Cytochrome p450 comprises a superfamily of heme-thiolate proteins named for the spectral absorbance peak of their carbon-monoxide-bound species at 450 nm. Having been found in every class of organism, including Archaea, the p450 superfamily is believed to have originated from an ancestral gene that existed over 3 billion years ago. Repeated gene duplications have subsequently given rise to one of the largest of multigene families. These enzymes are notable both for the diversity of reactions that they catalyze and the range of chemically dissimilar substrates upon which they act. Cytochrome p450s support the oxidative, peroxidative and reductive metabolism of such endogenous and xenobiotic substrates as environmental pollutants, agrochemicals, plant allelochemicals, steroids, prostaglandins and fatty acids. In humans, Cytochrome p450s are best known for their central role in phase I drug metabolism where they are of critical importance to two of the most significant problems in clinical pharmacology: drug interactions and interindividual variability in drug metabolism.


Anti-infection >
Arenavirus Bacterial CMV Enterovirus Filovirus Fungal HBV HCV HIV HSV Influenza Virus Parasite Reverse Transcriptase RSV SARS-CoV
Antibody-drug Conjugate >
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Apoptosis >
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Autophagy >
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Antifolate APC ATM/ATR Aurora Kinase Casein Kinase CDK Checkpoint Kinase (Chk) CRISPR/Cas9 Deubiquitinase DNA Alkylator/Crosslinker DNA-PK DNA/RNA Synthesis Eukaryotic Initiation Factor (eIF) G-quadruplex Haspin Kinase HDAC HSP IRE1 Kinesin LIM Kinase (LIMK) Microtubule/Tubulin Mps1 Nucleoside Antimetabolite/Analog p97 PAK PARP PERK Polo-like Kinase (PLK) PPAR RAD51 ROCK Sirtuin SRPK Telomerase TOPK Topoisomerase Wee1
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5-HT Receptor Adenosine Receptor Adenylate Cyclase Adiponectin Receptor Adrenergic Receptor Angiotensin Receptor Bombesin Receptor Bradykinin Receptor Cannabinoid Receptor CaSR CCR CGRP Receptor Cholecystokinin Receptor CRFR CXCR Dopamine Receptor EBI2/GPR183 Endothelin Receptor GHSR Glucagon Receptor Glucocorticoid Receptor GNRH Receptor GPCR19 GPR109A GPR119 GPR120 GPR139 GPR40 GPR55 GPR84 Guanylate Cyclase Histamine Receptor Imidazoline Receptor Leukotriene Receptor LPL Receptor mAChR MCHR1 (GPR24) Melatonin Receptor mGluR Motilin Receptor Neurokinin Receptor Neuropeptide Y Receptor Neurotensin Receptor Opioid Receptor Orexin Receptor (OX Receptor) Oxytocin Receptor P2Y Receptor Prostaglandin Receptor Protease-Activated Receptor (PAR) Ras RGS Protein Sigma Receptor Somatostatin Receptor TSH Receptor Urotensin Receptor Vasopressin Receptor Melanocortin Receptor
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ERK JNK KLF MAP3K MAP4K MAPKAPK2 (MK2) MEK Mixed Lineage Kinase MNK p38 MAPK Raf Ribosomal S6 Kinase (RSK)
Membrane Transporter/Ion Channel >
ATP Synthase BCRP Calcium Channel CFTR Chloride Channel CRAC Channel CRM1 EAAT2 GABA Receptor GlyT HCN Channel iGluR Monoamine Transporter Monocarboxylate Transporter Na+/Ca2+ Exchanger Na+/HCO3- Cotransporter Na+/K+ ATPase nAChR NKCC P-glycoprotein P2X Receptor Potassium Channel Proton Pump SGLT Sodium Channel TRP Channel URAT1
Metabolic Enzyme/Protease >
15-PGDH 5 alpha Reductase 5-Lipoxygenase Acetyl-CoA Carboxylase Acyltransferase Adenosine Deaminase Adenosine Kinase Aldehyde Dehydrogenase (ALDH) Aldose Reductase Aminopeptidase Angiotensin-converting Enzyme (ACE) ATGL ATP Citrate Lyase Carbonic Anhydrase Carboxypeptidase Cathepsin CETP COMT Cytochrome P450 Dipeptidyl Peptidase Dopamine β-hydroxylase E1/E2/E3 Enzyme Elastase Enolase FAAH FABP Factor Xa Farnesyl Transferase Fatty Acid Synthase (FAS) FXR Glucokinase GSNOR Gutathione S-transferase HCV Protease Hexokinase HIF/HIF Prolyl-Hydroxylase HIV Integrase HIV Protease HMG-CoA Reductase (HMGCR) HSP Indoleamine 2,3-Dioxygenase (IDO) Isocitrate Dehydrogenase (IDH) Lactate Dehydrogenase LXR MAGL Mineralocorticoid Receptor Mitochondrial Metabolism MMP Nampt NEDD8-activating Enzyme Neprilysin PAI-1 PDHK PGC-1α Phosphatase Phosphodiesterase (PDE) Phospholipase Procollagen C Proteinase Proteasome Pyruvate Kinase RAR/RXR Renin ROR Ser/Thr Protease SGK Stearoyl-CoA Desaturase (SCD) Thrombin Tryptophan Hydroxylase Tyrosinase Xanthine Oxidase
Neuronal Signaling >
5-HT Receptor AChE Adenosine Kinase Amyloid-β Beta-secretase CaMK CGRP Receptor COMT Dopamine Receptor Dopamine Transporter FAAH GABA Receptor GlyT iGluR Imidazoline Receptor mAChR Melatonin Receptor Monoamine Oxidase nAChR Neurokinin Receptor Opioid Receptor Serotonin Transporter γ-secretase
NF-κB >
NF-κB IKK Keap1-Nrf2 MALT1
PI3K/Akt/mTOR >
Akt AMPK ATM/ATR DNA-PK GSK-3 MELK mTOR PDK-1 PI3K PI4K PIKfyve PTEN
PROTAC >
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Protein Tyrosine Kinase/RTK >
Ack1 ALK Bcr-Abl BMX Kinase Btk c-Fms c-Kit c-Met/HGFR Discoidin Domain Receptor DYRK EGFR Ephrin Receptor FAK FGFR FLT3 IGF-1R Insulin Receptor IRAK Itk PDGFR PKA Pyk2 ROS Src Syk TAM Receptor Trk Receptor VEGFR
Stem Cell/Wnt >
Casein Kinase ERK Gli GSK-3 Hedgehog Hippo (MST) JAK Notch Oct3/4 PKA Porcupine ROCK sFRP-1 Smo STAT TGF-beta/Smad Wnt YAP β-catenin γ-secretase
TGF-beta/Smad >
TGF-beta/Smad PKC ROCK TGF-β Receptor
Vitamin D Related >
VD/VDR
Others >
Androgen Receptor Aromatase Estrogen Receptor/ERR Progesterone Receptor Thyroid Hormone Receptor Others

Proadifen hydrochloride

Proadifen hydrochloride is a Cytochrome P450 inhibitor (IC50 = 19μM). IC50 value: 19μMTarget: P450Proadifen HCl has many biochemical functions, some of which include: inhibitory effects on NOS1 (neuronal nitric oxide synthase; IC50 = 90 mM), adult mouse skeletal muscle AChR (acetyl choline receptor), hepatic drug metabolism via the CYP (cytochrome P450) system, CYP-dependent (cytochrome P450-dependent) arachidonate metabolism (90% at 50 μM), transmembrane calcium influx, and platelet thromboxane synthesis. This compound has also been shown to block KIR6.1 (ATP-sensitive inward rectifier potassium channel 8; IC50 = 4.4 mM) and stimulate endothelial cell prostacyclin production.

  • CAS Number: 62-68-0
  • MF: C23H32ClNO2
  • MW: 389.959
  • Catalog: Cytochrome P450
  • Density: N/A
  • Boiling Point: 460.8ºC at 760 mmHg
  • Melting Point: 122-123ºC
  • Flash Point: 132.3ºC

Fenofibrate

Fenofibrate is a PPARα agonist with an EC50 of 30 μM.

  • CAS Number: 49562-28-9
  • MF: C20H21ClO4
  • MW: 360.831
  • Catalog: Autophagy
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 469.8±35.0 °C at 760 mmHg
  • Melting Point: 80-81ºC
  • Flash Point: 165.4±24.9 °C

CYP4A11/CYP4F2-IN-2

CYP4A11/CYP4F2-IN-2 is a potent and orally active dual inhibitor of cytochrome P450 (CYP) 4A11 and CYP4F2, with IC50s of 140 nM and 40 nM, respectively. CYP4A11/CYP4F2-IN-2 has potential for the research of renal diseases[1].

  • CAS Number: 2126874-77-7
  • MF: C16H20N4O2
  • MW: 300.36
  • Catalog: Cytochrome P450
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Chrysosplenetin

Chrysosplenetin is one of the polymethoxylated flavonoids in Artemisia annua L. (Compositae) and other several Chinese herbs. Chrysosplenetin inhibits P-gp activity and reverses the up-regulated P-gp and MDR1 levels induced by artemisinin (ART). Chrysosplenetin significantly augments the rat plasma level and anti-malarial efficacy of ART, partially due to the uncompetitive inhibition effect of Chrysosplenetin on rat CYP3A[1].

  • CAS Number: 603-56-5
  • MF: C19H18O8
  • MW: 374.341
  • Catalog: P-glycoprotein
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 615.8±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 222.7±25.0 °C

Liarozole

Liarozole (R75251; R85246) is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of retinoic acid (IC50=7 μM), resulting in increased tissue levels of retinoic acid. Liarozole shows antitumoral properties[1][2][3].

  • CAS Number: 115575-11-6
  • MF: C17H13ClN4
  • MW: 308.76500
  • Catalog: Cytochrome P450
  • Density: 1.36g/cm3
  • Boiling Point: 578.2ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 303.5ºC

Olivetol-d7

Olivetol-d7 is the deuterium labeled Olivetol. Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors CB1 and CB2[4]. Olivetol also inhibits CYP2C19 and CY

  • CAS Number: 1175096-29-3
  • MF: C11H9D7O2
  • MW: 187.29
  • Catalog: Cannabinoid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Oxiconazole

Oxiconazole (Ro 13-8996) is a broad spectrum anti-fungal agent which can inhibit the growth of Candida, Aspergillus and Trichophyton. Oxiconazole is also a highly efficacious activator of CYP3A4 transactivation, which could be antagonized by Rifampicin (HY-B0272) in a competitive manner. Oxiconazole exhibits inhibitory effect against colorectal cancer (CRC) via peroxiredoxin-2 (PRDX2)-mediated autophagy arrest[1][2][3].

  • CAS Number: 64211-45-6
  • MF: C18H13Cl4N3O
  • MW: 429.127
  • Catalog: Fungal
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 576.8±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 302.6±32.9 °C

CYP4A11/CYP4F2-IN-1

CYP4A11/CYP4F2-IN-1 is a potent dual inhibitor of cytochrome P450 (CYP) 4A11 and CYP4F2, with IC50s of 19 nM and 17 nM, respectively. CYP4A11/CYP4F2-IN-1 has potential for the research of renal diseases[1].

  • CAS Number: 502654-40-2
  • MF: C15H15N3OS
  • MW: 285.36
  • Catalog: Cytochrome P450
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ratic

Ranitidine is a potent, selective and orally active histamine H2-receptor antagonist with an IC50 of 3.3 μM that inhibits gastric secretion. Ranitidine is a weak inhibitor of CYP2C19 and CYP2C9[1][2].

  • CAS Number: 66357-35-5
  • MF: C13H22N4O3S
  • MW: 314.404
  • Catalog: Bacterial
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 437.1±45.0 °C at 760 mmHg
  • Melting Point: 69-70°C
  • Flash Point: 218.2±28.7 °C

BI 689648

BI 689648 is a novel, highly selective aldosterone synthase inhibitor which can inhibit CYP11B1 and CYP11B2 with IC50s of 310 and 2.1 nM, respectively.

  • CAS Number: 1633009-87-6
  • MF: C16H18N4O2
  • MW: 298.34
  • Catalog: Cytochrome P450
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CYP11B2-IN-1

CYP11B2-IN-1 is a CYP11B2 inhibitor with an IC50 of 2.3 nM. CYP11B2-IN-1 inhibits CYP11B1 with an IC50 of 142 nM[1].

  • CAS Number: 1356479-78-1
  • MF: C18H18FN3O
  • MW: 311.35
  • Catalog: Cytochrome P450
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

6',7'-DIHYDROXYBERGAMOTTIN

6',7'-Dihydroxybergamottin (6′,7′-DHB) is a furanocoumarin that inhibits CYP3A4 and is found in grapefruit juice and Seville orange juice[1].

  • CAS Number: 145414-76-2
  • MF: C21H22O6
  • MW: 370.396
  • Catalog: Cytochrome P450
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 611.3±55.0 °C at 760 mmHg
  • Melting Point: 112-113 °C
  • Flash Point: 323.5±31.5 °C

(+)-Cedrol

Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochrome P-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with Ki of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes[1]. Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, sedative, insecticidal, and anti-fungal activities[2].

  • CAS Number: 77-53-2
  • MF: C15H26O
  • MW: 222.366
  • Catalog: Cytochrome P450
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 277.2±8.0 °C at 760 mmHg
  • Melting Point: 55-59 °C(lit.)
  • Flash Point: 115.5±10.9 °C

Olivetol-d9

Olivetol-d9 is the deuterium labeled Olivetol. Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors CB1 and CB2[3]. Olivetol also inhibits CYP2C19 and CYP2D6 activi

  • CAS Number: 137125-92-9
  • MF: C11H7D9O2
  • MW: 189.29900
  • Catalog: Cannabinoid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BVT 948

BVT948 is a protein tyrosine phosphatase (PTP) inhibitor which can also inhibit several cytochrome P450 (P450) isoforms and lysine methyltransferase SETD8.

  • CAS Number: 39674-97-0
  • MF: C14H11NO3
  • MW: 241.24200
  • Catalog: Histone Methyltransferase
  • Density: 1.39g/cm3
  • Boiling Point: 400.8ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 196.2ºC

4-(5-HYDROXYMETHYLIMIDAZOL-1-YLMETHYL)BENZONITRILE

CYP19A1/CYP11B2-IN-1 (Compound X21) is a potent and selective aromatase and aldosterone synthase dual inhibitor with IC50s of 2.3 nM and 29 nM for aromatase (CYP19A1) and aldosterone synthase (CYP11B2), respectively. CYP19A1/CYP11B2-IN-1 has excellent antiproliferative and pro-apoptotic activity against the cancer cell. CYP19A1/CYP11B2-IN-1 can be used for research of breast cancer[1].

  • CAS Number: 183500-36-9
  • MF: C12H11N3O
  • MW: 213.23500
  • Catalog: Cytochrome P450
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Orteronel

Orteronel is a highly selective inhibitor of human 17,20-lyase with IC50 of 38 nM, and exhibits >1000-fold selectivity over other CYPs such as 11-hydroxylase and CYP3A4.

  • CAS Number: 566939-85-3
  • MF: C18H17N3O2
  • MW: 307.346
  • Catalog: Cytochrome P450
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 685.1±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 368.2±28.7 °C

Acetylshikonin

DL-Acetylshikonin is a non-selective, reversible Cytochrome P450 inhibitor with IC50 values of 1.4-4.0 μM. DL-Acetylshikonin has anti-cancer and anti-inflammatory activities[1].

  • CAS Number: 54984-93-9
  • MF: C18H18O6
  • MW: 330.33200
  • Catalog: Cytochrome P450
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Kushenol M

Kushenol M is a flavonoid from Sophora flavescens. Kushenol M is a cytochrome P450 (CYP) inhibitor, with IC50 values of 1.29 μM for CYP3A4 in in human liver microsomes[1].

  • CAS Number: 101236-51-5
  • MF: C30H36O7
  • MW: 508.603
  • Catalog: Cytochrome P450
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 737.7±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 240.1±26.4 °C

Seneciphylline

Seneciphylline is a toxic pyrrolizidine alkaloid in Senecio plants[1]. Seneciphylline significantly increases the activities of epoxide hydrase and glutathione-S-transferase but causes reduction of cytochrome P-450 and related monooxygenase activities[2].

  • CAS Number: 480-81-9
  • MF: C18H23NO5
  • MW: 333.379
  • Catalog: Cytochrome P450
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 577.7±50.0 °C at 760 mmHg
  • Melting Point: 217ºC
  • Flash Point: 303.2±30.1 °C

BMS-764459

BMS-764459 is a CRF1 antagonist. BMS-764459 can be used for the research of neurological disorders such as depression and anxiety. BMS-764459 is also an atypical CYP1A1 inducer[1][2].

  • CAS Number: 1188407-45-5
  • MF: C19H21F2N5O3
  • MW: 405.39900
  • Catalog: CRFR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Antitumor agent-87

Antitumor agent-87 is a potent antitumor agent. Antitumor agent-87 shows a high affinity for CYP1A1 with a Ki value of 0.23 µM. Antitumor agent-87 shows antiproliferative activity. Antitumor agent-87 induces cell cycle arrest at the G2/M phase. Antitumor agent-87 show antitumoral activity[1].

  • CAS Number: 1422527-88-5
  • MF: C22H28N2O6S
  • MW: 448.53
  • Catalog: Cytochrome P450
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Erysolin

Erysolin is a CYP1A inhibitor with antigenic toxicity. Erysolin reduces benzo(a)pyrene-induced genotoxicity[1].

  • CAS Number: 504-84-7
  • MF: C6H11NO2S2
  • MW: 193.29
  • Catalog: Cytochrome P450
  • Density: 1.19g/cm3
  • Boiling Point: 385.5ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 186.9ºC

quinidine polygalacturonate

Quinidine polygalacturonate is an antiarrhythmic agent. Quinidine polygalacturonate is a potent, orally active, selective cytochrome P450db inhibitor. Quinidine polygalacturonate is also a K+ channel blocker with an IC50 of 19.9 μM, and can induce apoptosis. Quinidine polygalacturonate can be used for malaria research[1][2][3][4].

  • CAS Number: 27555-34-6
  • MF: C26H34N2O9
  • MW: 518.556
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Verapamil-d3-1 hydrochloride

Verapamil-d3-1 (hydrochloride) is the deuterium labeled Verapamil hydrochloride[1]. Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research[2][3][4].

  • CAS Number: 2714485-49-9
  • MF: C27H36D3ClN2O4
  • MW: 494.08
  • Catalog: Calcium Channel
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Peucedanol

Peucedanol is a non-competitive inhibitor of CYP3A4 with a Ki value of 4.07 μM and a competitive inhibitor of CYP1A2 and CYP2D6 with Ki values of 3.39 μM and 6.77 μM, respectively[1].

  • CAS Number: 46992-81-8
  • MF: C14H16O5
  • MW: 264.274
  • Catalog: Cytochrome P450
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 531.6±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 204.8±23.6 °C

(R)-Mephenytoin

(R)-Mephenytoin ((-)-Mephenytoin), the R-enantiomer of Mephenytoin. Mephenytoin is an Anticonvulsant agent[1][2].

  • CAS Number: 71140-51-7
  • MF: C12H14N2O2
  • MW: 218.25200
  • Catalog: Cytochrome P450
  • Density: 1.154g/cm3
  • Boiling Point: N/A
  • Melting Point: 137-138ºC
  • Flash Point: N/A

Antitumor agent-88

Antitumor agent-88 exhibits potent antimitotic activity and arrests cell in the G2/M phase. Antitumor agent-88 disrupts the microtubule and the cytoskeleton in CYP1A1-expressing breast cancer cells. Antitumor agent-88 is also a competitive inhibitor of CYP1A1 (Ki: 1.4 μM)[1].

  • CAS Number: 1422527-87-4
  • MF: C23H30N2O7S
  • MW: 478.56
  • Catalog: Cytochrome P450
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CYP3A4-IN-1

CYP3A4-IN-1 (compound 5a) is a potent cytochrome P450 3A4 (CYP3A4) inhibitor with an IC50 value of 0.085 µM[1].

  • CAS Number: 2771297-34-6
  • MF: C31H37N5O3S
  • MW: 559.72
  • Catalog: Cytochrome P450
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mephenytoin-d3

(Rac)-Mephenytoin-d3 is a labelled racemic Mephenytoin. Mephenytoin, an anticonvulsant, is the CYP2C19 and CYP2B6 substrate[1].

  • CAS Number: 1185101-86-3
  • MF: C12H11D3N2O2
  • MW: 221.27000
  • Catalog: Cytochrome P450
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A