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CYP1A2 substrates

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By Targets:	Cholinesterase (ChE) (2) Cytochrome P450 (6) Proton Pump (1) Reference Standards (1)
By Research Areas:	Cancer (1) Inflammation/Immunology (1) Metabolic Disease (2) Neurological Disease (5)

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-111338

Tacrine 5+ Cited Publications	Cholinesterase (ChE)	Neurological Disease
Tacrine is an effective oral acetylcholine (AChE) inhibitor (IC₅₀ = 109 nM) and also acts as an active substrate for *CYP1A2*. Tacrine can restore cognitive dysfunction in elderly rats. Tacrine can cause liver toxicity and is used in research related to Alzheimer's disease .

HY-N5132

(-)-Fenchone	Cytochrome P450	Others
(-)-Fenchone is a bicyclic monoterpene and serves as a substrate for human liver microsomal cytochrome P450 enzymes CYP2A6 and CYP2B6. (-)-Fenchone is not metabolized by human CYP1A1, CYP1A2, CYP1B1, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, or CYP3A4 enzymes. (-)-Fenchone undergoes hydroxylation to produce 6-exo-hydroxyfenchone, 6-endo-hydroxyfenchone, and 10-hydroxyfenchone. During the metabolism of (-)-Fenchone, CYP2A6 may play a more important role than CYP2B6 .

HY-W267897

7-Benzyloxy-4-(trifluoromethyl)coumarin 7-BFC	Cytochrome P450	Others
7-Benzyloxy-4-(trifluoromethyl)coumarin (7-BFC) is a coumarin fluorescent substrate. 7-Benzyloxy-4-(trifluoromethyl)coumarin is a substrate for cDNA-expressed CYP1A2 and CYP3A4 and is metabolized to 7-hydroxy-4-trifluoromethylcoumarin (HFC). 7-Benzyloxy-4-(trifluoromethyl)coumarin is used for rapid CYP isoform metabolism and inhibition screening studies .

HY-116780A

Prothipendyl hydrochloride	Cytochrome P450	Neurological Disease
Prothipendyl hydrochloride is a tricyclic azaphenothiazine neuroleptic agent. Prothipendyl hydrochloride is a substrate of the CYP isozymes CYP1A2, CYP2D6, CYP2C19 and CYP3A4. Prothipendyl hydrochloride has sedating and psychomotorically damping effects. Prothipendyl hydrochloride can be used for psychomotoric agitation, sleep disorder and anxiety research .

HY-W015697

3-Methylquinoline	Cytochrome P450	Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
3-Methylquinoline is a selective cytochrome P450 (CYP1A2) inhibitor with an IC₅₀ of 13 μM. 3-Methylquinoline can reduce the metabolic clearance of CYP1A2 substrate drugs. 3-Methylquinoline can inhibit the activation of carcinogenic precursors .

HY-D0144

Resorufin methyl ether Methoxyresorufin	Cytochrome P450	Others
Resorufin methyl ether (Methoxyresorufin) is a cytochrome P450 fluorometric substrate . Resorufin methyl ether is a relatively specific substrate for CYP1A2 activity in rodents .

HY-124158

KR-60436	Proton Pump	Metabolic Disease
KR-60436 is a reversible H ⁺/K ⁺-ATPase inhibitor. KR-60436 can potently inhibit the metabolism of CYP1A2 substrates .

HY-116780

Prothipendyl	Cytochrome P450	Neurological Disease
Prothipendyl is a tricyclic azaphenothiazine neuroleptic agent. Prothipendyl is a substrate of the CYP isozymes CYP1A2, CYP2D6, CYP2C19 and CYP3A4. Prothipendyl has sedating and psychomotorically damping effects. Prothipendyl can be used for psychomotoric agitation, sleep disorder and anxiety research .

HY-111338R

Tacrine (Standard)	Cholinesterase (ChE) Reference Standards	Neurological Disease
Tacrine (Standard) is the analytical standard of Tacrine. This product is intended for research and analytical applications. Tacrine is an effective oral acetylcholine (AChE) inhibitor (IC50 = 109 nM) and also acts as an active substrate for CYP1A2. Tacrine can restore cognitive dysfunction in elderly rats. Tacrine can cause liver toxicity and is used in research related to Alzheimer's disease .

Resorufin methyl ether Methoxyresorufin	Fluorescent Dye
Resorufin methyl ether (Methoxyresorufin) is a cytochrome P450 fluorometric substrate . Resorufin methyl ether is a relatively specific substrate for CYP1A2 activity in rodents .

(-)-Fenchone	Structural Classification Other Monoterpenes Classification of Application Fields Terpenoids Other Diseases Umbelliferae Plants Vernonia Schreb. Disease Research Fields Source Classification	Cytochrome P450
(-)-Fenchone is a bicyclic monoterpene and serves as a substrate for human liver microsomal cytochrome P450 enzymes CYP2A6 and CYP2B6. (-)-Fenchone is not metabolized by human CYP1A1, CYP1A2, CYP1B1, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, or CYP3A4 enzymes. (-)-Fenchone undergoes hydroxylation to produce 6-exo-hydroxyfenchone, 6-endo-hydroxyfenchone, and 10-hydroxyfenchone. During the metabolism of (-)-Fenchone, CYP2A6 may play a more important role than CYP2B6 .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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CYP1A2 substrates

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