0.1-10 nM.

A-192621 is a selective antagonist of ET-B endothelin receptors, inhibiting ET-1 binding to ETA and ET-3 binding to ETB receptors with IC₅₀ values of 4280 nM and 4.5 nM, respectively¹.
In vivo, A-192621 inhibits ETB-mediated dilatory and pressor responses induced by Sarafotoxin 6c (ED₅₀ = 30 mg/kg), and causes an elevation of arterial blood pressure and plasma ET-1 level².

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored desiccated at -20°C.

Soluble in DMSO or NaOH 1Eq. Centrifuge all products before use (10000 x g 5 min).

Up to three months at -20°C.

1-100 µM.

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.

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored desiccated at -20°C.

Soluble in DMSO with gentle warming. Centrifuge all products before use (10000 x g 5 min).

Up to three months at -20°C.

0.01-10 nM.

Atrasentan is a potent and highly selective antagonist of ET-A endothelin receptors, exhibiting a 1000-fold selectivity for ET-A over ET-B receptors, inhibiting endothelin-1 radioligand binding with an IC₅₀ of 0.36 nM and endothelin-1-stimulated phosphoinositol hydrolysis with IC₅₀ of 0.16 nM¹.

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.

Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).

Up to three months at -20°C.

0.1-100 nM.

Avosentan is a selective antagonist of ET-A endothelin receptors, shown to significantly inhibit endothelin-1-induced contractions in isolated porcine ciliary arteries at 10 nM-1 µM¹.

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.

Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).

Up to three months at -20°C.

100 nM – 10 µM.

BMS 182874 hydrochloride is a potent, selective and competitive antagonist of ET-A endothelin receptors. It exhibits a 1000-fold selectivity for ET-A over ET-B receptors, inhibiting endothelin-1 radioligand binding to ET-A and ET-B with K_i of 61 nM and >50 µM, respectively. In vitro, BMS 182874 inhibits endothelin-1 induced calcium mobilization with K_B of 140 nM¹. BMS 182874 is orally bioavailable and active in vivo^1,2.

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 +4°C.

Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).

Up to three months at -20°C.

10-100 nM.

BQ788 is a potent and highly specific ET-B receptor antagonist, exhibiting selectivity for ET-B over ET-A human receptors when inhibiting the binding of [¹²⁵I]-Endothelin-1 (IC₅₀ of 1.2 nM and 1300 nM, respectively)¹.

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.

Soluble in DMSO and ethanol. Centrifuge all products before use (10000 x g 5 min).

Up to three months at -20°C.

10-100 nM.

BQ788 is a potent and highly specific ET-B receptor antagonist, exhibiting selectivity for ET-B over ET-A human receptors when inhibiting the binding of [¹²⁵I]-Endothelin-1 (IC₅₀ of 1.2 nM and 1300 nM, respectively)¹.

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored desiccated at -20°C.

Soluble in DMSO and ethanol. Centrifuge all products before use (10000 x g 5 min).

Up to three months at -20°C.

10 nM – 10 µM.

BQ-123, a cyclic peptide provided as a sodium salt, is a potent and selective antagonist of ET-A endothelin receptors, exhibiting a 1000-fold selectivity for ET-A over ET-B receptors (inhibiting endothelin-1 radioligand binding to ET-A and ET-B with IC₅₀ of 22 nM and 18 µM, respectively). In vitro, BQ-123 inhibits endothelin-1 induced contractions of porcine coronary artery with K_B of 40 nM¹.

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored desiccated at -20°C.

Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).

Up to three months at -20°C.

1 nM – 1 µM.

Darusentan is a selective antagonist of ET-A Endothelin receptors, inhibiting Endothelin-1 radioligand binding to ET-A and ET-B receptors with K_i of 6 nM and 371 nM, respectively¹. in vitro Darusentan inhibits Endothelin-induced vascular contractility in isolated endothelium-denuded rat aortic rings with pA₂ of 8.1². Darusentan is orally bioavailable and active in vivo³.

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.

Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).

Up to three months at -20°C.

1 nM – 1 µM.

FR 139317 is a potent and selective antagonist of ET-A receptors, inhibiting Endothelin-1 radioligand binding to ET-A and ET-B with K_i of 1 nM and 7.3 µM, respectively¹. in vitro, FR 139317 shifted Endothelin-1-induced contractile response curve to the right with pA₂ of 7.2 in isolated rabbit aorta².

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored desiccated at -20°C.

Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).

Up to three months at -20°C.

0.1-10 µM.

IRL 2500 is a potent antagonist of endothelin ET-B receptors, exhibiting selectivity for ET-B over ET-A receptors when inhibiting the binding of [¹²⁵I]-Endothein-1 (IC₅₀ of 1.3 nM and 94 nM, respectively). IRL 2500 attenuates the effects of ETB-selective agonists in vitro and in-vivo, such as saraphotoxin S6c-mediated dog saphenous vein contraction or IRL-1620-induced transient decrease in arterial pressure and increase in renal vascular resistance in rat^1,2.

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored desiccated at -20°C.

Soluble in NaOH. Centrifuge all products before use (10000 x g 5 min).

Up to three months at -20°C.

1-100 nM.

PD-156707 is a potent and selective antagonist of the ET-A Endothelin receptors, inhibiting Endothelin-1 radioligand binding to ET-A and ET-B receptors with K_i of 0.17 nM and 133.8 nM, respectively. in vitro, PD-156707 inhibits ET-A and ET-B receptor-mediated arterial vasoconstriction with pA₂ of 7.5 and 4.7, respectively. PD-156707 is orally bioavailable and active in vivo¹.

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.

Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).

Up to three months at -20°C.

1-100 nM.

PD-164333 is a selective antagonist of the ET-A receptors, inhibiting Endothelin-1 radioligand binding to ET-A and ET-B receptors with K_d of 0.99 nM and 2.41 µM, respectively. in vitro, PD164333 shifts Endothelin-1 concentration-response curve to the right with pA₂ of 8.84 in isolated human saphenous vein¹.

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.

Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).

Up to three months at -20°C.

0.1-10 µM.

Ro 46-8443 is a non-peptide, selective and competitive antagonist of ET-B receptors. It shows over 100-fold selectivity for human ET-B in competitive binding assays (IC₅₀ of 34-69 nM), and competitively inhibits the binding of selective ET-B agonist [¹²⁵I]Sarafotoxin-S6c to porcine trachea membranes (IC₅₀ = 4.9 nM)¹.

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.

Up to 100 mM in DMSO. Centrifuge all products before use (10000 x g 5 min).

Up to three months at -20°C.

0.2-20 nM.

SB209670 is a potent mixed antagonist of ET-A and ET-B Endothelin receptors, shown to inhibit Endothelin-1 radioligand binding to human ET-A and ET-B with K_i of 0.2 nM and 18 nM, respectively. SB209670 inhibits Endothelin-1-evoked vasoconstriction in isolated vascular tissues in vitro, and is orally bioavailable and active in vivo¹.

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.

Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).

Up to three months at -20°C.

1-100 nM.

Sitaxsentan is a potent and selective antagonist of ET-A Endothelin receptors, inhibiting Endothelin-1 radioligand binding to human ET-A and ET-B receptors with IC₅₀ of 1.4 nM and 9.8 µM, respectively (a 7000-fold selectivity). in vitro, Sitaxsentan inhibits Endothelin-1 induced phosphoinositide turnover with a pA₂ of 8.0¹. Sitaxsentan is orally bioavailable and active in vivo^1,2.

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.

Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).

Up to three months at -20°C.

Synthetic

0.5 – 1 µM.

TAK-044 is a non-selective endothelin receptor antagonist¹.

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.

Soluble in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).

Up to four weeks at 4°C or three months at -20°C.

1 nM – 10 µM.

Zibotentan is a selective antagonist of ET-A Endothelin receptors, inhibiting Endothelin-1 radioligand binding to human ET-A with IC₅₀ of 21 nM (whilst showing no effect on ET-B at 10 µM). Zibotentan is orally bioavailable and active in vivo.¹

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.

Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).

Up to three months at -20°C.