2. GPCR/G Protein
  3. Endothelin Receptor
  4. Aprocitentan

Aprocitentan  (Synonyms: ACT-132577)

製品番号: HY-15895 純度: 99.55%
COA 取扱説明書 Technical Support

Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of Macitentan. Aprocitentan is an orally active dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively. Aprocitentan is an antihypertensive agent.

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Aprocitentan

Aprocitentan 構造式

CAS 番号 : 1103522-45-7

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 237 在庫あり
Solution
10 mM * 1 mL in DMSO USD 237 在庫あり
Solid
1 mg $80 在庫あり
5 mg $197 在庫あり
10 mg $285 在庫あり
25 mg $497 在庫あり
50 mg $696 在庫あり
100 mg $940 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 3 publication(s) in Google Scholar

Other Forms of Aprocitentan:

Aprocitentan 関連抗体

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

すべてのアイソフォームを表示
ETA ETB

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製品説明

Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of Macitentan. Aprocitentan is an orally active dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively. Aprocitentan is an antihypertensive agent[1].

IC50 & Target[1]

ETA

3.4 nM (IC50)

ETA

6.7 (pA2)

ETB

987 nM (IC50)

ETB

5.5 (pA2)

Cellular Effect
Cell Line Type Value Description References
CHO IC50
3.4 nM
Compound: 71
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
[PMID: 22862294]
CHO IC50
3.4 nM
Compound: 75
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
Displacement of [125I]-ET-1 from human ETA receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
[PMID: 27321813]
CHO IC50
987 nM
Compound: 71
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
[PMID: 22862294]
CHO IC50
987 nM
Compound: 75
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
Displacement of [125I]-ET-1 from human ETB receptor expressed in CHO cell membranes after 2 hrs by scintillation counting
[PMID: 27321813]
体外実験

Aprocitentan (ACT-132577) achieves full inhibition of intracellular calcium increase induced by ET-1 on nonrecombinant cells (primary human pulmonary smooth muscle cells and rat aortic smooth muscle cell line A10 and mouse fibroblast cell line 3T3)[1].

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

Aprocitentan 関連抗体
体内実験

Aprocitentan (ACT-132577) has a volume of distribution greater than the plasma volume and a longer half-life than its parent compound in the rat[1]. In rat plasma, the mean recovery of Aprocitentan (ACT-132577) ranges from 82.6% to 90.6%, matrix effect of Aprocitentan (ACT-132577) in rat plasma ranges from 101.4% to 115.2%[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
分子量

546.19

分子式

C16H14Br2N6O4S
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=S(N)(NC1=NC=NC(OCCOC2=NC=C(Br)C=N2)=C1C3=CC=C(Br)C=C3)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 25 mg/mL (45.77 mM; ultrasonic and warming and heat to 60°C; 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 1.8309 mL 9.1543 mL 18.3086 mL
5 mM 0.3662 mL 1.8309 mL 3.6617 mL
10 mM 0.1831 mL 0.9154 mL 1.8309 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

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 (4.58 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.58 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)

g

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).
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: 99.55%

COA (250 KB) HNMR (165 KB) LCMS (103 KB)

取扱説明書 (2659 KB)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8309 mL 9.1543 mL 18.3086 mL 45.7716 mL
5 mM 0.3662 mL 1.8309 mL 3.6617 mL 9.1543 mL
10 mM 0.1831 mL 0.9154 mL 1.8309 mL 4.5772 mL
15 mM 0.1221 mL 0.6103 mL 1.2206 mL 3.0514 mL
20 mM 0.0915 mL 0.4577 mL 0.9154 mL 2.2886 mL
25 mM 0.0732 mL 0.3662 mL 0.7323 mL 1.8309 mL
30 mM 0.0610 mL 0.3051 mL 0.6103 mL 1.5257 mL
40 mM 0.0458 mL 0.2289 mL 0.4577 mL 1.1443 mL
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Aprocitentan Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

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
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.

Keywords:

Aprocitentan1103522-45-7ACT-132577ACT132577ACT 132577Endothelin ReceptorInhibitorinhibitorinhibit

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