5072 Results for "

Metabolites

" in MedChemExpress (MCE) Product Catalog:

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179

Clozapine N-oxide

179 Publications Verification

Cat. No.: HY-17366

CAS No.: 34233-69-7

Target:

Drug Metabolite mAChR Dopamine Receptor

Research Areas:

Neurological Disease

Clozapine N-oxide is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide can't cross the blood-brain barrier . Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC₅₀=11 nM) agonist .

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179

Clozapine N-oxide dihydrochloride

179 Publications Verification

Cat. No.: HY-17366A

CAS No.: 2250025-93-3

Target:

mAChR Dopamine Receptor Drug Metabolite

Research Areas:

Neurological Disease

Clozapine N-oxide dihydrochloride is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide dihydrochloride activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide dihydrochloride cannot cross the blood-brain barrier . Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC₅₀=11 nM) agonist .

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156

Retinoic acid

156 Cited Publications

Cat. No.: HY-14649

CAS No.: 302-79-4

Purity: 99.81%

Synonyms: Vitamin A acid; all-trans-Retinoic acid; ATRA

Category:

Ketones, Aldehydes, Acids Whitening Agent Cosmetic Research Endogenous metabolite Disease Research Fields Cancer

Target:

Organoid RAR/RXR PPAR Endogenous Metabolite Autophagy

Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC₅₀s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with K_d of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha.

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154

Erlotinib Hydrochloride

154 Cited Publications

Cat. No.: HY-12008

CAS No.: 183319-69-9

Purity: 99.94%

Synonyms: CP-358774 hydrochloride; NSC 718781 hydrochloride; OSI-774 hydrochloride

Target:

EGFR OAT ERK GSK-3 β-catenin

Research Areas:

Endocrinology Cancer

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 .

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154

Erlotinib

154 Cited Publications

Cat. No.: HY-50896

CAS No.: 183321-74-6

Synonyms: CP-358774; NSC 718781; OSI-774

Target:

EGFR OAT ERK GSK-3 β-catenin

Research Areas:

Endocrinology Cancer

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 .

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103

4-Octyl itaconate

103 Cited Publications

Cat. No.: HY-112675

CAS No.: 3133-16-2

Purity: 99.92%

Synonyms: 4-OI

Target:

Keap1-Nrf2

Research Areas:

Inflammation/Immunology

4-Octyl Itaconate is a cell-permeable Itaconate derivative. Itaconate is an anti-inflammatory metabolite that activates Nrf2 via alkylation of KEAP1 .

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Deschloroclozapine

94 Cited Publications

Cat. No.: HY-42110

CAS No.: 1977-07-7

Target:

mAChR

Research Areas:

Neurological Disease

Deschloroclozapine, a metabolite of Clozapine, is a highly potent muscarinic DREADDs agonist, with blood-brain barrier permeability. Deschloroclozapine binds to DREADD receptor subtypes hM3Dq and hM4Di with K_i of 6.3 and 4.2 nM, respectively. [ ¹¹C]-Deschloroclozapine is developed as a promising PET tracer for DREADD imaging .

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Deschloroclozapine dihydrochloride

94 Cited Publications

Cat. No.: HY-42110A

Target:

mAChR

Research Areas:

Neurological Disease

Deschloroclozapine dihydrochloride, a metabolite of Clozapine, is a highly potent muscarinic DREADDs agonist, with blood-brain barrier permeability. Deschloroclozapine dihydrochloride binds to DREADD receptor subtypes hM3Dq and hM4Di with K_i of 6.3 and 4.2 nM, respectively. [ ¹¹C]-Deschloroclozapine dihydrochloride is developed as a promising PET tracer for DREADD imaging .

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