Potent, selective ET A receptor antagonist (IC 50 values are 7.3 and 18,000 nM for ET A and ET B endothelin receptors respectively). Some ability to cross the blood-brain barrier. Anti-ischemic activity in vivo .
Storage Temp
Store at -20°C,Desiccated
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
ANTAGONIST
Mechanism of action
Antagonist of ET A receptor
Note
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one week. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
1.Maayah ZH et al.. (2020) Breast cancer diagnosis is associated with relative left ventricular hypertrophy and elevated endothelin-1 signaling.. BMC Cancer, 20 (751). [PMID:32787791]
2.Wu Q et al.. (2018) CT perfusion imaging of cerebral microcirculatory changes following subarachnoid hemorrhage in rabbits: Specific role of endothelin-1 receptor antagonist.. Brain Res, 1701 (196-203). [PMID:30244111]
3.Kobayashi Y et al.. (2021) Early manifestations and differential gene expression associated with photoreceptor degeneration in Prom1-deficient retina.. Dis Model Mech, 14 (11):[PMID:34664634]
4.Furukawa A et al.. (2018) Endothelin Signaling Contributes to Modulation of Nociception in Early-stage Tongue Cancer in Rats.. Anesthesiology, 128 (6):(1207-1219). [PMID:29461271]
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K2218158