Piclamilast
Based on 1 Customer Validation
Piclamilast (RP 73401) is a phosphodiesterase 4 (PDE4) inhibitor, with IC50 values of 16 nM and 2 nM in pig aorta and eosinophil soluble, respectively.
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- Pureté: 99.74%
- CAS No.: 144035-83-6
- Formule: C18H18Cl2N2O3
- Masse moléculaire:381.25
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[4]|
PDE4 16 nM (IC50, in pig aorta) |
PDE4 2 nM (IC50, in eosinophil soluble) |
PDE1 >100 μM (IC50) |
PDE2 40 μM (IC50) |
PDE3 >100 μM (IC50) |
PDE5 14 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
0.013 μM
Compound: 1
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Inhibition of PDE4 expressed in HEK293 cells coexpressing cyclic nucleotide gated ion channel mutant assessed as inhibition of NECA-induced cAMP production treated 15 mins before NECA challenge measured after 45 mins by FLIPR assay
Inhibition of PDE4 expressed in HEK293 cells coexpressing cyclic nucleotide gated ion channel mutant assessed as inhibition of NECA-induced cAMP production treated 15 mins before NECA challenge measured after 45 mins by FLIPR assay
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[PMID: 20378348] |
| Sf21 | IC50 |
11.4 μM
Compound: 1
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Inhibition of His-tagged catalytic domain Trypanosoma brucei brucei PDEB2 expressed in baculovirus infected insect Sf21 cells
Inhibition of His-tagged catalytic domain Trypanosoma brucei brucei PDEB2 expressed in baculovirus infected insect Sf21 cells
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[PMID: 22023548] |
| Sf21 | IC50 |
4.7 μM
Compound: 1
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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
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[PMID: 22023548] |
| U-937 | EC50 |
0.04 μM
Compound: RP-73401
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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
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[PMID: 9632360] |
In Vitro
Piclamilast (RP 73401, 1 μM, 30 min) significantly inhibits the changes in 23 genes via mechanisms involving AP-1 activation and c-Jun phosphorylation at Ser63[2].
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Piclamilast (RP 73401) exhibits IC50 values >100 μM, 40 μM, >100 μM, 14 μM for PDE1, PDE2, PDE3 and PDE5. Respectively[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human A549 type II lung epithelial cells.
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Concentration:1 μM (H2O2 200 μM).
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Incubation Time:30 min.
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Result:Prevented H2O2 -induced changes in gene expression levels in A549 cells.
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Cell Line:NB4 cells.
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Concentration:30 μM.
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Incubation Time:3 days.
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Result:Exerted a significant enhancing effect on the induction of STAT1 observed in ATRA-treated NB4 cells.
Caused a significant increase in the number of cells expressing NBT-R activity.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID mice[3].
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Dosage:10 mg/kg (combined with ATRA (HY-14649)).
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Administration:Injection daily.
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Result:Significantly more effective than ATRA alone in increasing the MST (40 days; interval 34–45 days) of leukemia-bearing animals.
Chemical Information
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CAS No. 144035-83-6
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Appearance Solid
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Masse moléculaire 381.25
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Formule C18H18Cl2N2O3
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Color White to off-white
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SMILES
O=C(NC1=C(Cl)C=NC=C1Cl)C2=CC=C(OC)C(OC3CCCC3)=C2
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Synonyms
RP 73401; RPR 73401
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 25 mg/mL (65.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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:
- 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (278 KB)
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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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. M J Ashton, et al. Selective type IV phosphodiesterase inhibitors as antiasthmatic agents. The syntheses and biological activities of 3-(cyclopentyloxy)-4-methoxybenzamides and analogues. J Med Chem. 1994 May 27;37(11):1696-703. [Content Brief]
[2]. Manuel Mata, et al. Piclamilast inhibits the pro-apoptotic and anti-proliferative responses of A549 cells exposed to H(2)O(2) via mechanisms involving AP-1 activation. Free Radic Res. 2012 May;46(5):690-9. [Content Brief]
[3]. Edoardo Parrella, et al. Phosphodiesterase IV inhibition by piclamilast potentiates the cytodifferentiating action of retinoids in myeloid leukemia cells. Cross-talk between the cAMP and the retinoic acid signaling pathways. J Biol Chem . 2004 Oct 1;279(40):42026-40. [Content Brief]
[4]. T Ukita, et al. Novel, potent, and selective phosphodiesterase-4 inhibitors as antiasthmatic agents: synthesis and biological activities of a series of 1-pyridylnaphthalene derivatives. J Med Chem. 1999 Mar 25;42(6):1088-99. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6230 mL | 13.1148 mL | 26.2295 mL | 65.5738 mL |
| 5 mM | 0.5246 mL | 2.6230 mL | 5.2459 mL | 13.1148 mL | |
| 10 mM | 0.2623 mL | 1.3115 mL | 2.6230 mL | 6.5574 mL | |
| 15 mM | 0.1749 mL | 0.8743 mL | 1.7486 mL | 4.3716 mL | |
| 20 mM | 0.1311 mL | 0.6557 mL | 1.3115 mL | 3.2787 mL | |
| 25 mM | 0.1049 mL | 0.5246 mL | 1.0492 mL | 2.6230 mL | |
| 30 mM | 0.0874 mL | 0.4372 mL | 0.8743 mL | 2.1858 mL | |
| 40 mM | 0.0656 mL | 0.3279 mL | 0.6557 mL | 1.6393 mL | |
| 50 mM | 0.0525 mL | 0.2623 mL | 0.5246 mL | 1.3115 mL | |
| 60 mM | 0.0437 mL | 0.2186 mL | 0.4372 mL | 1.0929 mL |
Piclamilast Related Classifications
HY-12887 Related Classifications
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