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

Aprocitentan (Synonyms: ACT-132577)

Cat. No.: HY-15895 Purity: 98.13%
Handling Instructions

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

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

Aprocitentan Chemical Structure

Aprocitentan Chemical Structure

CAS No. : 1103522-45-7

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 505 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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

IC50 & Target[1]

ETA

3.4 nM (IC50)

ETA

6.7 (pA2)

ETB

987 nM (IC50)

ETB

5.5 (pA2)

In Vitro

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].

In Vivo

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].

Clinical Trial
Molecular Weight

546.19

Formula

C₁₆H₁₄Br₂N₆O₄S

CAS No.

1103522-45-7

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 46 mg/mL (84.22 mM)

*"≥" means soluble, but saturation unknown.

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
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

AprocitentanACT-132577ACT132577ACT 132577Endothelin ReceptorInhibitorinhibitorinhibit

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