Free shipping on all orders over $ 500

Aprocitentan

Cat. No. M13956

All AbMole products are for research use only, cannot be used for human consumption.

Aprocitentan Structure
Synonym:

ACT-132577

Size Price Availability Quantity
10mM*1mL in DMSO USD 140  USD140 In stock
1mg USD 53  USD53 In stock
5mg USD 115  USD115 In stock
10mg USD 165  USD165 In stock
25mg USD 310  USD310 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

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. Aprocitentan (ACT-132577) achieves full inhibition of intracellular calcium increase induced by ET-1 on nonrecombinant cells.

Chemical Information
Molecular Weight 546.19
Formula C16H14Br2N6O4S
CAS Number 1103522-45-7
Form Solid
Solubility (25°C) DMSO 23 mg/mL
Storage 2-8°C, protect from light
References

[1] Fabio Angeli, et al. Aprocitentan, A Dual Endothelin Receptor Antagonist Under Development for the Treatment of Resistant Hypertension

[2] Emily K McCoy, et al. Aprocitentan (a Dual Endothelin-Receptor Antagonist) for Treatment-Resistant Hypertension

[3] Patricia N Sidharta, et al. Absorption, Distribution, Metabolism, and Excretion of Aprocitentan, a Dual Endothelin Receptor Antagonist, in Humans

[4] Patricia N Sidharta, et al. Effects of Multiple-Dose Administration of Aprocitentan on the Pharmacokinetics of Rosuvastatin

[5] Patricia N Sidharta, et al. Effect of Multiple-Dose Aprocitentan Administration on the Pharmacokinetics of Midazolam in Healthy Male Subjects

Related Endothelin Receptor Products
Zibotentan

Zibotentan (ZD4054) is a more selective and specific endothelin-A receptor (ETAR) antagonist with an IC50 value of 21 nM.

Ambrisentan

Ambrisentan is an orally active, highly selective antagonist of the endothelin-1 type A receptor.

Sitaxsentan sodium

Sitaxsentan (TBC-11251) is an orally active, highly selective antagonist of endothelin A receptors.

Macitentan

Macitentan is an orally-active, tissue-targeting dual ET receptor antagonist.

Bosentan Hydrate

Bosentan is an endothelin (ET) receptors antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively.

  Catalog
Abmole Inhibitor Catalog




Keywords: Aprocitentan, ACT-132577 supplier, Endothelin Receptor, inhibitors, activators

All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.



Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.