1. Metabolic Enzyme/Protease
  2. Drug Metabolite Angiotensin-converting Enzyme (ACE) Endogenous Metabolite
  3. Ramiprilat

Ramiprilat  (Synonyms: HOE 498 diacid; Ramipril diacid)

製品番号: HY-A0115 純度: 97.09%
COA 取扱説明書 Technical Support

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 has acute antlhypertensive effect. Ramiprilat can be used for high blood pressure and heart failure research.

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Ramiprilat

Ramiprilat 構造式

CAS 番号 : 87269-97-4

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 121 在庫あり
Solution
10 mM * 1 mL in DMSO USD 121 在庫あり
Solid
1 mg $47 在庫あり
5 mg $110 在庫あり
10 mg $160 在庫あり
25 mg $320 在庫あり
50 mg   お問い合わせ  
100 mg   お問い合わせ  

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Endogenous Metabolite アイソフォーム固有の製品をすべて表示:

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製品説明

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 has acute antlhypertensive effect. Ramiprilat can be used for high blood pressure and heart failure research[1][2][3][4][5].

IC50 & Target

Ki: 7 pM (ACE)[1]

体外実験

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 I2 (PGI2) release in endothelial cells[2].

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

体内実験

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
t1/2 k10 (h) 0.16 (0.09-0.31) 0.13 (0.10-0.16) 0.17 (0.10-0.27)
Vc (L/kg) 0.15
Vc/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
Kd (nmol/L) 1.35 1.47 1.19
fcirc (%) 5.01 5.80 6.08
Bmax (nmol/L) 109.46 79.31 91.72
Pmax (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.

分子量

388.46

分子式

C21H28N2O5

CAS 番号
Appearance

Solid

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

Structure Classification
Initial Source
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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
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. 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)

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

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始)

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体積 (開始)

V1

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体内:

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 (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.

    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 (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.

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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g

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(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).
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.
純度とドキュメンテーション

純度: 97.45%

参考文献

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. 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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  • Molarity Calculator

  • Dilution Calculator

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

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The dilution calculator equation

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

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
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    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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製品名:
Ramiprilat
製品番号:
HY-A0115
数量:
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