Epub 2018 Jul 18. PMID: 30022611; PMCID: PMC6158093.
In vitro protocol:
TBD
In vivo protocol:
1. Zhu XJ, Wang YW, Zhang WH, Gao L, Xiao YJ, Gao QW, Wang RR, Chen L. [Positive inotropic effect of phosphodiesterase type 9 inhibitor PF-04449613 in rats and its underlying mechanism]. Sheng Li Xue Bao. 2021 Apr 25;73(2):275-285. Chinese. PMID: 33903889. 2. Lai B, Li M, Hu W, Li W, Gan WB. The Phosphodiesterase 9 Inhibitor PF-04449613 Promotes Dendritic Spine Formation and Performance Improvement after Motor Learning. Dev Neurobiol. 2018 Sep;78(9):859-872. doi: 10.1002/dneu.22623. Epub 2018 Jul 18. PMID: 30022611; PMCID: PMC6158093.
1. Claffey, M.M., Helal, C.J., Verhoest, P.R., et al. Application of structure-based drug design and parallel chemistry to identify selective, brain penetrant, in vivo active phosphodiesterase 9A inhibitors. J. Med. Chem. 55(21), 9055-9068 (2012). 2. Lai, B., Li, M., Hu, A., et al. The phosphodiesterase 9 inhibitor PF-04449613 promotes dendritic spine formation and performance improvement after motor learning. Dev. Neurobiol. 78(9), 859-872 (2018).