Cat. No.: HY-A0115

Ramiprilat

(Synonyms: HOE 498 diacid; Ramipril diacid)

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Ramiprilat (HOE 498 diacid), an active metabolite of Ramipril, is a potent and orally active angiotensin converting enzyme (ACE) inhibitor with a K_i value of 7 pM. Ramiprilat has acute antlhypertensive effect. Ramiprilat can be used for high blood pressure and heart failure research.

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Pureté: 97.09%
CAS No.: 87269-97-4
Formule: C₂₁H₂₈N₂O₅
Masse moléculaire:388.46

Stockage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Ramiprilat Chemical Structure

CAS No.: 87269-97-4

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

Ki: 7 pM (ACE)^[1]

Voir tous les produits spécifiques à Isoform Endogenous Metabolite :

In Vitro

Ramiprilat (0.1, 1 μM, 0-30 min) induces cyclic GMP increase in endothelial cells^[2].
Ramiprilat (0.3 μM, 15 min) elicits a significant nitric oxide release and an increase in prostaglandin I_{2 (PGI2) release in endothelial cells^[2].}

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

In Vivo

Ramiprilat (2 mg/kg, i.v., a single dose for 60 min) decreases the blood pressure of spontaneously hypertensive rats^[5].

Pharmacokinetic-pharmacodynamic parameters (mean±SD) for Ramiprilat after different IV and PO ramipril doses^[4]

Parameters	IV (0.05 mg/kg)	PO (0.40 mg/kg)	PO (0.80 mg/kg)
k₁₀ (1/h)	5.09	5.49	4.10
t_{1/2 k10} (h)	0.16 (0.09-0.31)	0.13 (0.10-0.16)	0.17 (0.10-0.27)
V_c (L/kg)	0.15
V_c/F (L/kg)		2.35	1.97
Cl (L/kg/h)	0.77
Cl/F (L/kg/h)		12.82	7.79
F (%)		6.52	9.08
K_d (nmol/L)	1.35	1.47	1.19
f_circ (%)	5.01	5.80	6.08
B_max (nmol/L)	109.46	79.31	91.72
P_max (nmol/L)	5.27	4.60	5.08
IC₅₀ (nmol/L)	1.05	1.07	0.88

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

Chemical Information

CAS No. 87269-97-4
Appearance Solid
Masse moléculaire 388.46
Formule C₂₁H₂₈N₂O₅
Color White to off-white
SMILES

O=C([C@@H]1C[C@@](CCC2)([H])[C@@]2([H])N1C([C@@H](N[C@H](C(O)=O)CCC3=CC=CC=C3)C)=O)O
Synonyms

HOE 498 diacid; Ramipril diacid
Structure Classification
- Alkaloids
- Pyrrole Alkaloids
Initial Source
- Endogenous metabolite
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (257.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5743 mL

12.8713 mL

25.7427 mL

5 mM

0.5149 mL

2.5743 mL

5.1485 mL

10 mM

0.2574 mL

1.2871 mL

2.5743 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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 (6.44 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.44 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.44 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (280 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Ramiprilat (HOE 498 diacid), an active metabolite of Ramipril, is a potent and orally active angiotensin converting enzyme (ACE) inhibitor with a Ki value of 7 pM. Ramiprilat can be used for high blood pressure and heart failure research^[1]. [Content Brief]

[2]. Wiemer G, et al. Ramiprilat enhances endothelial autacoid formation by inhibiting breakdown of endothelium-derived bradykinin. Hypertension. 1991 Oct;18(4):558-63. [Content Brief]

[3]. Wall TM, et al. Ramiprilat attenuates hypoxia/reoxygenation injury to cardiac myocytes via a bradykinin-dependent mechanism. Eur J Pharmacol. 1996 Jun 13;306(1-3):165-74. [Content Brief]

[4]. Serrano-Rodríguez JM, et al. Pharmacokinetics and pharmacodynamics of ramipril and ramiprilat after intravenous and oral doses of ramipril in healthy horses. Vet J. 2016 Feb;208:38-43. [Content Brief]

[5]. Cachofeiro V, et al. Kinins, nitric oxide, and the hypotensive effect of captopril and ramiprilat in hypertension. Hypertension. 1992 Feb;19(2):138-45. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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
DMSO	1 mM	2.5743 mL	12.8713 mL	25.7427 mL	64.3567 mL
	5 mM	0.5149 mL	2.5743 mL	5.1485 mL	12.8713 mL
	10 mM	0.2574 mL	1.2871 mL	2.5743 mL	6.4357 mL
	15 mM	0.1716 mL	0.8581 mL	1.7162 mL	4.2904 mL
	20 mM	0.1287 mL	0.6436 mL	1.2871 mL	3.2178 mL
	25 mM	0.1030 mL	0.5149 mL	1.0297 mL	2.5743 mL
	30 mM	0.0858 mL	0.4290 mL	0.8581 mL	2.1452 mL
	40 mM	0.0644 mL	0.3218 mL	0.6436 mL	1.6089 mL
	50 mM	0.0515 mL	0.2574 mL	0.5149 mL	1.2871 mL
	60 mM	0.0429 mL	0.2145 mL	0.4290 mL	1.0726 mL
	80 mM	0.0322 mL	0.1609 mL	0.3218 mL	0.8045 mL
	100 mM	0.0257 mL	0.1287 mL	0.2574 mL	0.6436 mL

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Ramiprilat

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Voir tous les produits spécifiques à Isoform Endogenous Metabolite

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Ramiprilat

Metabolism/Protease Compound Library

FDA-Approved Drug Library

Drug Repurposing Compound Library

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Alkaloids Library

Angiogenesis-Related Compound Library

Drug Metabolite Library

Rare Diseases Drug Library

Human Metabolite Library

Heterocyclic Compound Library

Off-patent Drug Library

Antihypertensive Compound Library

Protease Inhibitor Library

Membrane Protein-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

RO5 Drug-like Natural Product Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Natural Product Diversity Scaffold Library

Voir tous les produits spécifiques à Isoform Endogenous Metabolite

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Ramiprilat Related Classifications

HY-A0115 Related Classifications