2. Metabolic Enzyme/Protease GPCR/G Protein
  3. Phosphodiesterase (PDE) Adenosine Receptor
  4. Propentofylline

Propentofylline (HWA 285) is an orally active and brain-penetrant phosphodiesterase inhibitor. Propentofylline blocks adenosine reuptake and prevents cyclic nucleotide degradation. Propentofylline can be used for the research of primary degenerative (Alzheimer's) dementia, vascular dementia, cerebral ischemia, acute stroke, and learning and memory disorders.

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Propentofylline

Propentofylline Chemical Structure

CAS No. : 55242-55-2

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10 mM * 1 mL in DMSO
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Other Forms of Propentofylline:

Propentofylline Related Antibodies

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PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

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Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

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Description

Propentofylline (HWA 285) is an orally active and brain-penetrant phosphodiesterase inhibitor. Propentofylline blocks adenosine reuptake and prevents cyclic nucleotide degradation. Propentofylline can be used for the research of primary degenerative (Alzheimer's) dementia, vascular dementia, cerebral ischemia, acute stroke, and learning and memory disorders[1][2][3][4].

In Vitro

Propentofylline (50 μM) significantly reduces Concanavalin A (HY-P2149)-stimulated reactive oxygen intermediate release from rat peritoneal macrophages and rat microglial cells[1].
Propentofylline dose-dependently inhibits proliferation of cultured neonatal rat brain microglial cells[1].
Propentofylline (0.1-3 mM) increases nerve growth factor synthesis and secretion by cultured mouse astroglial cells by more than 10-fold relative to controls[1].
Propentofylline significantly reduces the release of proinflammatory cytokines from activated human blood mononuclear cells and activated microglial cells[1].
Propentofylline completely inhibits adenosine transport via the es nucleoside transport system in cultured mouse leukemic L1210/B23.1 cells with an IC50 of 9 μM[2].
Propentofylline completely inhibits adenosine transport via the ei nucleoside transport system in cultured mouse leukemic L1210/C2 cells and rat carcinosarcoma Walker 256 cells with an IC50 of 170 μM[2].
Propentofylline completely inhibits adenosine transport via the N1 (cif) nucleoside transport system in cultured mouse leukemic L1210/MA27.1 cells with an IC50 of 6 mM[2].
Propentofylline (10 μM - 1 mM) inhibits [3H] Nitrobenzylthioinosine (HY-W010936) binding to nucleoside transporters in heart and brain tissue[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Propentofylline Related Antibodies
In Vivo

Propentofylline (10 mg/kg; i.p.; daily; 14 days) enhances survival of CA1 pyramidal neurons and reduces ischemia-induced neuronal damage, Ca2+ accumulation, and reactive gliosis in gerbils with global forebrain ischemia[2].
Propentofylline (40 mg/kg/day; p.o.; 4 weeks) does not alter adenosine receptor or es nucleoside transporter binding densities in the brains of normal gerbils[2].
Propentofylline (25 mg/kg; p.o.; daily; 15 days) significantly improves impaired active avoidance learning in aged male SHR rats, without altering blood pressure[3].
Propentofylline (25 mg/kg; p.o.; daily; 14 days) does not alter intact active avoidance learning in aged male WKY rats, and does not affect blood pressure[3].
Propentofylline (3.8-30 mg/kg; i.p.; single dose) significantly improves Cycloheximide (HY-12320)-induced amnesia in male ICR mice, with a dose-related effect[3].
Propentofylline (15-30 mg/kg; i.p.; single dose) significantly prevents Cycloheximide-induced amnesia in male ICR mice[3].
Propentofylline (30 mg/kg; i.p.; single dose) does not alter step-down latency in naive male ICR mice[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mongolian gerbils[2]
Dosage: 10 mg/kg
Administration: i.p.; daily; 14 days
Result: Enhanced survival of CA1 pyramidal neurons in the hippocampus following ischemic injury.
Reduced necrosis of ischemic hippocampal pyramidal cells and inhibited post-ischemic increase of glial fibrillary acidic protein associated with reactive gliosis.
Reduced ischemia-induced neuronal damage and Ca2+ accumulation in the brain.
Animal Model: Mongolian gerbils[2]
Dosage: 40 mg/kg/day
Administration: p.o.; 4 weeks
Result: No changes in binding densities of adenosine A1 receptors (measured via [3H] cyclohexyladenosine), A2a receptors (measured via [3H] CGS 21680), or es nucleoside transporters (measured via [3H] nitrobenzylthioinosine) in brain tissue.
Animal Model: SHR (12-month-old male, spontaneously hypertensive)[3]
Dosage: 25 mg/kg
Administration: p.o.; daily; 15 days
Result: Showed significantly higher numbers of correct avoidance responses than controls at the 10th, 12th, 13th, 14th, and 15th training sessions.
Demonstrated no significant difference in blood pressure compared to control rats after the study.
Animal Model: Wistar-Kyoto (WKY) (12-month-old male)[3]
Dosage: 25 mg/kg
Administration: p.o.; daily; 14 days
Result: Did not affect the number of correct avoidance responses, which increased similarly in treated and control groups from the 6th to 14th sessions.
Demonstrated no significant difference in blood pressure compared to control rats after the study.
Animal Model: ICR (6-week-old male, 30-40 g, cycloheximide-induced amnesia)[3]
Dosage: 3.8 mg/kg; 7.5 mg/kg; 15 mg/kg; 30 mg/kg
Administration: i.p.; single dose
Result: Produced a 10.0% retention rate at 3.8 mg/kg, which did not significantly improve retention compared to the Cycloheximide plus saline group (10.5% retention rate).
Produced a 31.0% retention rate at 7.5 mg/kg, which significantly improved retention compared to the Cycloheximide plus saline group.
Produced a 33.3% retention rate at 15 mg/kg, which significantly improved retention compared to the Cycloheximide plus saline group.
Produced a 40.0% retention rate at 30 mg/kg, which significantly improved retention compared to the Cycloheximide plus saline group.
Animal Model: ICR (6-week-old male, 30-40 g, cycloheximide-induced amnesia)[3]
Dosage: 15 mg/kg; 30 mg/kg
Administration: i.p.; single dose
Result: Produced a 35.1% retention rate at 15 mg/kg, which significantly improved retention compared to the saline plus Cycloheximide group (12.5% retention rate).
Produced a 37.1% retention rate at 30 mg/kg, which significantly improved retention compared to the saline plus Cycloheximide group.
Animal Model: ICR (6-week-old male, 30-40 g)[3]
Dosage: 30 mg/kg
Administration: i.p.; single dose
Result: Demonstrated a mean step-down latency of 7.6 sec, which did not significantly differ from the untreated control latency of 11.8 sec.
Molecular Weight

306.36

Formula

C15H22N4O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C2=C(N(C)C(N1CCCCC(C)=O)=O)N=CN2CCC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (326.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 12.5 mg/mL (40.80 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2641 mL 16.3207 mL 32.6413 mL
5 mM 0.6528 mL 3.2641 mL 6.5283 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.88%

SDS (393 KB)

COA (246 KB) HNMR (257 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 3.2641 mL 16.3207 mL 32.6413 mL 81.6033 mL
5 mM 0.6528 mL 3.2641 mL 6.5283 mL 16.3207 mL
10 mM 0.3264 mL 1.6321 mL 3.2641 mL 8.1603 mL
15 mM 0.2176 mL 1.0880 mL 2.1761 mL 5.4402 mL
20 mM 0.1632 mL 0.8160 mL 1.6321 mL 4.0802 mL
25 mM 0.1306 mL 0.6528 mL 1.3057 mL 3.2641 mL
30 mM 0.1088 mL 0.5440 mL 1.0880 mL 2.7201 mL
40 mM 0.0816 mL 0.4080 mL 0.8160 mL 2.0401 mL
DMSO 50 mM 0.0653 mL 0.3264 mL 0.6528 mL 1.6321 mL
60 mM 0.0544 mL 0.2720 mL 0.5440 mL 1.3601 mL
80 mM 0.0408 mL 0.2040 mL 0.4080 mL 1.0200 mL
100 mM 0.0326 mL 0.1632 mL 0.3264 mL 0.8160 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Propentofylline Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Propentofylline55242-55-2HWA 285HWA285HWA-285Phosphodiesterase (PDE)Adenosine ReceptorP1 receptoradenosine transportermouse leukemic L1210/B23.1 cellscyclic nucleotide phosphodiesteraseadenosine receptorhuman blood mononuclear cellsmouse astroglial cellsrat peritoneal macrophagesrat hippocampal neuronsrat carcinosarcoma Walker 256 cellsmicroglial cellsInhibitorinhibitorinhibit

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