|Other names||· N-hydroxy-N’-(4-n-butyl-2-methylphenyl)Formamidine,
|Appearance||Light pink solid|
|Benefits||20-HETE inhibitor, cure for cerebral-vascular disease|
What is HET0016?
HET0016 is one of the latest products from Herb Nutritionals Co., Ltd, and not so much information available from the internet. However, in order to have you a better understanding of what HET0016 is, we offer the detailed information from our lab and chemists.
HET0016 is a potent and selective inhibitor of the biosynthesis of 20-HETE acting via inhibition of CYP4A. It inhibits cerebrovascular constriction induced by Ca2+ or arachidonate and inhibits angiogenesis and endothelial cell sprouting in various models.
What is 20-HETE?
In order to understand HET0016 better, you need to know 20-HETE first. 20-HETE, also known as 20-hydroxy Arachidonic Acid with CAS number 79551-86-3, is a major biologically active cytochrome P450 (CYP450) metabolite of arachidonic acid in the kidney and liver. It regulates renal vascular and tubular functions as well as vascular tone in the cerebral circulation. HET0016 is an inhibitor of 20-HETE formation in human renal microsomes with an IC50 of 8.9 nM, selectively inhibiting CYP4A and 4F isoforms. HET0016 inhibits CYP2C9, CYP2D6, and CYP3A4, enzymes important in drug metabolism, significantly less effectively with IC50s in the µM range. The IC50 values for inhibition of cyclooxygenase and epoxyeicosatrienoic acids (EETs) formation are 2.3 and 2.8 µM, respectively.
Benefits of HET0016
There are patents and experiments available on HET0016 as the 20-HETE Synthesizing enzyme inhibitors, thus as therapy for cerebral-vascular disease.
Reduced cerebral blood flow can cause a range of problems from light headaches to severe brain damage and health. There are many situations that can lead to reduced cerebral blood flow. Examples of such situations include hemorrhagic stroke, brain injuries, occlusive stroke, cerebral vasospasm and hypotension.
Subarachnoid hemorrhage (SAH) accounts for 5-10% of all strokes. The incidence is 2-20 events per 100,000 populations per year with a case fatality rate of 20% to 60%. Subarachnoid hemorrhage occurs most commonly after rupture of cerebral aneurysms or head trauma leading to subarachnoid bleeding and clot formation. After the bleeding, cerebral blood flow initially falls due to an elevated cerebrospinal fluid pressure that reduces effective perfusion pressure combined with the release of vascular tone.
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