VTP-27999 |
Katalog-Nr.GC16809
One-Click Copy Product Info
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A renin inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 942142-51-0
Sample solution is provided at 25 µL, 10mM.
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VTP-27999 is a highly potent and selective renin inhibitor (IC50 = 0.47 nM). It exhibits >1000 selectivity for renin over >150 receptors, ion channels and enzymes.
Renin is an asparyl protease that cleaves angiotensinogen into angiotension I in the plasma. It functions as a regulator of blood pressure and sodium homeostasis.
In vitro, VTP-27999 increases renin immunoreactivity by ≥30%, it bind to acid-activated, intact prorenin and promotes immunoreactivity in a renin assay. In vascular smooth muscle cells, VTP-27999 also blocks renin's ability to activate extracellular signal-regulated kinase 1/2 phosphorylation. [1]
In double transgenic rats engineered to express human renin and angiotensinogen with severe hypertension, 24h treatment of 10 mg/kg VTP-27999 induces a greater reduction in mean arterial blood pressure and a longer duration of action. [2]
References:
1. Krop M, Lu X, Verdonk K, Schalekamp MA et al. New renin inhibitor VTP-27999 alters renin immunoreactivity and does not unfold prorenin. Hypertension. 2013 May;61(5):1075-82.
2. Jia L, Simpson RD, Yuan J et al. Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility. ACS Med Chem Lett. 2011 Aug 9;2(10):747-51.
| Cas No. | 942142-51-0 | SDF | |
| Chemical Name | methyl (2-((3-chlorophenyl)(1-((2-(methylamino)-3-(tetrahydro-2H-pyran-3-yl)propyl)carbamoyl)piperidin-3-yl)methoxy)ethyl)carbamate | ||
| Canonical SMILES | CNC(CNC(N1CCCC(C(OCCNC(OC)=O)C2=CC(Cl)=CC=C2)C1)=O)CC3CCCOC3 | ||
| Formula | C26H41ClN4O5 | M.Wt | 525.08 |
| Löslichkeit | 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 | 1.9045 mL | 9.5224 mL | 19.0447 mL |
| 5 mM | 380.9 μL | 1.9045 mL | 3.8089 mL |
| 10 mM | 190.4 μL | 952.2 μL | 1.9045 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 30 reference(s) in Google Scholar.)