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Aprocitentan

$142$2,100

Products Details

Product 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].

Web ID

– HY-15895

Storage Temperature

– -20°C, 3 years; 4°C, 2 years (Powder)

Shipping

– Room Temperature

Applications

– COVID-19-immunoregulation

Molecular Formula

– C16H14Br2N6O4S

References

– [1]Zhang J, et al. Pharmacokinetic study of ACT-132577 in rat plasma by ultra performance liquid chromatography-tandem mass spectrometry. Int J Clin Exp Med. 2015 Oct 15;8(10):18420-6|[2]Iglarz M, et al. Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonist. J Pharmacol Exp Ther. 2008 Dec;327(3):736-45.

CAS Number

– 1103522-45-7

Molecular Weight

– 546.19

Compound Purity

– 99.98

SMILES

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

Clinical Information

– Phase 3

Research Area

– Cardiovascular Disease; Endocrinology

Solubility

– DMSO : 25 mg/mL (ultrasonic;warming;heat to 60°C)

Target

– Endothelin Receptor

Isoform

– ETA;ETB

Pathway

– GPCR/G Protein

Product type

– Reference compound

Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.

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