This product has recently been released.
This product is freeze dried. All water molecules have been removed.
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Bosentan is a dual antagonist of the ET-A and ET-B Endothelin receptors, shown to inhibit Endothelin-1 radioligand binding to ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively. in vitro it competitively inhibits aortic contractions induced by Endothelin-1 and tracheal contractions induced by Sarafotoxin S6C with pA2 of 7.2 and 6.0, respectively1. Bosentan is orally bioavailable and active in vivo2.
Bosentan hydrate (Ro 47-0203), is a synthetic nonpeptide compound that acts as an antagonist of endothelin A (ET-A) and endothelin B (ET-B) receptors. Bosentan hydrate is obtained by structural optimization of Ro 46-2005, a less potent ET-A/ET-B antagonist that is orally bioavailable and active in vivo. Bosentan hydrate competitively inhibits the specific binding of radioligand endothelin-1 to ET-A receptors in human smooth muscle cells with Ki value of 4.7 nM, and to ET-B receptors in human placenta with a Ki of 95 nM1. Bosentan may be used as a useful drug in the management of clinical disorders associated with vasoconstriction1,2.
ET-A receptors are predominantly detected in peripheral tissues, especially in vascular smooth muscle tissues where they mediate vasoconstriction. They are also expressed in several 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 present in medium- and large-sized cell bodies of human trigeminal ganglia.
ET-A receptor has high affinity for endothelin-1 and endothelin-2 and relatively low affinity for endothelin-3, while ET-B receptor has high affinity equally for all endothelin isopeptides3,4.
Alomone Labs is pleased to offer Bosentan hydrate (#B-170).
- Anti-Endothelin Receptor A (#AER-001)
- Anti-Endothelin Receptor B (#AER-002)
- Guinea pig Anti-Endothelin Receptor B (#AGP-037)
- Endothelin Receptor Agonist Explorer Kit (#EK-255)
- Endothelin Receptor Antagonist Explorer Kit (#EK-256)
- Endothelin Receptor Pharmacology Explorer Kit (#EK-257)
- Sarafotoxin S6b (#SPE-160)
- BQ-3020 (#SPE-200)
- IRL-1620 (#SPE-220)
- [Ala1,3,11,15] Endothelin-1 (#SPE-240)
- IRL 2500 (#I-190)
- ACT-132577 (#A-350)
- A-192621 (#A-360)
- BQ788 (#B-175)
- BQ788 sodium salt (#B-176)
- Ro46-8443 (#R-185)
- Darusentan (#D-265)