Cat. No.: HY-107203

Propentofylline

(Synonyms: HWA 285)

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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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Pureté: 99.88%
CAS No.: 55242-55-2
Formule: C₁₅H₂₂N₄O₃
Masse moléculaire:306.36

Stockage:

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

Propentofylline Chemical Structure

CAS No.: 55242-55-2

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Activité biologique
- Description
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Voir tous les produits spécifiques à Isoform Phosphodiesterase (PDE) :

Voir tous les produits spécifiques à Isoform Adenosine Receptor :

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.

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), A_2a 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.

Chemical Information

CAS No. 55242-55-2
Appearance Solid
Masse moléculaire 306.36
Formule C₁₅H₂₂N₄O₃
Color White to off-white
SMILES

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

HWA 285
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.2641 mL

16.3207 mL

32.6413 mL

5 mM

0.6528 mL

3.2641 mL

6.5283 mL

10 mM

0.3264 mL

1.6321 mL

3.2641 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (281 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Noble S, et al. Propentofylline. CNS Drugs. 1997 Sep;8(3):257-264.

[2]. Parkinson FE, et al. Propentofylline: a nucleoside transport inhibitor with neuroprotective effects in cerebral ischemia. Gen Pharmacol. 1994 Oct;25(6):1053-8. [Content Brief]

[3]. Goto M, et al. Effects of propentofylline on disorder of learning and memory in rodents. Jpn J Pharmacol. 1987 Nov;45(3):373-8. [Content Brief]

[4]. Rother M, et al. Propentofylline in the treatment of Alzheimer's disease and vascular dementia: a review of phase III trials. Dement Geriatr Cogn Disord. 1998;9 Suppl 1:36-43. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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Voir tous les produits spécifiques à Isoform Phosphodiesterase (PDE)

Voir tous les produits spécifiques à Isoform Adenosine Receptor

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Propentofylline Related Classifications

HY-107203 Related Classifications