Chemical Structure : TP0472993
CAS No.:
2126874-77-7
TP0472993
(TP 0472993)
Catalog No.: PC-20707Not For Human Use, Lab Use Only.
TP0472993 is a potent, selective 20-Hydroxyeicosatetraenoic acid (20-HETE) synthesis inhibitor, inhibits 20-HETE formation in human and rat renal microsomes with IC50 of 29 and 347 nM, respectively.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
TP0472993 is a potent, selective 20-Hydroxyeicosatetraenoic acid (20-HETE) synthesis inhibitor, inhibits 20-HETE formation in human and rat renal microsomes with IC50 of 29 and 347 nM, respectively.
TP0472993 concentration dependently inhibits 20-HETE production by CYP4F2 and CYP4A11 with IC50 values of 37 and 425 nM, respectively.
TP0472993 displays no an apparent affinity for 55 representative receptors, enzymes, ion channels and transporters at 30 uM.
Chronic treatment with TP0472993 (0.3 and 3 mg/kg, twice a day) attenuated the degree of kidney fibrosis in the folic acid nephropathy and the unilateral ureteral obstruction (UUO) mice.
TP0472993 reduced renal inflammation, as demonstrated by markedly reducing IL-1β and TNF-α levels in the renal tissue.
TP0472993 suppressed the kidney fibrosis progression via a reduction in the ERK1/2 and STAT3 signaling pathway.
Physicochemical Properties
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M.Wt
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300.36
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Formula
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C16H20N4O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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CC(N1CCC(COC2=CC=C(C3=CC=NN3)N=C2)CC1)=O
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References
1. Takashi Hirata, et al. J Pharmacol Exp Ther. 2023 May 4;JPET-AR-2022-001521.
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