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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
S-(+)-Rolipram, the S-isomer of rolipram (ME3167; SB-95952; ZK62711), is a potent phosphodiesterase PDE4-inhibitor with potent anti-inflammatory and anti-depressant activity. It inhibits human monocyte cyclic AMP-specific PDE4 with an IC50 of 0.75 μM, and is less potent than its R enantiomer. Rolipram (also known as ZK-62711 and SB 95952, the racemic mixture of R- and S-rolipram) is a novel, potent and selective phosphodiesterases PDE4 inhibitor with IC50s of 3 nM, 130 nM and 240 nM for PDE4A, PDE4B, and PDE4D, respectively. PDE4 inhibitor Rolipram has anti-inflammatory activity. Rolipram inhibits human monocyte. Rolipram inhibits human monocyte cyclic AMP-specific PDE4 with IC50 of 0.75 μM. It has potent anti-inflammatory and anti-depressant activity in the central nervous system, and the S-(+)-Rolipram is less potent than its R enantiomer.
ln Vitro |
At an IC50 of 550 nM, (+)-Rolipram (0.015-1000 μM; 20 h) dose-dependently inhibits human mononuclear cells' (MNC) production of TNF produced by LPS[1].
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ln Vivo |
(+)-Rolipram dose-dependently inhibits locomotor activity and causes twitches in the head of rats (0.025–6.25 mg/kg; one intraperitoneal)[2]. Rats' rectal temperatures drop in proportion to the dosage when given 0.06–25 mg/kg of (+)-Rolipram intraperitoneally[2].
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Animal Protocol |
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References |
[1]. Semmler J, et, al. The specific type IV phosphodiesterase inhibitor rolipram suppresses tumor necrosis factor-alpha production by human mononuclear cells. Int J Immunopharmacol. 1993 Apr;15(3):409-13.
[2]. Wachtel H. Neurotropic effects of the optical isomers of the selective adenosine cyclic 3',5'-monophosphate phosphodiesterase inhibitor rolipram in rats in-vivo. J Pharm Pharmacol. 1983 Jul;35(7):440-4. [3]. Ortmann R, et, al. Rolipram forms a potent discriminative stimulus in drug discrimination experiments in rats. Psychopharmacology (Berl). 1986;89(3):273-7. |
Molecular Formula |
C16H21NO3
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Molecular Weight |
275.34
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CAS # |
85416-73-5
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Related CAS # |
Rolipram;61413-54-5;(R)-(-)-Rolipram;85416-75-7
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O(C1=C(C([H])=C([H])C(=C1[H])[C@]1([H])C([H])([H])C(N([H])C1([H])[H])=O)OC([H])([H])[H])C1([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H]
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.08 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.08 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.08 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 30% PEG400+0.5% Tween80+5% propylene glycol:10 mg/L |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.6319 mL | 18.1594 mL | 36.3187 mL | |
5 mM | 0.7264 mL | 3.6319 mL | 7.2637 mL | |
10 mM | 0.3632 mL | 1.8159 mL | 3.6319 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.