Date published: 2025-9-18

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CYP2C8 Inhibitors

CYP2C8, a pivotal enzyme within the cytochrome P450 family, plays an essential role in the metabolic processing of a wide variety of xenobiotics, including many drugs and environmental chemicals. Located predominantly in the liver, CYP2C8 facilitates the oxidation of substances, rendering them more soluble for excretion and thus less harmful to the body. Its activity influences the pharmacokinetics of drugs, affecting their absorption, distribution, metabolism, and excretion (ADME) profiles. By converting lipophilic compounds into more hydrophilic metabolites, CYP2C8 is integral to the body's defense mechanism against toxic substances, underscoring the enzyme's critical role in maintaining physiological balance and impeding the accumulation of toxic compounds. The inhibition of CYP2C8 can significantly alter the metabolic clearance of its substrates, leading to variations in drug efficacy. Inhibition can occur through various mechanisms, including competitive inhibition, where compounds directly compete with the enzyme's natural substrates for binding sites, thereby reducing its metabolic activity. Non-competitive inhibition also plays a role, where the inhibitor binds to a site other than the active site, causing a conformational change that reduces enzyme activity without directly competing with substrate binding. Additionally, mechanism-based inhibition involves the formation of a stable complex between the enzyme and the inhibitor, leading to irreversible enzyme inactivation. Such inhibition can result from specific chemical interactions that modify the enzyme's active site, making it unable to bind to its substrates. Understanding these inhibitory mechanisms is crucial for predicting drug-drug interactions and for the development of strategies to manage and mitigate adverse effects associated with reduced CYP2C8 activity.

Items 1 to 10 of 14 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Gemfibrozil 1-O-β-Glucuronide

91683-38-4sc-221665C
sc-221665
sc-221665-CW
sc-221665A
sc-221665B
sc-221665B-CW
sc-221665D
sc-221665E
500 µg
1 mg
1 mg
2 mg
5 mg
5 mg
10 mg
25 mg
$326.00
$500.00
$653.00
$842.00
$1581.00
$1734.00
$2856.00
$6050.00
2
(1)

Gemfibrozil 1-O-β-Glucuronide (CAS 91683-38-4) is a metabolite of the drug gemfibrozil. It acts as an inhibitor of the Cytochrome P450 2C8 (CYP2C8) enzyme, which is involved in the metabolism of various drugs and endogenous compounds in the liver.

Gemfibrozil

25812-30-0sc-204764
sc-204764A
5 g
25 g
$65.00
$262.00
2
(2)

Gemfibrozil acts as a competitive inhibitor of CYP2C8, directly interacting with the enzyme's active site to decrease the metabolism of substrates processed by this enzyme, leading to potential alterations in their pharmacokinetic profiles.

Terfenadine

50679-08-8sc-208421A
sc-208421B
sc-208421
500 mg
1 g
5 g
$43.00
$70.00
$118.00
(1)

Terfenadine exhibits distinctive interactions with CYP2C8, characterized by its ability to form stable complexes through π-π stacking and hydrophobic contacts. The compound's unique structural features enable selective binding, influencing the enzyme's catalytic efficiency. Its metabolic pathway involves intricate electron transfer mechanisms, which can alter reaction kinetics. Furthermore, terfenadine's conformational flexibility allows it to adapt within the active site, potentially affecting substrate turnover rates and enzyme regulation.

Clopidogrel Acyl-β-D-glucuronide

1314116-53-4 (S-isomer)sc-217936
1 mg
$970.00
4
(0)

Clopidogrel Acyl-β-D-glucuronide (CAS 1314116-53-4, S-isomer) is a metabolite of the drug clopidogrel. It acts as an inhibitor of the Cytochrome P450 2C8 (CYP2C8) enzyme.

Trimethoprim

738-70-5sc-203302
sc-203302A
sc-203302B
sc-203302C
sc-203302D
5 g
25 g
250 g
1 kg
5 kg
$66.00
$158.00
$204.00
$707.00
$3334.00
4
(1)

Trimethoprim inhibits CYP2C8 through a mechanism that likely involves direct competition for the enzyme's active site, which can interfere with the normal metabolic processing of substrates by this enzyme.

Clopidogrel

113665-84-2sc-507403
1 g
$120.00
1
(0)

Clopidogrel inhibits CYP2C8 activity through a mechanism that may involve the formation of a metabolite that interacts with the enzyme, leading to decreased metabolic processing of substrates that depend on this enzyme for clearance.

2′-Deoxy-2′,2′-difluorocytidine

95058-81-4sc-275523
sc-275523A
1 g
5 g
$56.00
$128.00
(1)

2'-Deoxy-2',2'-difluorocytidine acts as an inhibitor of CYP2C8, potentially through direct interaction or competitive inhibition, affecting the enzyme's ability to metabolize other substrates, including those used in chemotherapy.

Repaglinide

135062-02-1sc-219959
sc-219959A
sc-219959B
100 mg
250 mg
1 g
$215.00
$414.00
$1331.00
3
(0)

Repaglinide's inhibition of CYP2C8 can lead to reduced metabolic clearance of the drug itself and other substrates, potentially due to competitive inhibition or interaction with the enzyme's active site.

Taxol

33069-62-4sc-201439D
sc-201439
sc-201439A
sc-201439E
sc-201439B
sc-201439C
1 mg
5 mg
25 mg
100 mg
250 mg
1 g
$40.00
$73.00
$217.00
$242.00
$724.00
$1196.00
39
(2)

Taxol is known to inhibit CYP2C8, possibly through competitive interaction with the enzyme, which can affect the metabolic processing and pharmacokinetics of co-administered drugs metabolized by CYP2C8.

Ritonavir

155213-67-5sc-208310
10 mg
$122.00
7
(1)

Ritonavir exhibits inhibition of CYP2C8 among other cytochrome P450 enzymes, through a mechanism that may involve direct enzyme binding or the formation of metabolite-intermediate complexes that reduce enzyme activity.