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S-(+)-Rolipram PDE inhibitor

Name: S-(+)-Rolipram
Brand: Selleck Chemicals
SKU: S2127
Rating: 5 (1 reviews)

Cat.No.S2127

S-(+)-Rolipram inhibits human monocyte cyclic AMP-specific PDE4 with an IC50 of 0.75 μM, has anti-inflammatory and anti-depressant activity in the central nervous system, less potent than its R enantiomer.

Chemical Structure

Molecular Weight: 275.34

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Quality Control

Batch: S212701 DMSO]55 mg/mL]false]Ethanol]55 mg/mL]false]Water]Insoluble]false Purity: 100%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

100

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Drug Metabolite
Other PDE Inhibitors	Rolipram IBMX (3-Isobutyl-1-methylxanthine) Icariin Cilomilast Mardepodect (PF-2545920) Deltarasin PF-8380 Enpp-1-IN-1 Ibudilast BRL-50481

Chemical Information, Storage & Stability

Molecular Weight	275.34	Formula	C₁₆H₂₁NO₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	85416-73-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	COC1=C(C=C(C=C1)C2CC(=O)NC2)OC3CCCC3

Solubility

In vitro
Batch:

DMSO : 55 mg/mL (199.75 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 55 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	30%PEG400 1 0.5%Tween80 2 5%propylene glycol Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (36.32mM)	Taking the 1 mL working solution as an example, add 300 μL of 33.33 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol to the above system, mix evenly to clarify it; then continue to add 645 μL ddH2O Dilute to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	PDE4 0.75 μM
In vitro	S-(+)-Rolipram suppresses LPS-induced TNFα expression from human monocytes through inhibiting PDE4 with an IC50 of about 2 μM. 1 μM of this compound significantly antagonises ovalbumin (OA)-induced concentration-related contractions of tracheal rings which are isolated from OA-sensitised guinea pigs. This chemical inhibits PDE4 activity in a CHO-K1 cell line which stably expresses a recombinant full length human PDE-4a with an IC50 at 450 nM. Treatment of the human glioma cell line A-172 with Rolipram (including both R- and S-enantiomers of Rolipram) results in increased expression of the cell cycle inhibitors p21 and p27 , and decreased activity of cdk2, a cyclin-dependent kinase essential for cell cycle progression. As a result, the proliferation of A-172 cells is inhibited, with induction of a G1 block. Eventually, Rolipram-treated A-172 cells undergo differentiation, which is followed by apoptotic cell death.
In vivo	In anaesthetised, ventilated OA-sensitive guinea pigs, S-(+)-Rolipram reduces OA-induced bronchoconstriction with ID50 values of approximately 0.25 mg/kg i.v. Histamine- and leukotriene D4-induced bronchoconstriction are not affected by doses of this compound which abolish the response to OA. Higher doses (3-10 mg/kg) reduce histamine-, but not the leukotriene D4-induced bronchoconstriction. In conscious OA-sensitive guinea pigs, intragastric pretreatment with this chemical dose-dependently reduces both the OA-induced decreases in specific conductance as well as the corresponding pulmonary eosinophil influx as assessed by both bronchoalveolar lavage and histological evaluation.
References	[1] https://pubmed.ncbi.nlm.nih.gov/8762090/ [2] https://pubmed.ncbi.nlm.nih.gov/8392555/ [3] https://pubmed.ncbi.nlm.nih.gov/9631244/ [4] https://pubmed.ncbi.nlm.nih.gov/12432276/

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