VTP-27999 (Hydrochloride)

Cat. No.: HY-76652 Purity: 98.18%: Data Sheet
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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.

VTP-27999 (Hydrochloride) Chemical Structure

CAS No. : 1264191-73-2

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in Water	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Other Forms of VTP-27999 (Hydrochloride):

VTP-27999 TFA In-stock
VTP-27999 Get quote

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Biological Activity
Purity & Documentation
References
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Description

In Vitro

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.

Parmacokinetics

Species	Dose	Route	T_1/2	CL	V_ss	AUC_0-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 %

In Vivo

VTP-27999 (Compound 9) (10 mg/kg; p.o.; single dose) Hydrochloride exhibits superior oral efficacy over Aliskiren (HY-12176) in a double transgenic rat model of hypertension, with a greater reduction in mean arterial blood pressure at 24 hours and a longer duration of action^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Double transgenic rats (engineered to express human renin and angiotensinogen)^[1]
Dosage:	10 mg/kg
Administration:	p.o.; single dose
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.

Molecular Weight

561.54

Formula

C₂₆H₄₂Cl₂N₄O₅

CAS No.

1264191-73-2

Appearance

Solid

Color

White to yellow

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

Shipping

Room temperature in continental US; may vary elsewhere.

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

In Vitro:

H₂O : ≥ 100 mg/mL (178.08 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7808 mL	8.9041 mL	17.8082 mL
5 mM	0.3562 mL	1.7808 mL	3.5616 mL
10 mM	0.1781 mL	0.8904 mL	1.7808 mL

View the 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.

* 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

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Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 98.18%

Select Batch:

Data Sheet (275 KB) SDS (252 KB)

COA (250 KB) LCMS (89 KB)

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.

[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.

[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

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.