Rolipram [61413-54-5]
Katalog-Nummer HY-16900-1ml
Size : 10mM/1mL
Marke : MedChemExpress
Rolipram is a selective phosphodiesterases PDE4 inhibitor with IC50s of 3 nM, 130 nM and 240 nM for PDE4A, PDE4B, and PDE4D, respectively.
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Rolipram Chemische Struktur
CAS. Nr. : 61413-54-5
This product is a controlled substance and not for sale in your territory.
Based on 10 publication(s) in Google Scholar
Other Forms of Rolipram:
- (R)-(-)-Rolipram In-stock
- (S)-(+)-Rolipram In-stock
Beschreibung |
Rolipram is a selective phosphodiesterases PDE4 inhibitor with IC50s of 3 nM, 130 nM and 240 nM for PDE4A, PDE4B, and PDE4D, respectively. |
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IC50 & Target |
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In Vitro |
The PDE4 selective inhibitor, Rolipram, inhibits immunopurified PDE4B and PDE4D activities similarly, with IC50s of approx. 130 nM and 240 nM respectively. In contrast, Rolipram inhibits immunopurified PDE4A activity with a dramatically lower IC50 of around 3 nM. Rolipram increases phosphorylation of cAMP-response-element-binding protein (CREB) in U937 cells in a dose-dependent fashion, which implies the presence of both high affinity (IC50 approx. 1 nM) and low affinity (IC50 approx. 120 nM) components. Rolipram dose-dependently inhibits the IFN-gamma-stimulated phosphorylation of p38 MAPK in a simple monotonic fashion with an IC50 of approx. 290 nM[1]. Rolipram is a selective PDE4 inhibitor that inhibits all PDE4 isoforms A, B, C and D. Rolipram inhibits LPS-induced TNF production in a dose-dependent manner (IC50 25.9 nM), and maximal/submaximal inhibition is observed with 2 μM drug concentration in J774 cells[2]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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In Vivo |
TNF mRNA and protein expression is induced by LPS in peritoneal macrophages (PM) from WT mice, and that is clearly (by 74 and 63% for TNF mRNA and TNF protein, respectively) inhibited by Rolipram. LPS-induced TNF production is enhanced in PM from MKP-1(-/-) mice as compared to that in PM from WT mice, which is in line with the published results. Interestingly, the inhibition of TNF mRNA and protein expression by Rolipram is markedly attenuated in PM from MKP-1(-/-) mice and does not reach statistical significance[2]. Repeated administration of Rolipram (1.25 mg/kg, i.p.) reduces the number of escape failures in learned helplessness rats[3]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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Klinische Studie |
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Molekulargewicht |
275.34 |
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Formel |
C16H21NO3 |
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CAS. Nr. |
61413-54-5 |
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Appearance |
Solid |
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Color |
White to off-white |
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SMILES |
O=C1NCC(C2=CC=C(OC)C(OC3CCCC3)=C2)C1 |
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Versand | Room temperature in continental US; may vary elsewhere. |
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Speicherung |
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Lösungsmittel & Löslichkeit |
In Vitro:
DMSO : ≥ 41 mg/mL (148.91 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) H2O : < 0.1 mg/mL (insoluble) *"≥" means soluble, but saturation unknown. Preparing
Stock Solutions
View the Complete Stock Solution Preparation Table
*
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.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
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:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO
+
%
+
%
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).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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Reinheit & Dokumentation |
Purity: 99.58% |
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Verweise |
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Complete Stock Solution Preparation Table
*
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.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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DMSO | 1 mM | 3.6319 mL | 18.1594 mL | 36.3187 mL | 90.7968 mL |
5 mM | 0.7264 mL | 3.6319 mL | 7.2637 mL | 18.1594 mL | |
10 mM | 0.3632 mL | 1.8159 mL | 3.6319 mL | 9.0797 mL | |
15 mM | 0.2421 mL | 1.2106 mL | 2.4212 mL | 6.0531 mL | |
20 mM | 0.1816 mL | 0.9080 mL | 1.8159 mL | 4.5398 mL | |
25 mM | 0.1453 mL | 0.7264 mL | 1.4527 mL | 3.6319 mL | |
30 mM | 0.1211 mL | 0.6053 mL | 1.2106 mL | 3.0266 mL | |
40 mM | 0.0908 mL | 0.4540 mL | 0.9080 mL | 2.2699 mL | |
50 mM | 0.0726 mL | 0.3632 mL | 0.7264 mL | 1.8159 mL | |
60 mM | 0.0605 mL | 0.3027 mL | 0.6053 mL | 1.5133 mL | |
80 mM | 0.0454 mL | 0.2270 mL | 0.4540 mL | 1.1350 mL | |
100 mM | 0.0363 mL | 0.1816 mL | 0.3632 mL | 0.9080 mL |