66 Results for "

P450 substrate

" in MedChemExpress (MCE) Product Catalog:
Products (66)

66 Results for "P450 substrate" in MCE Product Catalog:

5
5 Cited Publications
Cat. No.: HY-13463
CAS No.: 570406-98-3
Purity:  99.83%
Synonyms: AKR-501; E5501; YM477
Research Areas:  

Inflammation/Immunology Cancer

Avatrombopag (AKR-501) is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag mimics the biological activities of TPO. Avatrombopag increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A .
loading...
    loading...
5
5 Cited Publications
Cat. No.: HY-13463A
CAS No.: 677007-74-8
Purity:  99.88%
Synonyms: AKR-501 maleate; E5501 maleate; YM477 maleate
Avatrombopag (AKR-501) maleate is an orally active, non-peptide thrombopoietin receptor (TPO receptor) agonist (EC50: 3.3 nM). Avatrombopag maleate mimics the biological activity of TPO. Avatrombopag maleate increases platelet production by activating intracellular signaling systems and promotes the production of platelets and megakaryocytes from hematopoietic precursor cells. Avatrombopag maleate is a substrate for cytochrome P450 (CYP) 2C9 and CYP3A .
loading...
    loading...
5
5 Cited Publications
Cat. No.: HY-13463B
CAS No.: 570403-17-7
Purity:  97.05%
Synonyms: AKR-501 hydrochloride; E5501 hydrochloride; YM477 hydrochloride
Research Areas:  

Cardiovascular Disease Cancer

Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag hydrochloride mimics the biological activities of TPO. Avatrombopag hydrochloride increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag hydrochloride is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A .
loading...
    loading...
2
2 Cited Publications
Cat. No.: HY-N2574
CAS No.: 511-96-6
Gitogenin is a natural steroid isolated from the whole plant of Tribulus longipetalus. Gitogenin is a selective inhibitor of UDP-glucuronosyltransferase 1A4 (UGT1A4) and enzyme α-glucosidase with IC50 values of 0.69 μM (use trifluoperazine as a substrate) and 37.2 μM, respectively, and does not inhibit the activities of major human cytochrome P450 isoforms .
loading...
    loading...
2
2 Cited Publications
Cat. No.: HY-N0419
CAS No.: 491-50-9
Synonyms: Quercetin-7-O-β-D-glucopyranoside
Quercimeritrin (Quercetin-7-O-β-D-glucopyranoside) is an orally active α-glucosidase inhibitor (with an IC50 of 79.88 μM against the Saccharomyces cerevisiae enzyme) and a P-gp substrate, with anti-angiogenic and antioxidant activities. Quercimeritrin does not cross the blood-brain barrier and does not inhibit cytochrome P450 enzymes. Quercimeritrin precisely binds to and inhibits the active sites of c-Kit, MMP-2, Aurora-A kinases and α-glucosidase, thereby disrupting target functions. Quercimeritrin effectively regulates postprandial blood glucose and also exhibits significant anti-angiogenic activity, which inhibits endothelial cell proliferation and microvascular growth. Quercimeritrin can be used in the research of diabetes and breast cancer .
loading...
    loading...
1
1 Cited Publications
Cat. No.: HY-D0145
CAS No.: 5725-91-7
Synonyms: Resorufin ethyl ether
7-Ethoxyresorufin (Resorufin ethyl ether) is a fluorometric substrate and competitive inhibitor of cytochrome P450, especially CYP1A1. 7-Ethoxyresorufin also inhibits NO synthase .
loading...
    loading...
1
1 Cited Publications
Cat. No.: HY-D0055
CAS No.: 117620-77-6
3-Cyano-7-ethoxycoumarin is a fluorescent cytochrome P-450 substrate that generates a blue fluorescent product upon enzymatic cleavage. 3-Cyano-7-ethoxycoumarin is used to detect the activity of mixed-function oxidases in isolated rat hepatocytes. 3-Cyano-7-ethoxycoumarin serves as a biological dye and indicator for research .
loading...
    loading...
1
1 Cited Publications
Cat. No.: HY-125904
CAS No.: 66592-72-1
Purity:  95.11%
4-Hydroxyretinoic acid (4-HRA) is a derivative of Retinoic acid (HY-14649). 4-Hydroxyretinoic acid is formed via the catalysis of retinol by cytochrome P-450 isoenzymes. 4-Hydroxyretinoic acid also serves as a substrate for UDP-glucuronosyltransferase (s) and recombinant UGT2B7. 4-Hydroxyretinoic acid binds to the nuclear receptor RAR (Retinoic Acid Receptor), activates RAR and RXR-alpha, subsequently regulates gene expression and cell differentiation, and induces cancer cell apoptosis (Apoptosis). 4-Hydroxyretinoic acid also participates in multiple physiological processes such as immunoregulation, neuroprotection and antioxidation .
loading...
    loading...
1
1 Cited Publications
Cat. No.: HY-17570
CAS No.: 382-67-2
Desoximetasone is a corticosteroid and a substrate of cytochrome P450 3A4. Desoximetasone has anti-inflammatory, anti-allergic, and immunosuppressive effects. Desoximetasone can be used in the research of various skin diseases, such as skin allergies, atopic dermatitis, and psoriasis .
loading...
    loading...
Cat. No.: HY-B1184A
CAS No.: 70989-04-7
Synonyms: (+)-Mephenytoin
Target:  

Cytochrome P450

Research Areas:  

Neurological Disease

(S)-Mephenytoin ((+)-Mephenytoin) is an anticonvulsive agent. (S)-Mephenytoin is a substrate of the cytochrome P450 (CYP) isoform CYP2C19. (S)-Mephenytoin can be used for the analysis of cytochrome P450 metabolism .
loading...
    loading...
Cat. No.: HY-A0024
CAS No.: 124937-51-5
Synonyms: (R)-(+)-Tolterodine; (+)-Tolterodine; (R)-Tolterodine; PNU-200583
Target:  

mAChR Cytochrome P450

Research Areas:  

Neurological Disease Cancer

Tolterodine ((R)-(+)-Tolterodine) is a mAChR inhibitor and substrate for cytochrome P450 enzymes. Tolterodine competitively binds acetylcholine, reduces sympathetic excitation, and inhibits involuntary bladder muscle contraction. Tolterodine restores the Nrf2/NF-κB signaling pathway, mediates protection against inflammatory response and ferroptosis. Tolterodine ameliorates LPS (HY-D1056)-induced reactive oxygen species production and lipid oxidation. Tolterodine can be used for the research of urinary tract infections and overactive bladder .
loading...
    loading...
Cat. No.: HY-90010
CAS No.: 124937-52-6
Synonyms: Kabi-2234; PNU-200583E
Target:  

mAChR Cytochrome P450

Research Areas:  

Neurological Disease Cancer

Tolterodine tartrate (Kabi-2234) is a mAChR inhibitor and substrate for cytochrome P450 enzymes. Tolterodine tartrate competitively binds acetylcholine, reduces sympathetic excitation, and inhibits involuntary bladder muscle contraction. Tolterodine tartrate restores the Nrf2/NF-κB signaling pathway, mediates protection against inflammatory response and ferroptosis. Tolterodine tartrate ameliorates LPS (HY-D1056)-induced reactive oxygen species production and lipid oxidation. Tolterodine tartrate can be used for the research of urinary tract infections and overactive bladder .
loading...
    loading...
Cat. No.: HY-N7136
CAS No.: 80-26-2
α-Terpinyl acetate is a monoterpene ester isolated from Laurus nobilis L. essential oil. α-Terpinyl acetate is a competitive P450 2B6 substrate which binding to the active site of P450 2B6 with a Kd value of 5.4 μM .
loading...
    loading...
Cat. No.: HY-133091
CAS No.: 31005-02-4
Purity:  99.84%
Synonyms: 7-O-Ethylumbelliferone
7-Ethoxycoumarin is a substrate of cytochrome P450 (CYP450). 7-Ethoxycoumarin has been used for the functional characterization of various CYPs and for the generation of 7-hydroxycoumarin (HY-N0573) .
loading...
    loading...
Cat. No.: HY-A0069
CAS No.: 562-10-7
Doxylamine succinate is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine succinate is orally active, possessing analgesic and hypnotic activities. Doxylamine succinate enhances the activities of CYP2B, CYP2A, CYP3A and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine succinate decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine succinate induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine succinate can be used for the research of nausea, allergy, insomnia .
loading...
    loading...
Cat. No.: HY-N5132
CAS No.: 7787-20-4
(-)-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 .
loading...
    loading...
Cat. No.: HY-132184
CAS No.: 87173-80-6
Purity:  ≥99.0%
Synonyms: 5,6-EET; (±)5,6-EpETrE
Research Areas:  

Endocrinology

5,6-Epoxyeicosatrienoic acid (5,6-EET; (±)5,6-EpETrE) is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5,6-Epoxyeicosatrienoic acid degrades into 5,6-DiHET and 5,6-δ-lactone, which can be converted to 5,6-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5,6-Epoxyeicosatrienoic acid has been implicated in the mobilization of calcium and hormone secretion. 5,6-Epoxyeicosatrienoic acid is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhibits isoforms Cav3.1, Cav3.2 (IC50=0.54 μM), and Cav3. and decreases nifedipine-resistant phenylephrine-induced vasoconstriction in isolated mouse mesenteric arteries via Cav3.2 blockade when used at a concentration of 3 μM. In addition, it is a substrate of COX-1 and COX-2.
loading...
    loading...
Cat. No.: HY-D0149
CAS No.: 575-03-1
4-(Trifluoromethyl)umbelliferone is fluorescent probe substrate for rat hepatic cytochrome P450 enzymes .
loading...
    loading...
Cat. No.: HY-116862
CAS No.: 97744-44-0
Purity:  99.54%
Synonyms: DBF
Dibenzylfluorescein (DBF) is a fluorogenic probe (Fluoresecent dye) that acts as a substrate for specific cytochrome P450 (CYP) isoforms, including CYP3A4, CYP2C8, CYP2C9, CYP2C19, and aromatase (CYP19). Dibenzylfluorescein is typically used near its Km value of 0.87-1.9 μM (Ex=485 nm,Em=535 nm). Dibenzylfluorescein is used to detect changes in CYP catalytic activity caused by drugs or disease .
loading...
    loading...
Cat. No.: HY-W014018
CAS No.: 92-71-7
Synonyms: PPO; DPO; POP
2,5-Diphenyloxazole (PPO; DPO; POP) is a fluorescent dye, as well as a substrate and metabolite precursor of cytochrome P-450 (cytochrome P-448/P1-450). 2,5-Diphenyloxazole serves as a scintillator .
loading...
    loading...