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Home / Biochemicals / Small Molecules

ACT-132577

SKU : BHB21300025

An Antagonist of Endothelin Receptors

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Alomone Labs

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Mfr.No.	A-350, A-350_10 mg, A-350_25 mg, A-350_5 mg, A-350_50 mg
Description	ACT-132577 (#A-350) is a highly pure, synthetic, and biologically active compound.
Molecular Formula	C16H14Br2N6O4S.
Synonyms	Synthetic
Background	ACT-132577 is an active metabolite of Macitentan that acts as an endothelin B (ET-B) and endothelin A (ET-A) receptor antagonist. ACT-132577 antagonizes the specific binding of endothelin-1 on membranes of cells overexpressing ET-A and ET-B receptors with IC50 values of 3.4 nM and 987 nM, respectively1. It also has the ability to reach full inhibition of intracellular Ca2+ increase induced by endothelin-1 on non-recombinant cells1.Endothelin receptors belong to the superfamily of G-protein coupled receptors and include two subtypes: ET-A and ET-B. ET-A receptors are predominantly expressed in peripheral tissues, especially in vascular smooth muscle tissues to mediate vasoconstriction. They are also present in several different regions of the brain. ET-B receptors play an important role in regulating renal function and blood pressure and are expressed in sensory nerves. They are mainly detected in medium- and large-sized cell bodies of human trigeminal ganglia.The ET-A receptor has high affinity for endothelin-1 and endothelin-2 and relatively low affinity for endothelin-3, while the ET-B receptor has high affinity for all endothelin isopeptides2,3.
Shipping	Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C
Concentration	1-100 uM.
Reconstitution	Soluble in DMSO with gentle warming. Centrifuge all products before use (10000 x g 5 min).
Cas Number	1103522-45-7
Molecular Weight	546.19
Solubility	Soluble in DMSO with gentle warming. Centrifuge all products before use (10000 x g 5 min).
Target	Endothelin receptors
Activity	ACT-132577, a metabolite of macitentan, is a dual antagonist of ET-A and ET-B endothelin receptors, inhibiting binding of 125I-ET-1 to recombinant ET-A and ET-B receptors with IC50 values of 3.4 nM and 987 nM, respectively1.
Country Of Origin	Israel/IL
UNSPSC Code	41116134
Application	FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay
Lead Time	1-2 Business Days
Notes	Bioassay Tested: Yes Chemical Name: 5-(4-bromophenyl)-4-(2-(5-bromopyrimidin-2-yl)oxyethoxy)-6-(sulfamoylamino)pyrimidine.

Purity	>98%
Form	Lyophilized powder.
Storage	Storage After Reconstitution: The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles. Storage of solutions: Up to three months at -20°C.

Product Manual	SDS

Reference	Iglarz, M. et al. (2008) J. Pharmacol. Exp. Ther. 327, 736. Saeki, T. et al. (1991) Biochem. Biophys. Res. Commun. 179, 286. Xie, C. and Wang, D.H. (2009) Hypertension 54, 1298. Iglarz, M. et al. (2008) J. Pharmacol. Exp. Ther. 327, 736.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHB21300025-1	A-350_10 mg	10 mg	$406		Add to Cart
BHB21300025-2	A-350_25 mg	25 mg	$730		Add to Cart
BHB21300025-3	A-350_5 mg	5 mg	$235		Add to Cart
BHB21300025-4	A-350_50 mg	50 mg	$1148		Add to Cart

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