| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
Renin.
|
|---|---|
| ln Vitro |
VTP-27999 is a highly potent and selective renin inhibitor with an IC50 of 0.47 nM. It increases renin immunoreactivity for a given amount of renin by ≥30%. The compound demonstrates excellent selectivity over related and unrelated off-targets.
|
| ln Vivo |
No detailed in vivo activity data is available beyond general descriptions. VTP-27999 has demonstrated oral efficacy in a double transgenic rat model of hypertension, confirming its in vivo activity as a renin inhibitor for blood pressure reduction.
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| Enzyme Assay |
The compound's renin inhibitory activity is assessed in cell-free enzymatic assays using purified human renin. The assay measures the conversion of angiotensinogen to angiotensin I in the presence of varying concentrations of VTP-27999 to determine the IC50 value of 0.47 nM.
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| Cell Assay |
No detailed in vitro cell-based experimental protocol is available for this compound. As a renin inhibitor targeting the enzymatic activity of renin in the bloodstream, cell-based assays are less commonly used, with activity typically assessed in plasma or biochemical systems.
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| Animal Protocol |
In vivo efficacy studies are conducted in double transgenic rat models of hypertension to assess blood pressure-lowering effects. The compound is administered orally, and blood pressure is monitored over time to evaluate efficacy and duration of action.
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| ADME/Pharmacokinetics |
VTP-27999 demonstrates >15% oral bioavailability in three species, good exposure in humans, and excellent selectivity. It is an orally efficacious renin inhibitor with favorable PK properties for further development.
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| Toxicity/Toxicokinetics |
No detailed toxicological data is available for this compound. As a preclinical research compound, standard toxicity assessments have not been published in the current literature.
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| References | |
| Additional Infomation |
VTP-27999 TFA has a molecular formula of C26H41ClN4O5·CF3CO2H and a molecular weight of 639.10. The compound is useful for hypertension and end-organ diseases research. It is a highly potent and selective renin inhibitor that has demonstrated oral efficacy and good exposure in preclinical models. It has not advanced to clinical trials and is not FDA-approved.
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| Molecular Formula |
C28H42CLF3N4O7
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|---|---|
| Molecular Weight |
639.1102
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| Exact Mass |
638.269
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| CAS # |
1013937-63-7
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| Related CAS # |
VTP-27999 Hydrochloride;1264191-73-2;VTP-27999;942142-51-0
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| PubChem CID |
77147237
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| Appearance |
Colorless to light yellow ointment
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| LogP |
5.323
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
43
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| Complexity |
756
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(N1CCC[C@@H]([C@@H](OCCNC(OC)=O)C2=CC=CC(Cl)=C2)C1)NC[C@@H](NC)C[C@@H]3COCCC3.O=C(C(F)(F)F)O
|
| InChi Key |
SYWYSVAEGXHOJO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H41ClN4O5.C2HF3O2/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;3-2(4,5)1(6)7/h3,7,9,15,19,21,23-24,28H,4-6,8,10-14,16-18H2,1-2H3,(H,29,33)(H,30,32);(H,6,7)
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| Chemical Name |
methyl N-[2-[(3-chlorophenyl)-[1-[[2-(methylamino)-3-(oxan-3-yl)propyl]carbamoyl]piperidin-3-yl]methoxy]ethyl]carbamate;2,2,2-trifluoroacetic acid
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| Synonyms |
VTP 27999 TFAVTP-27999 VTP27999
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
H2O : ~10 mg/mL (~15.65 mM)
Ethanol : ~2.4 mg/mL (~3.76 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 25 mg/mL (39.12 mM) (saturation unknown) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5647 mL | 7.8234 mL | 15.6468 mL | |
| 5 mM | 0.3129 mL | 1.5647 mL | 3.1294 mL | |
| 10 mM | 0.1565 mL | 0.7823 mL | 1.5647 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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