A CYP4A11 and CYP4F2 inhibitor
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TP-0472993

Item No. 39757

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[4-[[[6-(1H-pyrazol-3-yl)-3-pyridinyl]oxy]methyl]-1-piperidinyl]-ethanone
CAS Number
2126874-77-7
Molecular Formula
C16H20N4O2
Formula Weight
300.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly Soluble: 1-10 mg/ml
SMILES
O=C(C)N1CCC(CC1)COC2=CC=C(C3=NNC=C3)N=C2
InChi Code
InChI=1S/C16H20N4O2/c1-12(21)20-8-5-13(6-9-20)11-22-14-2-3-15(17-10-14)16-4-7-18-19-16/h2-4,7,10,13H,5-6,8-9,11H2,1H3,(H,18,19)
InChi Key
GNQGSUOEYQIORN-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $113

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    10 mg

    $214

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    25 mg

    $449

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    50 mg

    $674

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    Product Description

    TP-0472993 is an inhibitor of the cytochrome P450 (CYP) isoforms CYP4A11 and CYP4F2 (IC50s = 140 and 40 nM, respectively).1 It is selective for CYP4A11 and CYP4F2 over a panel of eight additional CYPs at 10 µM. TP-0472993 inhibits 20-HETE (Item No. 90030) production in rat renal microsomes (IC50 = 347 nM). In vivo, TP-0472993 (0.03-1 mg/kg) inhibits 20-HETE production in rats. It also reduces renal fibrosis and IL-1β and TNF-α levels in a mouse model of folic acid-induced nephropathy and a mouse model of unilateral ureteral obstruction-induced neuropathy when administered at a dose of 3 mg/kg.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kawamura, M., Kobashi, Y., Tanaka, H., et al. Discovery of novel pyrazolylpyridine derivatives for 20-hydroxyeicosatetraenoic acid synthase inhibitors with selective CYP4A11/4F2 inhibition. J. Med. Chem. 65(21), 14599-14613 (2022).

    2. Hirata, T., Ohara, H., Kojima, N., et al. Renoprotective effect of TP0472993, a novel and selective 20-hydroxyeicosatetraenoic acid synthesis inhibitor, in mouse models of renal fibrosis. J. Pharmacol. Exp. Ther. 386(1), 56-69 (2023).