Electrolyte and fluid transport in the kidney are regulated in part by arachidonic acid and its metabolites. (±)17-HETE is the racemic version of a cytochrome P450 (CYP450) metabolite of arachidonic acid that has stereospecific effects on sodium transport in the kidney. At a concentration of 2 µM the (S)-enantiomer of 17-HETE inhibits proximal tubule ATPase activity by as much as 70%, whereas the (R)-isomer is inactive.
17-HETE is arachidonic acid metabolite through cytochrome P-450 pathways, which consists of 17R-HETE and 17S-HETE enantiomers. 17-HETE serves as allosteric activator of the cytochrome P450 1B1 and inhibitor of ATPase, induces cardic hypertrophy[1][2].
IC50&Target
CYP1B1
体外研究
17-HETE (5-20 μM) promotes the development of human cardiac hypertrophy by enhancing the activity and protein levels of CY1B1.
Real Time qPCR
Cell Line:
AC16
Concentration:
5-20 µM
Incubation Time:
24 hours
Result:
Increased mRNA levels of β-MHC and ANP, increased cell surface area.
Western Blot Analysis
Cell Line:
AC16
Concentration:
20 µM
Incubation Time:
24 hours
Result:
Increased expression of CYP 1B1.
体内研究
17-HETE (1-20 μg, arterial injection) stereospecifically (S-enantiomer) inhibits proximal tubular ATPase activity in New Zealand white rabbits [2].
Animal Model:
New Zealand White rabbit
Dosage:
1-20 μg
Administration:
injection into artery
Result:
17S inhibited more than 70% ATPase activity at the concentration of 2 μM, while 17R enantiomer remained inactive.
分子式
C20H32O3
分子量
320.5
CAS号
128914-47-6
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Isse FA, et al., 17-(R/S)-hydroxyeicosatetraenoic acid (HETE) induces cardiac hypertrophy through the CYP1B1 in enantioselective manners. Prostaglandins Other Lipid Mediat. 2023 Oct;168:106749.
[2]. Carroll MA, e al., Cytochrome P-450-dependent HETEs: profile of biological activity and stimulation by vasoactive peptides. Am J Physiol. 1996 Oct;271(4 Pt 2):R863-9.