Cat. No.: HY-16900

Rolipram

(Synonyms: (R,S)-Rolipram; (±)-Rolipram; ZK 62711)

19 Cited Publications

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Based on 19 publication(s) in Google Scholar

Rolipram is a PDE4 inhibitor, with blood-brain barrier permeability, that reverses β-amyloid-induced learning and memory impairment in rats. Rolipram elevates intracellular cAMP and clevels and regulates the cAMP/CREB signaling pathway, thereby alleviating neuroinflammation and apoptotic responses. Rolipram promotes neuronal differentiation of human bone marrow mesenchymal stem cells and inhibits Methamphetamine- and morphine-induced hyperlocomotion in mice. Rolipram also reduces the viability of glioblastoma stem-like cells and enhances Bevacizumab (HY-P9906)-induced cell death. Rolipram inhibits the expression of proinflammatory cytokines and enhances central noradrenergic transmission. Rolipram is mainly used in studies related to various central nervous system diseases including Alzheimer's disease, major depressive disorder, glioblastoma multiforme, and multiple sclerosis.

For research use only. We do not sell to patients.

Purity: 99.87%
CAS No.: 61413-54-5
Formula: C₁₆H₂₁NO₃
Molecular Weight:275.35

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Rolipram Chemical Structure

CAS No.: 61413-54-5

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (19)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
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Bioz

Biological Activity

Description

IC₅₀ & Target

PDE4

All HIV Isoforms :

All Phosphodiesterase (PDE) Isoforms :

All Epigenetic Reader Domain Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	>100 μM Compound: Rol	Antiproliferative activity against human A549 cells after 48 hrs by MTT assay Antiproliferative activity against human A549 cells after 48 hrs by MTT assay	[PMID: 34311158]
COS-7	IC₅₀	105 nM Compound: rolipram	Inhibition of PDE4B2 expressed in COS7 cells assessed as cAMP hydrolysis Inhibition of PDE4B2 expressed in COS7 cells assessed as cAMP hydrolysis	[PMID: 18222088]
HEK293	EC₅₀	0.16 μM Compound: Rolipram	Inhibition of PDE4B1 (unknown origin) transfected in HEK293 cells assessed as forskolin-induced cAMP accumulation pretreated for 30 mins before forskolin challenge by luciferase reporter gene assay Inhibition of PDE4B1 (unknown origin) transfected in HEK293 cells assessed as forskolin-induced cAMP accumulation pretreated for 30 mins before forskolin challenge by luciferase reporter gene assay	10.1039/C2MD00273F
HEK293	EC₅₀	0.22 μM Compound: Rolipram	Inhibition of PDE4B expressed in HEK293 cells assessed as fold reduction in forskolin-stimulated cAMP production pretreated for 30 mins measured 4 hrs after forskolin challenge by luciferase reporter gene assay Inhibition of PDE4B expressed in HEK293 cells assessed as fold reduction in forskolin-stimulated cAMP production pretreated for 30 mins measured 4 hrs after forskolin challenge by luciferase reporter gene assay	[PMID: 22386978]
HEK293	EC₅₀	0.67 μM Compound: Rolipram	Inhibition of PDE4D3 (unknown origin) transfected in HEK293 cells assessed as forskolin-induced cAMP accumulation pretreated for 30 mins before forskolin challenge by luciferase reporter gene assay Inhibition of PDE4D3 (unknown origin) transfected in HEK293 cells assessed as forskolin-induced cAMP accumulation pretreated for 30 mins before forskolin challenge by luciferase reporter gene assay	10.1039/C2MD00273F
HEK293	EC₅₀	131.5 nM Compound: 1	Inhibition of PDE4 expressed in HEK293 cells coexpressing G-protein coupled receptor and cyclic nucleotide gated ion channel by fluorescence assay Inhibition of PDE4 expressed in HEK293 cells coexpressing G-protein coupled receptor and cyclic nucleotide gated ion channel by fluorescence assay	[PMID: 19464886]
HEK293	EC₅₀	2.62 μM Compound: Rolipram	Inhibition of PDE4A4 (unknown origin) transfected in HEK293 cells assessed as forskolin-induced cAMP accumulation pretreated for 30 mins before forskolin challenge by luciferase reporter gene assay Inhibition of PDE4A4 (unknown origin) transfected in HEK293 cells assessed as forskolin-induced cAMP accumulation pretreated for 30 mins before forskolin challenge by luciferase reporter gene assay	10.1039/C2MD00273F
MCF7	IC₅₀	>100 μM Compound: Rol	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 34311158]
NCI-H460	IC₅₀	>100 μM Compound: Rol	Antiproliferative activity against human NCI-H460 cells after 48 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells after 48 hrs by MTT assay	[PMID: 34311158]
PBMC	EC₅₀	0.13 μM Compound: rolipram	Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha production after 24 hrs by ELISA Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha production after 24 hrs by ELISA	[PMID: 22891752]
PBMC	IC₅₀	>30 μM Compound: IV	Cytotoxicity against human PBMC by MTS assay Cytotoxicity against human PBMC by MTS assay	[PMID: 29173945]
PBMC	IC₅₀	0.13 μM Compound: Rolipram	Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha production after 24 hrs by ELISA Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha production after 24 hrs by ELISA	[PMID: 29432948]
PBMC	IC₅₀	0.15 μM Compound: Rolipram	Inhibition of LPS stimulated Tumor Necrosis Factor-alpha (TNF-alpha) release by human PBMC Inhibition of LPS stimulated Tumor Necrosis Factor-alpha (TNF-alpha) release by human PBMC	[PMID: 9873600]
PBMC	IC₅₀	0.16 μM Compound: Rolipram	Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha release in after 24 hrs by FACS Array analysis Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha release in after 24 hrs by FACS Array analysis	[PMID: 19303290]
PBMC	IC₅₀	0.23 μM Compound: Rolipram	Antiinflammatory activity in human PBMC assessed as inhibition of phytohemagglutininin-induced IFN-gamma release after 24 hrs by FACSArray analysis Antiinflammatory activity in human PBMC assessed as inhibition of phytohemagglutininin-induced IFN-gamma release after 24 hrs by FACSArray analysis	[PMID: 19303290]
PBMC	IC₅₀	0.23 μM Compound: Rolipram	Antiinflammatory activity in human PBMC assessed as inhibition of phytohemagglutininin-induced IL2 release after 24 hrs by FACS Array analysis Antiinflammatory activity in human PBMC assessed as inhibition of phytohemagglutininin-induced IL2 release after 24 hrs by FACS Array analysis	[PMID: 19303290]
PBMC	IC₅₀	0.27 μM Compound: Rolipram	Inhibition of LPS-induced TNF-alpha production in human PBMC Inhibition of LPS-induced TNF-alpha production in human PBMC	[PMID: 24852119]
PBMC	IC₅₀	0.27 μM Compound: Rolipram	Inhibition of LPS-induced TNF-alpha production in rat PBMC Inhibition of LPS-induced TNF-alpha production in rat PBMC	[PMID: 24852119]
PBMC	IC₅₀	0.5 μM Compound: Rolipram	Antiinflammatory activity in human PBMC assessed as inhibition of phytohemagglutininin-induced IL5 release after 48 hrs by FACS Array analysis Antiinflammatory activity in human PBMC assessed as inhibition of phytohemagglutininin-induced IL5 release after 48 hrs by FACS Array analysis	[PMID: 19303290]
PBMC	IC₅₀	0.5 μM Compound: 1	Inhibition of TNF-alpha release from LPS-stimulated human mononuclear cells Inhibition of TNF-alpha release from LPS-stimulated human mononuclear cells	[PMID: 9784096]
PBMC	IC₅₀	0.88 μM Compound: Rolipram	Antiinflammatory activity in human PBMC assessed as inhibition of phytohemagglutininin-induced IL10 release after 48 hrs by FACS Array analysis Antiinflammatory activity in human PBMC assessed as inhibition of phytohemagglutininin-induced IL10 release after 48 hrs by FACS Array analysis	[PMID: 19303290]
PBMC	IC₅₀	10.85 μM Compound: 1	Inhibition of LPS-induced TNFalpha production in human PBMC pre-incubated for 30 mins before LPS stimulation for 18 hrs by TR-FRET assay Inhibition of LPS-induced TNFalpha production in human PBMC pre-incubated for 30 mins before LPS stimulation for 18 hrs by TR-FRET assay	[PMID: 28888661]
PBMC	IC₅₀	12.5 μM Compound: Rolipram	Anti-inflammatory activity in human PBMC assessed as suppression of LPS-induced TNF-alpha release preincubated for 30 mins followed by LPS stimulation for 18 hrs by TR-FRET assay Anti-inflammatory activity in human PBMC assessed as suppression of LPS-induced TNF-alpha release preincubated for 30 mins followed by LPS stimulation for 18 hrs by TR-FRET assay	[PMID: 27289320]
PBMC	IC₅₀	18.6 μM Compound: Rolipram	Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha secretion preincubated for 30 mins followed by LPS stimulation for 18 hrs by TR-FRET assay Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha secretion preincubated for 30 mins followed by LPS stimulation for 18 hrs by TR-FRET assay	[PMID: 28196708]
PBMC	IC₅₀	60 nM Compound: Rolipram	Inhibition of LPS-induced TNFalpha production in human PBMC Inhibition of LPS-induced TNFalpha production in human PBMC	[PMID: 19049349]
RAW264.7	IC₅₀	0.19 μM Compound: Rolipram	Inhibition of LPS-induced TNFalpha production in mouse RAW264.7 cells pretreated for 30 mins before LPS challenge by ELISA assay Inhibition of LPS-induced TNFalpha production in mouse RAW264.7 cells pretreated for 30 mins before LPS challenge by ELISA assay	10.1039/C2MD00273F
Sf21	IC₅₀	>100 μM Compound: 7	Inhibition of His-tagged catalytic domain Trypanosoma brucei brucei PDEB1 expressed in baculovirus infected insect Sf21 cells Inhibition of His-tagged catalytic domain Trypanosoma brucei brucei PDEB1 expressed in baculovirus infected insect Sf21 cells	[PMID: 22023548]
Sf21	IC₅₀	95 nM Compound: 1	Inhibition of human full length PDE4A4 expressed in baculovirus infected sf21 cells Inhibition of human full length PDE4A4 expressed in baculovirus infected sf21 cells	[PMID: 23806553]
Sf9	IC₅₀	0.092 μM Compound: rolipram	Inhibition of human recombinant PDE4D expressed in Sf9 cells Inhibition of human recombinant PDE4D expressed in Sf9 cells	[PMID: 19827751]
Sf9	IC₅₀	0.15 μM Compound: 4	Inhibition of human full length N-terminal GST-tagged PDE4B1 expressed in baculovirus infected Sf9 cells using cAMP as substrate incubated for 1 hr by fluorescence polarization assay Inhibition of human full length N-terminal GST-tagged PDE4B1 expressed in baculovirus infected Sf9 cells using cAMP as substrate incubated for 1 hr by fluorescence polarization assay	[PMID: 30822711]
Sf9	IC₅₀	0.3 μM Compound: 4	Inhibition of human N-terminal GST-tagged PDE4D7 (2 to 748 residues) expressed in baculovirus infected Sf9 cells using cAMP as substrate after 1 hr by fluorescence polarization assay Inhibition of human N-terminal GST-tagged PDE4D7 (2 to 748 residues) expressed in baculovirus infected Sf9 cells using cAMP as substrate after 1 hr by fluorescence polarization assay	[PMID: 30822711]
Sf9	IC₅₀	0.94 μM Compound: Rolipram	Inhibition of recombinant His-tagged human PDE4B expressed in Sf9 cells using cAMP as substrate preincubated with enzyme for 15 mins followed by substrate addition and incubated for 1 hr by PDELight HTS cAMP phosphodiesterase Kit based luminometry Inhibition of recombinant His-tagged human PDE4B expressed in Sf9 cells using cAMP as substrate preincubated with enzyme for 15 mins followed by substrate addition and incubated for 1 hr by PDELight HTS cAMP phosphodiesterase Kit based luminometry	[PMID: 31035240]
Sf9	IC₅₀	0.94 μM Compound: Rolipram	Inhibition of His-tagged recombinant human PDE4B1 expressed in baculovirus infected sf9 cells using cAMP as substrate preincubated for 15 mins followed by substrate addition measured after 1 hr by luminescence assay Inhibition of His-tagged recombinant human PDE4B1 expressed in baculovirus infected sf9 cells using cAMP as substrate preincubated for 15 mins followed by substrate addition measured after 1 hr by luminescence assay	10.1039/C2MD00273F
Sf9	IC₅₀	0.941 μM Compound: Rolipram	Inhibition of PDE4B1 (unknown origin) expressed in sf9 cells using cAMP as substrate preincubated for 15 mins before substrate addition measured after 1 hr by luminescence assay Inhibition of PDE4B1 (unknown origin) expressed in sf9 cells using cAMP as substrate preincubated for 15 mins before substrate addition measured after 1 hr by luminescence assay	[PMID: 23415088]
Sf9	IC₅₀	1 μM Compound: Rolipram	Inhibition of recombinant His-tagged PDE4B (unknown origin) expressed in Sf9 cells using cAMP as substrate incubated for 15 mins prior to substrate addition measured after 1 hr by luminescence-based assay Inhibition of recombinant His-tagged PDE4B (unknown origin) expressed in Sf9 cells using cAMP as substrate incubated for 15 mins prior to substrate addition measured after 1 hr by luminescence-based assay	[PMID: 23380174]
Sf9	IC₅₀	1.03 μM Compound: Rolipram	Inhibition of recombinant human PDE4B expressed in baculovirus infected Sf9 cells using [3H] cAMP as substrate after 30 min by scintillation proximity assay Inhibition of recombinant human PDE4B expressed in baculovirus infected Sf9 cells using [3H] cAMP as substrate after 30 min by scintillation proximity assay	[PMID: 32209292]
Sf9	IC₅₀	2.3 μM Compound: Rolipram	Inhibition of human recombinant PDE4 catalytic domain expressed in baculovirus-infected insect Sf9 cells by modified two-step method Inhibition of human recombinant PDE4 catalytic domain expressed in baculovirus-infected insect Sf9 cells by modified two-step method	[PMID: 19303290]
Sf9	IC₅₀	288 nM Compound: CHEMBL63	Inhibition of recombinant human PDE4D7 catalytic domain expressed in baculovirus infected sf9 cells using cAMP as substrate Inhibition of recombinant human PDE4D7 catalytic domain expressed in baculovirus infected sf9 cells using cAMP as substrate	[PMID: 26908025]
Sf9	IC₅₀	4 nM Compound: 1	Inhibition of recombinant human PDE4A expressed in Sf9 cells Inhibition of recombinant human PDE4A expressed in Sf9 cells	[PMID: 11052785]
T-cell	IC₅₀	>10 μM Compound: Rolipram	Inhibitory concentration against T cell proliferation using concanavalin A stimulated mice spleen cells Inhibitory concentration against T cell proliferation using concanavalin A stimulated mice spleen cells	[PMID: 11229767]
U-251	IC₅₀	>100 μM Compound: Rol	Antiproliferative activity against human U-251 cells after 48 hrs by MTT assay Antiproliferative activity against human U-251 cells after 48 hrs by MTT assay	[PMID: 34311158]
U-937	EC₅₀	1.23 μM Compound: Rolipram	Arbitary maximal response for cAMP elevation from baseline level was evaluated in Human U-937 cells Arbitary maximal response for cAMP elevation from baseline level was evaluated in Human U-937 cells	[PMID: 9632360]
U-937	EC₅₀	1100 nM Compound: 1, Rolipram	cAMP elevation in U937 cells cAMP elevation in U937 cells	[PMID: 16263279]
U-937	IC₅₀	0.4 μM Compound: Rolipram	Inhibition of phosphodiesterase 4 from U937 cells Inhibition of phosphodiesterase 4 from U937 cells	[PMID: 9873600]
U-937	IC₅₀	0.41 μM Compound: rolipram	Inhibition of PDE4 from human U937 cells Inhibition of PDE4 from human U937 cells	[PMID: 19827751]
U-937	IC₅₀	0.86 μM Compound: Rolipram	Inhibition of PDE4 in human U937 cells assessed as accumulation of [3H]adenosine by scintillation counting Inhibition of PDE4 in human U937 cells assessed as accumulation of [3H]adenosine by scintillation counting	[PMID: 19303290]
U-937	IC₅₀	0.93 μM Compound: Rolipram	Inhibition of phosphodiesterase type 4 isozyme (PDE4) from the U937 human cell line. Inhibition of phosphodiesterase type 4 isozyme (PDE4) from the U937 human cell line.	[PMID: 11123995]
U-937	IC₅₀	1.12 μM Compound: Rolipram	Anti-inflammatory activity in human U937 cells assessed as inhibition of LPS-induced TNFalpha production pre-incubated for 1 hr before LPS stimulation for 24 hrs by ELISA method Anti-inflammatory activity in human U937 cells assessed as inhibition of LPS-induced TNFalpha production pre-incubated for 1 hr before LPS stimulation for 24 hrs by ELISA method	[PMID: 28927905]
U-937	IC₅₀	1.17 μM Compound: Rolipram	Anti-inflammatory activity in human U937 cells assessed as inhibition of LPS-induced IL6 production pre-incubated for 1 hr before LPS stimulation for 24 hrs by ELISA method Anti-inflammatory activity in human U937 cells assessed as inhibition of LPS-induced IL6 production pre-incubated for 1 hr before LPS stimulation for 24 hrs by ELISA method	[PMID: 28927905]
U-937	IC₅₀	1.23 μM Compound: 1	Ability to elevate intracellular levels of cAMP in human U937 cells Ability to elevate intracellular levels of cAMP in human U937 cells	10.1016/S0960-894X(97)00097-8
U-937	IC₅₀	1.3 μM Compound: 1	Inhibition of PDE4B isolated from human U937 cells using [3H]-cAMP as substrate after 30 mins Inhibition of PDE4B isolated from human U937 cells using [3H]-cAMP as substrate after 30 mins	[PMID: 26320621]
U-937	IC₅₀	3.5 μM Compound: Rolipram	Inhibition of Phosphodiesterase 4 from human U937 cells Inhibition of Phosphodiesterase 4 from human U937 cells	[PMID: 10999488]
U-937	IC₅₀	3.5 μM Compound: Rolipram	Inhibition of human phosphodiesterase 4 from U937 cells Inhibition of human phosphodiesterase 4 from U937 cells	[PMID: 11814830]
U-937	IC₅₀	3.5 μM Compound: Rolipram	Inhibition of Phosphodiesterase 4 (PDE-4) from human U937 cells Inhibition of Phosphodiesterase 4 (PDE-4) from human U937 cells	[PMID: 12039574]
U-937	IC₅₀	880 nM Compound: (+/-)-Rolipram	Inhibition of PDE4 isolated from human U937 cells using [3H]-cAMP as substrate after 30 mins by liquid scintillation counting analysis Inhibition of PDE4 isolated from human U937 cells using [3H]-cAMP as substrate after 30 mins by liquid scintillation counting analysis	10.1039/C0MD00215A

In Vitro

Rolipram (0.5-25 μM; 6-24 h) upregulates the expression of neural precursor cell genes in hBM-MSCs in a dose- and time-dependent manner, with the maximal effect observed at 1 μM for 12 h^[2].
Rolipram (1-25 μM; 12 h) shows no toxicity to hBM-MSCs at concentrations ≤5 μM, but induces significant cytotoxicity at 10 μM and 25 μM^[2].
Rolipram (1 μM; 12 h) significantly increases the neuronal differentiation rate, neurite length, and neurite number of hBM-MSCs following neuronal induction^[2].
Rolipram (1 μM; 12 h) enhances neuron-specific gene expression and suppresses non-neuronal lineage gene expression in hBM-MSCs following neuronal induction^[2].
Treatment with Rolipram (10 μM; 48 h) alone reduces the viability of CD133+/CD15+ human glioma stem cells (T2), and its cytotoxic effect is stronger when used in combination with bevacizumab than when either drug is used alone^[4].
Rolipram downregulates antigen-driven proliferation and the gene expression of IL-5 and IFN-γ in human peripheral blood mononuclear cells, but does not affect the gene expression of IL-4^[5].

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

In Vivo

Rolipram (0.1-0.5 mg/kg; i.p.; once daily; 24 days) dose-dependently reverses Aβ25-35-induced learning and long-term memory deficits in rats, alongside reversing associated hippocampal reductions in pCREB and Bcl-2, and increases in NF-κB p65 and Bax^[1].
Rolipram (0.5 mg/kg; i.p.; once daily; 14 days) reverses Aβ1-42-induced hippocampal changes in pCREB, NF-κB p65, Bcl-2, and Bax in rats, confirming effects observed with Aβ25-35^[1].
Rolipram (1.0-10 mg/kg; i.p.; single dose; 15 minutes pre-methamphetamine) significantly suppresses methamphetamine-induced hyperlocomotion in male ddY mice, with 10 mg/kg producing nearly complete inhibition^[3].
Rolipram (10-100 mg/kg/day; p.o.; daily; 5-14 days) induces dose-dependent toxic effects in female rats, including cardiac, vascular, gastrointestinal, and salivary gland changes, with lethal effects at 100 mg/kg/day within 5 days^[5].
Rolipram (0.02-400 mg/kg; systemic; single dose) induces a characteristic behavioral syndrome and mild hypothermia in rats, with effects linked to enhanced central adrenergic signal transduction^[5].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 61413-54-5
Appearance Solid
Molecular Weight 275.35
Formula C₁₆H₂₁NO₃
Color White to off-white
SMILES

O=C1NCC(C2=CC=C(OC)C(OC3CCCC3)=C2)C1
Synonyms

(R,S)-Rolipram; (±)-Rolipram; ZK 62711
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (19)

All In Vivo Efficacy StudyWBIHCBio/Physico-chemical AssayHistological Imaging/Staining

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Journal Impact Factor

Acta Pharmacol Sin

PDE4 inhibitor rolipram dynamically regulates the balance between D1-MSNs and D2-MSNs in the DMS to modulate abnormal "Go" behavior associated with alcohol addiction. [Abstract]

2026 Feb 6. PMID: 41652074
Acta Pharmacol Sin

In situ reprogramming of cardiac fibroblasts into cardiomyocytes in mouse heart with chemicals. [Abstract]

2024 Nov;45(11):2290-2299. PMID: 38890526

Rolipram purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Nov;45(11):2290-2299. [Abstract]

Schemes of generating Fsp1-Cre:R26R-loxp-tdTomato mice and drug treatment to induce in situ transdifferentiation. Fsp1-Cre mice were crossed with R26Rloxp-tdTomato mice in which the expression of tdTomato is prevented by a loxP-flanked STOP cassette. The F1 mice would have the red fluorescent protein tdTomato expressed specifically in the fibroblasts. CRFVPTM were given once a week for 6 weeks. Immunofluorescence staining of the cryosections of the hearts from Fsp1-Cre:R26R-loxp-tdTomato mice treated with vehicle (b) or CRFVPTM (c) for 6 weeks. C: CHIR99021, 14 mg/kg; R: RepSox, 8.6 mg/kg; F: Forskolin, 61.6 mg/kg; V: VPA, 250 mg/kg; T: TTNPB, 1 mg/kg and M: Rolipram, 2.5 mg/kg; P: Parnate, 2.7 mg/kg, CRFTM by oral gavage and VP by intraperitoneal injection once a week for 6 weeks in mice at about 8 weeks of age.

Rolipram purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Nov;45(11):2290-2299. [Abstract]

Whole-heart imaging with light-sheet fluorescence microscopy after tissue clearing of the hearts from Fsp1-Cre:R26R-loxp-tdTomato mice treated with vehicle (a) or CRFVPTM (b). (C: CHIR99021, 14 mg/kg; R: RepSox, 8.6 mg/kg; F: Forskolin, 61.6 mg/kg; V: VPA, 250 mg/kg; T: TTNPB, 1 mg/kg and M: Rolipram, 2.5 mg/kg; P: Parnate, 2.7 mg/kg, CRFTM by oral gavage and VP by intraperitoneal injection once a week for 6 weeks in mice at about 8 weeks of age).

Rolipram purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Nov;45(11):2290-2299. [Abstract]

a Schemes of obtaining PDGFRα-DreER:R26R-rox-tdTomato mice and drug treatment to induce in situ cardiac reprogramming in PDGFRα-DreER:R26R-roxtdTomato mice. PDGFRα-DreER mice were mated with R26R-rox-tdTomato mice in which the expression of tdTomato is prevented by a roxflanked STOP cassette. The expression of tdTomato in fibroblasts was turned on by tamoxifen treatment. CRFVPTM were given once a week for 6 weeks. b Body weigh change of the mice after chemical treatment. Immunofluorescence staining of the cryosections of the hearts from PDGFRα-DreER:R26R-rox-tdTomato mice treated with vehicle (c) or CRFVPTM (d) for 6 weeks. (C: CHIR99021, 14 mg/kg; R: RepSox, 8.6 mg/kg; F: Forskolin, 61.6 mg/kg; V: VPA, 250 mg/kg; T: TTNPB, 1 mg/kg and M: Rolipram, 2.5 mg/kg; P: Parnate, 2.7 mg/kg, CRFTM by oral gavage and VP by intraperitoneal injection once a week for 6 weeks in mice at about 8 weeks of age).

Rolipram purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Nov;45(11):2290-2299. [Abstract]

Immunofluorescence staining of α-actinin in cryosections of hearts from Fsp1-Cre:R26R-loxp-tdTomato mice treated with 7 C cocktail (CRFVPTM) or cocktails by removing 1 compound from 7 C (7C-X) for 6 weeks in vivo with Fsp1-Cre:R26R-loxp-tdTomato mice. (C: CHIR99021, 14 mg/kg; R: RepSox, 8.6 mg/kg; F: Forskolin, 61.6 mg/kg; V: VPA, 250 mg/kg; T: TTNPB, 1 mg/kg and M: Rolipram, 2.5 mg/kg; P: Parnate, 2.7 mg/kg, CRFTM by oral gavage and VP by intraperitoneal injection once a week for 6 weeks in mice at about 8 weeks of age).
Phytomedicine

Lycorine, a natural alkaloid, promotes the degradation of alpha-synuclein via PKA-mediated UPS activation in transgenic Parkinson's disease models. [Abstract]

2021 Jul:87:153578. PMID: 34038839

Rolipram purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2021 Jul:87:153578. [Abstract]

PC12 cells were transiently transfected with empty vector or WT α-syn plasmid for 36 h followed by 10 μM, 20 μM Rolipram or 1 μM Lycorine treatment for another 6 h in the presence of cycloheximide (50 μg/mL). Expression levels of phospho-(Ser/Thr) PKA substrates and α-syn were analyzed by western blot.
Biomed Pharmacother

Targeting hypoxia in combination with paclitaxel to enhance therapeutic efficacy in breast and ovarian cancer. [Abstract]

2024 Oct 29:180:117601. PMID: 39476764
Cell Rep

Enforced activation of the CREB/KDM2B axis prevents alcohol-induced embryonic developmental delay. [Abstract]

2024 Dec 10;43(12):115075. PMID: 39661511

Rolipram purchased from MedChemExpress. Usage Cited in: Cell Rep. 2024 Dec 10;43(12):115075. [Abstract]

Rolipram (2.5–5 mg/kg; i.p.; once daily for 3 days) significantly reversed the reductions in embryonic volume and weight caused by 50% ethanol exposure when embryos were harvested at E6.5.

Rolipram purchased from MedChemExpress. Usage Cited in: Cell Rep. 2024 Dec 10;43(12):115075. [Abstract]

Rolipram (2.5-5 mg/kg; i.p.; once daily for 3 days) prevented the decrease of CREB activity induced by ethanol exposure.
Cell Rep

Neuronal activity recruits the CRTC1/CREB axis to drive transcription-dependent autophagy for maintaining late-phase LTD. [Abstract]

2021 Jul 20;36(3):109398. PMID: 34289350
Sci Signal

Airway relaxation mechanisms and structural basis of osthole for improving lung function in asthma. [Abstract]

2020 Nov 24;13(659):eaax0273. PMID: 33234690

Rolipram purchased from MedChemExpress. Usage Cited in: Sci Signal. 2020 Nov 24;13(659):eaax0273. [Abstract]

VASP phosphorylation in human ASM cells stimulated without (control) or with Osthole (3 μM), Rolipram (Roli; 3 μM), Pimobendane (Pimo; 3 μM), PF-04957325 (PF-049; 0.1 μM), and combinations of two drugs as indicated for 15 min.

Rolipram purchased from MedChemExpress. Usage Cited in: Sci Signal. 2020 Nov 24;13(659):eaax0273. [Abstract]

Inhibition of the enzymatic activity of PDE4D5-S126D by osthole or 10 μM Rolipram (20 min).
Life Sci

Targeting Epac1 to protect the blood brain barrier from inflammation-induced dysfunction: Evidence from an in vitro model. [Abstract]

2025 Oct 14:382:124022. PMID: 41101634
PLoS Pathog

PDE4B deficiency aids macrophage differentiation and contributes to Cryptococcus neoformans brain infection. [Abstract]

2026 Mar 10;22(3):e1014040. PMID: 41805786
Front Pharmacol

East Indian Sandalwood Oil Is a Phosphodiesterase Inhibitor: A New Therapeutic Option in the Treatment of Inflammatory Skin Disease. [Abstract]

2018 Mar 9:9:200. PMID: 29593534
Antiviral Res

Artesunate inhibits PDE4 leading to intracellular cAMP accumulation, reduced ERK/MAPK signaling, and blockade of influenza A virus vRNP nuclear export. [Abstract]

2023 Jul:215:105635. PMID: 37192683
Int J Neuropsychopharmacol

Inhibition of phosphodiesterase 2 ameliorates post-traumatic stress-induced alcohol intake disorder by regulating cAMP/cGMP signaling. [Abstract]

2022 Nov 17;25(11):936-945. PMID: 36124735
Exp Cell Res

Low PDE4A expression promoted the progression of ovarian cancer by inducing Snail nuclear translocation. [Abstract]

2024 May 24:114100. PMID: 38797258
Appl Biochem Biotechnol

Zoledronic Acid Accelerates ER Stress-Mediated Inflammation by Increasing PDE4B Expression in Bisphosphonate-Related Osteonecrosis of the Jaw. [Abstract]

2024 Oct;196(10):7362-7374. PMID: 38523176
Psychopharmacology (Berl)

Inhibition of phosphodiesterase 2 by Bay 60-7550 decreases ethanol intake and preference in mice. [Abstract]

2018 Aug;235(8):2377-2385. PMID: 29876622
Neurogastroenterol Motil

Effect of phosphodiesterase-4 inhibitor rolipram on colonic hypermotility in water avoidance stress rat model. [Abstract]

2022 Jul;34(7):e14317. PMID: 35037375
bioRxiv

2026 Jan 13.
bioRxiv

2025 April 26.
Methods Mol Biol

Characterizing the Neuron-Glial Interactions by the Co-cultures of Human iPSC-Derived Oligodendroglia and Neurons. [Abstract]

2023:2683:103-111. PMID: 37300770

Solvent & Solubility

In Vitro:

DMSO : 40 mg/mL (145.27 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

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

3.6317 mL

18.1587 mL

36.3174 mL

5 mM

0.7263 mL

3.6317 mL

7.2635 mL

10 mM

0.3632 mL

1.8159 mL

3.6317 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (9.08 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (9.08 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (9.08 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

Cell Assay^[2]

J774 murine macrophages (ATCC) are cultured at 37°C in 5% CO₂ atmosphere in DMEM supplemented with glutamax-1 containing 10% heat-inactivated FBS. For experiments, cells are seeded on 24-well plates at a density of 2×10⁵ cells per well. Cell monolayers are grown for 72 h before the experiments are started. Rolipram, IBMX and BIRB 796 are dissolved in DMSO, and 8-Br-cAMP in HBSS. LPS (10 ng/mL) or the compounds of interest at concentrations indicated or the solvent (DMSO, 0.1% v/v) are added to the cells in fresh culture medium containing 10% FBS and the supplements. Cells are further incubated for the time indicated. The effect of LPS and the tested chemicals on cell viability is evaluated by Cell Proliferation Kit II (XTT)^[2].

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

Animal Administration^[2]

Mice^[2]
Inbred C57BL/6 MKP-1(-/-) mice are used. C57BL/6 mice (20-25 g) are divided into groups of six mice and treated with 200 μL of PBS or Rolipram (100 mg/kg in PBS) by an i.p. injection 2 h before applying carrageenan. Before the administration of carrageenan, the mice are anaesthetized by i.p. injection of 0.5 mg/kg of medetomidine. The mice receive a 30 μL i.d. injection of carrageenan (1.5%, dissolved in normal saline) in one hind paw. The contralateral paw receive 30 μL of saline and it is used as a control. Paw volume is measured before and 3 h after the carrageenan injection with a plethysmometer. Oedema is expressed as a change in paw volume over time.

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (292 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)
- 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)
Handling Instructions (2659 KB)

References

[1]. Wang C, et al. The phosphodiesterase-4 inhibitor rolipram reverses Aβ-induced cognitive impairment and neuroinflammatory and apoptotic responses in rats. Int J Neuropsychopharmacol. 2012;15(6):749-766. [Content Brief]

[2]. Joe IS, et al. PDE4 Inhibition by Rolipram Promotes Neuronal Differentiation in Human Bone Marrow Mesenchymal Stem Cells. Cell Reprogram. 2016;18(4):224-229. [Content Brief]

[3]. Mori T, et al. Effects of rolipram, a selective inhibitor of phosphodiesterase 4, on hyperlocomotion induced by several abused drugs in mice. Jpn J Pharmacol. 2000;83(2):113-118. [Content Brief]

[4]. Ramezani S, et al. Rolipram potentiates bevacizumab-induced cell death in human glioblastoma stem-like cells. Life Sci. 2017;173:11-19. [Content Brief]

[5]. Zhu J, et al. The antidepressant and antiinflammatory effects of rolipram in the central nervous system. CNS Drug Rev. 2001;7(4):387-398. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.6317 mL	18.1587 mL	36.3174 mL	90.7935 mL
	5 mM	0.7263 mL	3.6317 mL	7.2635 mL	18.1587 mL
	10 mM	0.3632 mL	1.8159 mL	3.6317 mL	9.0794 mL
	15 mM	0.2421 mL	1.2106 mL	2.4212 mL	6.0529 mL
	20 mM	0.1816 mL	0.9079 mL	1.8159 mL	4.5397 mL
	25 mM	0.1453 mL	0.7263 mL	1.4527 mL	3.6317 mL
	30 mM	0.1211 mL	0.6053 mL	1.2106 mL	3.0265 mL
	40 mM	0.0908 mL	0.4540 mL	0.9079 mL	2.2698 mL
	50 mM	0.0726 mL	0.3632 mL	0.7263 mL	1.8159 mL
	60 mM	0.0605 mL	0.3026 mL	0.6053 mL	1.5132 mL
	80 mM	0.0454 mL	0.2270 mL	0.4540 mL	1.1349 mL
	100 mM	0.0363 mL	0.1816 mL	0.3632 mL	0.9079 mL

Keywords

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Rolipram

Anti-Infection Compound Library

Epigenetics Compound Library

Metabolism/Protease Compound Library

Neuronal Signaling Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Antiviral Compound Library

CNS-Penetrant Compound Library

Drug Repurposing Compound Library

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Anti-COVID-19 Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Alzheimer's Disease Compound Library

Anti-Blood Cancer Compound Library

Neurodegenerative Disease-related Compound Library

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Transcription Factor-Targeted Library

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Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

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High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

RNA Binding Bioactive Compound Library

3D Diverse Fragment Library

Publications Citing Use of MedChemExpress (MCE) Rolipram

All HIV Isoforms

All Phosphodiesterase (PDE) Isoforms

All Epigenetic Reader Domain Isoforms

Biological Activity

Chemical Information

Publications (19)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Rolipram Related Classifications

Cat. No.: HY-16900