VTP-27999 (Hydrochloride)
Based on 1 Customer Validation
VTP-27999 Hydrochloride is an orally active renin inhibitor. VTP-27999 Hydrochloride functionally inhibits renin and acid-activated prorenin, suppresses plasma renin activity and modulates plasma and urinary aldosterone levels. VTP-27999 Hydrochloride reduces mean arterial blood pressure, induces plasma renin concentration increases, decreases plasma angiotensin II levels and enhances renin immunoreactivity. VTP-27999 (Hydrochloride) can be used for the research of hypertension and chronic renal disease.
For research use only. We do not sell to patients.
- Purity: 98.18%
- CAS No.: 1264191-73-2
- Formula: C26H42Cl2N4O5
- Molecular Weight:561.54
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
VTP-27999 (Compound 9) Hydrochloride inhibits 0.3 nM purified recombinant human renin in buffer with an IC50 of 0.47 nM[1].
VTP-27999 Hydrochloride inhibits renin 36 pM purified recombinant human renin in buffer with an IC50 of 0.30 nM[1].
VTP-27999 Hydrochloride inhibits human plasma renin activity with an IC50 of 1.1 nM[1].
VTP-27999 Hydrochloride does not inhibit human liver microsomal CYP3A4 with an IC50 greater than 30000 nM[1].
VTP-27999 (10 μM) Hydrochloride inhibits human β-secretase, cathepsin D, and cathepsin E by less than 10%[1].
VTP-27999 (0.001-100 μM; 48 h) binds to recombinant human prorenin but does not induce its unfolding[3].
VTP-27999 (1-300 nM) locks acid-activated recombinant human prorenin in its open conformation with a pIC50 of 8.4 and increases its renin immunoreactivity by 41%[3].
VTP-27999 (0.001 nM-10 μM) increases recombinant human renin immunoreactivity by 30% to 40% at concentrations ≥10 nM[3].
VTP-27999 (0.001 nM-10 μM) increases endogenous human plasma renin immunoreactivity by up to 70% (untreated) and 35% (trypsin-activated) at concentrations ≥10 nM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 | CL | Vss | AUC0-t | F |
|---|---|---|---|---|---|---|---|
| Rat[1] | 2.0 mg/kg | i.v. | 7.3 h | 128 mL/min/kg | 38 L/kg | / | / |
| Rat[1] | 10.0 mg/kg | p.o. | / | / | / | 477 ng·h/mL | 37 % |
| Monkey[1] | 1.0 mg/kg | i.v. | 12.3 h | 29.6 mL/min/kg | 4.7 L/kg | / | / |
| Monkey[1] | 2.0 mg/kg | p.o. | / | / | / | 404 ng·h/mL | 18 % |
| Dog[1] | 0.5 mg/kg | i.v. | 9.9 h | 12.9 mL/min/kg | 4.0 L/kg | / | / |
| Dog[1] | 1.0 mg/kg | p.o. | / | / | / | 484 ng·h/mL | 41 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Double transgenic rats (engineered to express human renin and angiotensinogen)[1]
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Dosage:10 mg/kg
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Administration:p.o.; single dose
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Result:Provided a greater reduction in mean arterial blood pressure (MAP) at 24 hours post-dose compared to Aliskiren at the same dose.
Exhibited a longer duration of action compared to Aliskiren at the same dose.
Chemical Information
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CAS No. 1264191-73-2
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Appearance Solid
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Molecular Weight 561.54
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Formula C26H42Cl2N4O5
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Color White to yellow
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SMILES
O=C(NC[C@H](C[C@@H]1COCCC1)NC)N(CCC2)C[C@]2([H])[C@](OCCNC(OC)=O)([H])C3=CC(Cl)=CC=C3.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H2O : ≥ 100 mg/mL (178.08 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Jia L, et al. Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility. ACS Med Chem Lett. 2011;2(10):747-751. Published 2011 Aug 9. [Content Brief]
[2]. Balcarek J, et al. Multiple ascending dose study with the new renin inhibitor VTP-27999: nephrocentric consequences of too much renin inhibition. Hypertension. 2014 May;63(5):942-50. [Content Brief]
[3]. Krop M, et al. New renin inhibitor VTP-27999 alters renin immunoreactivity and does not unfold prorenin. Hypertension. 2013;61(5):1075-1082. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 1.7808 mL | 8.9041 mL | 17.8082 mL | 44.5204 mL |
| 5 mM | 0.3562 mL | 1.7808 mL | 3.5616 mL | 8.9041 mL | |
| 10 mM | 0.1781 mL | 0.8904 mL | 1.7808 mL | 4.4520 mL | |
| 15 mM | 0.1187 mL | 0.5936 mL | 1.1872 mL | 2.9680 mL | |
| 20 mM | 0.0890 mL | 0.4452 mL | 0.8904 mL | 2.2260 mL | |
| 25 mM | 0.0712 mL | 0.3562 mL | 0.7123 mL | 1.7808 mL | |
| 30 mM | 0.0594 mL | 0.2968 mL | 0.5936 mL | 1.4840 mL | |
| 40 mM | 0.0445 mL | 0.2226 mL | 0.4452 mL | 1.1130 mL | |
| 50 mM | 0.0356 mL | 0.1781 mL | 0.3562 mL | 0.8904 mL | |
| 60 mM | 0.0297 mL | 0.1484 mL | 0.2968 mL | 0.7420 mL | |
| 80 mM | 0.0223 mL | 0.1113 mL | 0.2226 mL | 0.5565 mL | |
| 100 mM | 0.0178 mL | 0.0890 mL | 0.1781 mL | 0.4452 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
VTP-27999 (Hydrochloride) Related Classifications
HY-76652 Related Classifications
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