Sampatrilat (Synonyms: UK-81252)

Name: Sampatrilat
Brand: MedChemExpress
SKU: HY-123348
Rating: 4.5 (1 reviews)

Cat. No.: HY-123348 Purity: 99.22%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Sampatrilat (UK-81252) is a potent and orally active vasopeptidase inhibitor of ACE and neutral endopeptidase (NEP). Sampatrilat inhibits C-domain ACE (K_i=13.8 nM) 12.4-fold more potent than that for the N-domain (K_i=171.9 nM). Sampatrilat (UK-81252) can be used for the study of chronic heart failure and blood pressure regulation.

For research use only. We do not sell to patients.

Sampatrilat Chemical Structure

CAS No. : 129981-36-8

Size	Price	Stock	Quantity
5 mg	USD 660	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 1057	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 2114	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 3383	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Based on 1 publication(s) in Google Scholar

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Description

IC₅₀ & Target

Ki: 13.8 nM (cACE); 171.9 nM (nACE)^[1]

In Vivo

Sampatrilat (oral adminstration; 30 mg/kg; once a day; 5 weeks) reduces the mortality of the rats with CAL (20% versus 57% for untreated rats) and increase in the survival rate and improvement of hemodynamic function of the rats with CAL. This compound suppresses tissue ACE and neutral endopeptidase (NEP) activities, but it does not affect the arterial blood pressure, whereas it attenuates the CAL-induced increases in the left ventricular end-diastolic pressure, heart weight, and collagen content of the viable left Ventricle^[2].

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

Animal Model:	Left coronary artery ligation (CAL) and sham-operated rats^[2]
Dosage:	30 mg/kg
Administration:	Oral adminstration
Result:	Prevented the increases in heart weight and cardiac collagen content of the rats with CAL.

Molecular Weight

584.68

Formula

C₂₆H₄₀N₄O₉S

CAS No.

129981-36-8

Appearance

Solid

Color

White to off-white

SMILES

OC([C@H](CNC([C@@H](NS(C)(=O)=O)CCCCN)=O)CC1(CCCC1)C(N[C@H](C(O)=O)CC2=CC=C(O)C=C2)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°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:

DMSO : 100 mg/mL (171.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7103 mL	8.5517 mL	17.1034 mL
5 mM	0.3421 mL	1.7103 mL	3.4207 mL
10 mM	0.1710 mL	0.8552 mL	1.7103 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.28 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.28 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.28 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.22%

Select Batch:

Data Sheet (272 KB) SDS (251 KB)

COA (247 KB) HNMR (239 KB) RP-HPLC (241 KB) LCMS (85 KB)

Handling Instructions (2659 KB)

References

[1]. Sharma RK, et al. The Dynamic Nonprime Binding of Sampatrilat to the C-Domain of Angiotensin-Converting Enzyme. J Chem Inf Model. 2016 Dec 27;56(12):2486-2494. [Content Brief]

[2]. Maki T, et al. Beneficial effects of sampatrilat, a novel vasopeptidase inhibitor, on cardiac remodeling and function of rats with chronic heart failure following left coronary artery ligation.J Pharmacol Exp Ther. 2003 Apr;305(1):97-105. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7103 mL	8.5517 mL	17.1034 mL	42.7584 mL
	5 mM	0.3421 mL	1.7103 mL	3.4207 mL	8.5517 mL
	10 mM	0.1710 mL	0.8552 mL	1.7103 mL	4.2758 mL
	15 mM	0.1140 mL	0.5701 mL	1.1402 mL	2.8506 mL
	20 mM	0.0855 mL	0.4276 mL	0.8552 mL	2.1379 mL
	25 mM	0.0684 mL	0.3421 mL	0.6841 mL	1.7103 mL
	30 mM	0.0570 mL	0.2851 mL	0.5701 mL	1.4253 mL
	40 mM	0.0428 mL	0.2138 mL	0.4276 mL	1.0690 mL
	50 mM	0.0342 mL	0.1710 mL	0.3421 mL	0.8552 mL
	60 mM	0.0285 mL	0.1425 mL	0.2851 mL	0.7126 mL
	80 mM	0.0214 mL	0.1069 mL	0.2138 mL	0.5345 mL
	100 mM	0.0171 mL	0.0855 mL	0.1710 mL	0.4276 mL

Sampatrilat Related Classifications

Inflammation/Immunology Cardiovascular Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Sampatrilat (Synonyms: UK-81252)

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Complete Stock Solution Preparation Table

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