Rolipram GMP is Rolipram (HY-16900) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. 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.
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- CAS No.: 61413-54-5
- Formule: C16H21NO3
- Masse moléculaire:275.34
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
IC50: 3 nM (PDE4A), 130 nM (PDE4B), 240 nM (PDE4D)[1]
Rolipram GMP (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 GMP (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 GMP (1 μM; 12 h) significantly increases the neuronal differentiation rate, neurite length, and neurite number of hBM-MSCs following neuronal induction[2].
Rolipram GMP (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 GMP (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 GMP 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.
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Cell Line:human bone marrow-mesenchymal stem cells (hBM-MSCs)
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Concentration:0.5 μM; 1 μM; 5 μM; 25 μM
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Incubation Time:6 h; 12 h; 24 h
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Result:Increased expression of neuroprogenitor genes Nestin and CD133 in a dose-dependent manner at ≤1 μM for 12 h, with peak expression at 1 μM.
Decreased expression of neuroprogenitor genes Nestin and CD133 at 25 μM for 12 h.
Peaked expression of neuroprogenitor genes Nestin and CD133 at 12 h, then declined at 24 h when treated with 1 μM.
Significantly increased expression of neuroprogenitor genes Nestin, Musashi, CD133, GFAP, BDNF, and Syn1 under the optimal condition of 1 μM for 12 h compared to untreated hBM-MSCs.
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Cell Line:human bone marrow-mesenchymal stem cells (hBM-MSCs)
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Concentration:1 μM
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Incubation Time:12 h (pretreatment, followed by neuronal differentiation)
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Result:Showed significantly higher expression of neuronal-specific marker genes CD133, NF-M, MAP-2, KCNH5, SCN3A, and CACNA1A compared to dMSCs.
Exhibited significantly decreased expression of adipogenic (Adiponectin, FABP4), chondrogenic (MMP13), and osteogenic (ALP) marker genes compared to undifferentiated hBM-MSCs, similar to dMSCs.
Rolipram GMP (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 GMP (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 GMP (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 GMP (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.
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Animal Model:Rat[5]
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Dosage:0.02 mg/kg; 400 mg/kg
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Administration:systemic; single dose
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Result:Elicited a head twitch reaction, inhibited spontaneous motility, increased maintenance activity (forepaw shaking, grooming, head twitches), caused vocalization on touch, salivation, increased respiration rate, stimulated the hind limb flexor reflex in the spinal cord, and induced slight hypothermia.
Did not have behavioral effects blocked by cyproheptadine, pizotifen, or phenoxybenzamine.
Chemical Information
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CAS No. 61413-54-5
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Masse moléculaire 275.34
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Formule C16H21NO3
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SMILES
O=C1NCC(C2=CC=C(OC)C(OC3CCCC3)=C2)C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Rolipram (GMP) Related Classifications
HY-16900G Related Classifications
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