Scientific Reviews
Product Guides
Blogs
Topics
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
94 Results for "
CYP3A
" in MedChemExpress (MCE) Product Catalog:
Products (94)
94 Results for "CYP3A" in MCE Product Catalog:
143
143 Publications Verification
Cat. No.: HY-50896
CAS No.: 183321-74-6
Synonyms: CP-358774; NSC 718781; OSI-774
Erlotinib (CP-358774) is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib also acts as a substrate and inhibitor of OATP2B1, with an IC50 of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, fibronectin, α-SMA, collagen deposition, and renal injury markers. Erlotinib is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, pancreatic cancer, renal fibrosis, and other conditions [3] .
143
143 Publications Verification
Synonyms: CP-358774 hydrochloride; NSC 718781 hydrochloride; OSI-774 hydrochloride
Erlotinib (CP-358774) Hydrochloride is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib Hydrochloride also acts as a substrate and inhibitor of OATP2B1, with an IC50 of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib Hydrochloride blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib Hydrochloride inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, as well as the deposition of fibronectin, α-SMA, collagen and renal injury markers. Erlotinib Hydrochloride is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib Hydrochloride can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, EGFR inhibitor resistance and renal fibrosis [3] .
13
13 Cited Publications
Cat. No.: HY-N0693
CAS No.: 61281-38-7
Synonyms: Schizandrin-A; Wuweizisu-A; Deoxyschizandrin
Category:
Lignans Phenylpropanoids Plants Schisandraceae Disease Research Fields Schisandra chinensis (Turcz.) Baill. Cancer
Target:
12
Target:
Cobicistat is a potent and selective inhibitor of cytochrome P450 3A (CYP3A) enzymes with IC50s of 30-285 nM. Cobicistat is a pharmacokinetic enhancer which increases the overall absorption of several HIV medications.
5
5 Cited Publications
Synonyms: AKR-501; E5501; YM477
Target:
Research Areas:
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 [3].
5
5 Cited Publications
Synonyms: AKR-501 maleate; E5501 maleate; YM477 maleate
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
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 [3].
5
5 Cited Publications
Synonyms: AKR-501 hydrochloride; E5501 hydrochloride; YM477 hydrochloride
Target:
Research Areas:
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 [3].
3
2
2 Cited Publications
Cat. No.: HY-N0692
CAS No.: 58546-54-6
Synonyms: Gomisin-A; TJN-101; Wuweizi alcohol-B
1
1 Cited Publications
Cat. No.: HY-P74210
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: CYP3A4; CYPIIIA3; Prev. CYP3A3; Cytochrome P450, Subfamily IIIA (Niphedipine Oxidase), Polypeptide 3; Cytochrome P450, Subfamily IIIA (Niphedipine Oxidase), Polypeptide 4; Taurochenodeoxycholate 6-Alpha-Hydroxylase; Cytochrome P450, Family 3, Subfamily A,
Target:
Research Areas:
Troleandomycin (Triacetyloleandomycin), a macrolide acrolide antibiotic, is a selective CYP3A inhibitor. Troleandomycin is an oral corticosteroid for asthma study [3].
Cat. No.: HY-B0696A
CAS No.: 145821-59-6
Synonyms: NO050328 hydrochloride; NO328 hydrochloride; TGB hydrochloride
Target:
Research Areas:
Tiagabine hydrochloride (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine hydrochloride exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine hydrochloride is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease [3] .
Cat. No.: HY-B0696
CAS No.: 115103-54-3
Synonyms: NO050328; NO328; TGB
Target:
Research Areas:
Tiagabine (NO050328; NO328; TGB) is an orally active, highly selective, and reversible GAT-1 inhibitor and anticonvulsant that crosses the blood-brain barrier. By blocking the reuptake of GABA in neurons and glial cells, tiagabine increases extracellular GABA levels to enhance inhibitory signal transduction, thereby exerting multiple activities such as anticonvulsant, neuroprotective, and antioxidant effects. Tiagabine exhibits linear pharmacokinetic properties. Although it is metabolized by CYP3A and has a high protein binding rate, it carries a low risk of cognitive impairment. Tiagabine is widely used in research on related diseases including epilepsy (including refractory partial seizures), alcohol withdrawal symptoms, and Huntington's disease [3] .
Cat. No.: HY-50896R
CAS No.: 183321-74-6
Synonyms: CP-358774 (Standard); NSC 718781 (Standard); OSI-774 (Standard)
Research Areas:
Erlotinib Standard (CP-358774 Standard) is the analytical standard of Erlotinib (HY-50896). This product is intended for research and analytical applications. Erlotinib (CP-358774) is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib also acts as a substrate and inhibitor of OATP2B1, with an IC50 of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, as well as the deposition of fibronectin, α-SMA, collagen and renal injury markers. Erlotinib is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, EGFR inhibitor resistance and renal fibrosis [3] .
Target:
Research Areas:
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 [3].
Category:
Human Gut Microbiota Metabolites Natural Products Microorganisms Endogenous metabolite Disease Research Fields Cancer
Target:
Cat. No.: HY-W019847
CAS No.: 76530-44-4
Target:
Research Areas:
Azamulin is an irreversible, highly selective inhibitior of human CYP3Aa. Azamulin has CYP3A inhibition activity with IC50 values range from 0.03-0.24 μM. Azamulin can be used for the research of metabolism and antiinfection .
Cat. No.: HY-113482
CAS No.: 80434-32-8
Synonyms: 1β-OH-DCA
Target:
Cat. No.: HY-W040468
CAS No.: 92321-29-4
Target:
Research Areas:
2-Phenyl-2-(1-piperidinyl)propane is a selective and reversible human CYP2B6 inhibitor with an IC50 of 5.1 μM and a Ki of 5.6. 2-Phenyl-2-(1-piperidinyl)propane inhibits CYP2D6 (IC50=74 μM), CYP3A (IC50=200 μM) .
Cat. No.: HY-W013058
CAS No.: 84852-53-9
Synonyms: DBDPE; 1,2-Bis(perbromophenyl)ethane
Target:
Research Areas:
Decabromodiphenyl ethane (DBDPE) is a brominated flame retardant. Decabromodiphenyl ethane induces ROS-related cytotoxicity and apoptosis in human hepatoma cells, causes hepatocyte damage through oxidative stress, endoplasmic reticulum stress and decreased CYP3A expression, and accumulates and undergoes biotransformation in animal tissues. Decabromodiphenyl ethane can be used to study the environmental toxicology and biological effects of brominated flame retardants [3] .
-
-
Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
