MBCQ |
| Catalog No.GC16849 |
MBCQ는 IC50이 19nM인 강력하고 선택적인 cGMP 특이적 포스포디에스테라제(PDE V; PDE5) 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 150450-53-6
Sample solution is provided at 25 µL, 10mM.
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MBCQ is a cGMP-specific phosphodiesterase PDE5 inhibitor.
The phosphodiesterase type 5 inhibitor (PDE5 inhibitor) is an agent used to inhibit the degradative action of cGMP-specific PDE5 on cyclic GMP in the smooth muscle cells lining the blood vessels supplying the corpus cavernosum of the penis. PDE5 drugs are used in the treatment of erectile dysfunction and were the first effective oral treatment for this condition. Sinve PDE5 is also present in the arterial wall smooth muscle within the lungs, PDE5 inhibitors have also been applied for the pulmonary hypertension treatment.
In vitro: In previous study, it was found that the addition of MBCQ to the blood vessle samples could lead to an 80 to 85% inhibition of PDE activity, indicating that most of the activity present in these blood vessels could be attributed to PDE5. [1].
In vivo: In animal rat study, tolerance was induced by continuous exposure to glyceryl trinitrate (GTN) for 48 h. Results showed that MBCQ could significantly decrease the EC(50) values for GTN-induced relaxation in both tolerant and nontolerant tissues, but with the greatest relative shift showing in tolerant veins. Moreover, MBCQ could also increase the vasodilator potency of a nitric oxide donor (1,1-diethyl-2-hydroxy-2-nitrosohydrazine). A significant increase in cGMP PDE activity was found in tolerant femoral vein, whereas PDE activity was unchanged in femoral artery [1].
Clinical trial: Up to now, MBCQ is still in the preclinical development stage.
Reference:
[1] MacPherson JD, Gillespie TD, Dunkerley HA, Maurice DH, Bennett BM. Inhibition of phosphodiesterase 5 selectively reverses nitrate tolerance in the venous circulation. J Pharmacol Exp Ther. 2006 Apr;317(1):188-95.
| Cas No. | 150450-53-6 | SDF | |
| Chemical Name | N-(1,3-benzodioxol-5-ylmethyl)-6-chloro-4-quinazolinamine | ||
| Canonical SMILES | ClC1=CC2=C(C=C1)N=CN=C2NCC3=CC(OCO4)=C4C=C3 | ||
| Formula | C16H12ClN3O2 | M.Wt | 313.7 |
| Solubility | DMSO: 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. |
||
| 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 | 3.1878 mL | 15.9388 mL | 31.8776 mL |
| 5 mM | 637.6 μL | 3.1878 mL | 6.3755 mL |
| 10 mM | 318.8 μL | 1.5939 mL | 3.1878 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 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: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)
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