A 33 |
カタログ番号GC50419
One-Click Copy Product Info
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Ａ ３３ は、１５ｎＭのＩＣ５０を有する経口的に活性で選択的なＰＤＥ４Ｂ阻害剤である。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 915082-52-9
Sample solution is provided at 25 µL, 10mM.
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Potent and selective PDE4B inhibitor (IC50 = 15 nM); exhibits >100-fold selectivity for PDE4B over 4D. Regulates cAMP in inflammatory cells. Inhibits LPS-induced TNF-α production and neutrophil accumulation in mouse lungs. Reduces microglial and neutrophil activation, and improves behavioral deficits in a traumatic brain injury model in vivo. Also exhibits antidepressant-like effects. Orally bioavailable.
Naganuma et al (2009) Discovery of selective PDE4B inhibitors. Bioorg.Med.Chem.Lett. 19 3174 PMID:19447034 |Zhang et al (2017) Comparison of the pharmacological profiles of selective PDE4B and PDE4D inhibitors in the central nervous system. Sci.Rep. 7 40115 PMID:28054669 |Wilson et al (2017) Therapeutic benefits of phosphodiesterase 4B inhibition after traumatic brain injury. PLoS One 12 e0178013 PMID:28542295
| Cas No. | 915082-52-9 | SDF | |
| Canonical SMILES | CCC1=C(N=C(C2=CC=C(S2)Cl)N=C1NC3=CC=C(C=C3)CC(O)=O)C | ||
| Formula | C19H18ClN3O2S | M.Wt | 387.88 |
| 溶解度 | 38.7mg/ml in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5781 mL | 12.8906 mL | 25.7812 mL |
| 5 mM | 515.6 μL | 2.5781 mL | 5.1562 mL |
| 10 mM | 257.8 μL | 1.2891 mL | 2.5781 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
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 saline, 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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)