BC 11-38 |
| Catalog No.GC16048 |
Selective PDE11 inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 686770-80-9
Sample solution is provided at 25 µL, 10mM.
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BC 11-38 is a selective inhibitor of PDE11 with an IC50 value of 0.28 μM [1].
PDE11 is a PDE family. In humans the PDE11A gene encodes four isoforms hydrolyzing both cAMP and cGMP. PDE11A is expressed in skeletal muscle, brain, prostate, testis, kidney, pancreas, liver, lymphoid cells, and pituitary and adrenal glands [2].
In H295R human adenocarcinoma cells, BC11-38 significantly increased cortisol production and cAMP levels, both in the presence and absence of the adenylate cyclase activator forskolin. In H295R cells, BC11-38 elevated ATF-1 phosphorylation in a manner that corresponded with its potency against PDE11. In several lines including MDA-MB-231 and HeLa cells, there were very low levels of PDE11A mRNA. In MDA-MB-231 cells, BC11-38 failed to elevate cAMP levels and CREB phosphorylation. In HeLa cells, BC11-38 did not affect cAMP levels or CREB phosphorylation [2]. In p54nrb/NONOKD cells, combining treatment with BC11-38 and ACTH restored partially the capacity to produce DHEA and cortisol in response to cAMP stimulation and the ability to generate cAMP in response to ACTH stimulation [3].
An invention also relates to the use of compounds such as BC11-38 to elevate cortisol levels in a subject who has adrenal suppression, e.g. where a subject is being administered with a corticosteroid, or on a long-term corticosteroid treatment [4].
References:
[1]. Cichero E, D'Ursi P, Moscatelli M, et al. Homology modeling, docking studies and molecular dynamic simulations using graphical processing unit architecture to probe the type-11 phosphodiesterase catalytic site: a computational approach for the rational design of selective inhibitors. Chemical biology & drug design, 2013, 82(6): 718-731.
[2]. Ceyhan O, Birsoy K, Hoffman CS. Identification of biologically active PDE11-selective inhibitors using a yeast-based high-throughput screen. Chemistry & biology, 2012, 19(1): 155-163.
[3]. Lu JY, Sewer MB. p54nrb/NONO Regulates Cyclic AMP-Dependent Glucocorticoid Production by Modulating Phosphodiesterase mRNA Splicing and Degradation. Molecular and cellular biology, 2015, 35(7): 1223-1237.
[4]. Hoffman CS, Ceyhan O. Inhibitors of phosphodiesterase 11 (PDE11): U.S. Patent 9,173,884[P]. 2015-11-3.
| Cas No. | 686770-80-9 | SDF | |
| Chemical Name | 3-phenyl-2-(propylthio)-6,7-dihydrothieno[3,2-d]pyrimidin-4(3H)-one | ||
| Canonical SMILES | O=C1N(C2=CC=CC=C2)C(SCCC)=NC3=C1SCC3 | ||
| Formula | C15H16N2OS2 | M.Wt | 304.43 |
| Solubility | DMF: 30 mg/mL,DMSO: 30 mg/mL,DMSO:PBS (pH 7.2) (1:2): 0.33 mg/mL,Ethanol: 5 mg/mL | 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 | 3.2848 mL | 16.4241 mL | 32.8483 mL |
| 5 mM | 0.657 mL | 3.2848 mL | 6.5697 mL |
| 10 mM | 0.3285 mL | 1.6424 mL | 3.2848 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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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 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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 20 reference(s) in Google Scholar.)
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