VTP-27999 HydrochlorideAlkyl Amine Renin inhibitor CAS# 1264191-73-2 |
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| Cas No. | 1264191-73-2 | SDF | Download SDF |
| PubChem ID | 66577067 | Appearance | Powder |
| Formula | C26H42Cl2N4O5 | M.Wt | 561.54 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | H2O : ≥ 100 mg/mL (178.08 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | methyl N-[2-[(R)-(3-chlorophenyl)-[(3R)-1-[[(2S)-2-(methylamino)-3-[(3R)-oxan-3-yl]propyl]carbamoyl]piperidin-3-yl]methoxy]ethyl]carbamate;hydrochloride | ||
| SMILES | CNC(CC1CCCOC1)CNC(=O)N2CCCC(C2)C(C3=CC(=CC=C3)Cl)OCCNC(=O)OC.Cl | ||
| Standard InChIKey | XDXSPYSCCJMHRQ-VIEYARBJSA-N | ||
| Standard InChI | InChI=1S/C26H41ClN4O5.ClH/c1-28-23(14-19-6-5-12-35-18-19)16-30-25(32)31-11-4-8-21(17-31)24(20-7-3-9-22(27)15-20)36-13-10-29-26(33)34-2;/h3,7,9,15,19,21,23-24,28H,4-6,8,10-14,16-18H2,1-2H3,(H,29,33)(H,30,32);1H/t19-,21-,23+,24+;/m1./s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | VTP-27999 Hydrochloride is a potent inhibitor of renin with IC50 value of 0.3 nM for human renin. | |||||
| Targets | human renin | |||||
| IC50 | 0.3 nM | |||||
VTP-27999 Hydrochloride Dilution Calculator
VTP-27999 Hydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.7808 mL | 8.9041 mL | 17.8082 mL | 35.6163 mL | 44.5204 mL |
| 5 mM | 0.3562 mL | 1.7808 mL | 3.5616 mL | 7.1233 mL | 8.9041 mL |
| 10 mM | 0.1781 mL | 0.8904 mL | 1.7808 mL | 3.5616 mL | 4.452 mL |
| 50 mM | 0.0356 mL | 0.1781 mL | 0.3562 mL | 0.7123 mL | 0.8904 mL |
| 100 mM | 0.0178 mL | 0.089 mL | 0.1781 mL | 0.3562 mL | 0.4452 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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VTP-27999 hydrochlorideis a highly potent and selective renin inhibitor (IC50 = 0.47 nM). It exhibits >1000 selectivity for renin over >150 receptors, ion channels and enzymes. VTP-27999 hydrochloride is hydrochloride salt form of VTP-27999.
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, 24 h 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.
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VTP-27999 Hcl is an alkyl amine Renin inhibitor; VTP-27999 is useful for Hypertension and End-Organ Diseases.
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