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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
212 Results for "
microsomal
" in MedChemExpress (MCE) Product Catalog:
Products (212)
212 Results for "microsomal" in MCE Product Catalog:
Cat. No.: HY-118506
CAS No.: 612046-20-5
Target:
Research Areas:
BRP-7 is a 5-lipoxygenase activating protein (FLAP) inhibitor with an IC50 of 0.31 μM. BRP-7 inhibits the co-localization of 5-lipoxygenase (5-LOX) and FLAP by targeting FLAP, thereby blocking the transfer of arachidonic acid (AA) to 5-LOX and suppressing the production of leukotrienes (LTs) (IC₅₀ = 0.15 μM). BRP-7 does not inhibit cyclooxygenase (COX-1/COX-2) or microsomal prostaglandin E₂ synthase-1 (mPGES-1), and does not affect cell viability or AA release. BRP-7 exhibits significant anti-inflammatory effects in rat pleurisy and mouse peritonitis models. BRP-7 can be used for the study of inflammatory diseases .
Synonyms: ISC-27864; GRC-27864
Target:
Research Areas:
Zaloglanstat (ISC-27864; GRC-27864) is a selective, orally active microsomal mPGES-1 inhibitor. Zaloglanstat has an IC50 of 5 nM for human mPGES-1 without significant inhibitory effect on COX-1/2 (IC50 >10 μM). Zaloglanstat blocks the conversion of arachidonic acid metabolite prostaglandin PGH2 to prostaglandin PGE2, thereby inhibiting inflammation-related PGE2 overproduction and reducing inflammatory responses and pain. Zaloglanstat inhibits IL-1β-induced PGE2 release in A549 cells and human synovial fibroblasts in vitro. Zaloglanstat inhibits PGE2 release in pig and dog whole blood with IC50s of 161 nM and 154 nM, respectively. Zaloglanstat can be used in the study of asthma, osteoarthritis, and neurodegenerative diseases .
Cat. No.: HY-156208
CAS No.: 574738-16-2
Synonyms: AdaGalCer(d18:1/2:0); Admantanyl galactosylceramide (d18:1/2:0); Admantanyl galCer(d18:1/2:0)
Research Areas:
C2 Adamantanyl galactosylceramide (AdaGalCer) (d18:1/2:0) is a bioactive sphingolipid. C2 Adamantanyl galactosylceramide (d18:1/2:0) stimulates glucocerebrosidase activity in vitro. C2 Adamantanyl galactosylceramide (d18:1/2:0) inhibits microsomal LacCer and Gb3 synthase, and inhibits cell sulfatide synthesis. C2 Adamantanyl galactosylceramide (d18:1/2:0) reduces glucosylceramide (GlcCer) levels in normal and lysosomal storage disease (LSD) cells. C2 Adamantanyl galactosylceramide (d18:1/2:0) acts as a substrate for A4GALT and is able to lower Gb3 levels with an IC50 concentration of 40 μM in fabry disease cells .
Cat. No.: HY-175207
CAS No.: 3109469-27-1
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CHI3L1-IN-3 is a CHI3L1 inhibitor. CHI3L1-IN-3 binds to CHI3L1 with Kds of 13.76 μM and 13.5 μM in MST and SPR assays, respectively. CHI3L1-IN-3 demonstrates extended plasma half-lives and microsomal stability, along with reduced intrinsic clearance. CHI3L1-IN-3 induces dose-dependent cytotoxicity, reduces spheroid mass and inhibits migration in a 3D multicellular glioblastoma (GBM) spheroid model. CHI3L1-IN-3 can be used for the study of GBM .
Cat. No.: HY-182355
CAS No.: 3125953-23-0
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MTHFD2-IN-7 is an orally active, selective MTHFD2 inhibitor with IC50 values of 0.038 μM and 7.44 μM against human hMTHFD1 and hMTHFD2, respectively. MTHFD2-IN-7 exerts its function by binding to the substrate-binding site of MTHFD2 and maintaining interactions with NAD+. Verified by TSA and DARTS assays, MTHFD2-IN-7 not only binds effectively to the target protein, but also possesses Caco-2 permeability and liver microsomal metabolic stability. MTHFD2-IN-7 exhibits favorable pharmacokinetic properties in mice. MTHFD2-IN-7 also significantly inhibits cancer cell proliferation and reduces tumor volume, and serves as a promising small-molecule tool for acute myeloid leukemia research .
Research Areas:
Doxylamine succinate (Standard) is the analytical standard of Doxylamine succinate (HY-A0069). This product is intended for research and analytical applications. 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 .
Cat. No.: HY-A0069S
CAS No.: 1216840-94-6
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(3β)-3-(Acetyloxy)pregna-5,16-dien-20-one 20-oxime is a human 17α-hydroxylase/C17,20-lyase (P45017α) inhibitor with a human IC50 of 67 nM and a rat IC50 of 2754 nM. (3β)-3-(Acetyloxy)pregna-5,16-dien-20-one 20-oxime blocks the human testicular microsomal enzyme mediating androgen biosynthesis steps. (3β)-3-(Acetyloxy)pregna-5,16-dien-20-one 20-oxime does not inhibit human 5α-reductase in prostatic microsomes .
Cat. No.: HY-182356
CAS No.: 3125953-25-2
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MTHFD1/2-IN-1 is an orally active dual MTHFD1/MTHFD2 inhibitor, with IC50 values of 0.26 μM and 0.031 μM against human MTHFD1 and MTHFD2, respectively. MTHFD1/2-IN-1 blocks one-carbon metabolism by inhibiting the dehydrogenase activity of MTHFD1 as well as the dehydrogenase and cyclohydrolase activities of MTHFD2, thereby disrupting nucleotide biosynthesis and redox homeostasis in cancer cells. MTHFD1/2-IN-1 exhibits favorable Caco-2 permeability and hepatic microsomal metabolic stability. MTHFD1/2-IN-1 shows significant anti-leukemic activity, which not only reduces the viability of various leukemia cells but also inhibits tumor growth of acute myeloid leukemia (AML) in mouse models .
Cat. No.: HY-128795
CAS No.: 2095304-61-1
Research Areas:
KH176m is the major active metabolite of KH176 (HY-121577). KH176m is a microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor that can cross the blood-brain barrier, with an IC50 of 0.16 µM against mouse mPGES-1 and 1.51 µM against human mPGES-1. KH176m blocks LPS- or IL-1β-induced PGE2 production, scavenges ROS, inhibits lipid peroxidation, accelerates NADPH consumption, suppresses the growth of prostate cancer spheroids, reduces the CD44 + CD24 − prostate cancer stem cell population, and protects fibroblasts with oxidative phosphorylation defects from redox stress-induced death. KH176m can be used in research related to mitochondrial diseases, inflammatory pain, inflammatory neurological diseases, inflammatory cancers, and prostate cancer .
Cat. No.: HY-P81245
Synonyms: Cytochrome P450 1A2; cytochrome P450, family 1, subfamily a, polypeptide 2; Cytochrome P450 family 1 polypeptide 2; Cytochrome P450 subfamily I aromatic compound inducible polypeptide 2; Cyp1a2; CYPD45; P-450d; RATCYPD45; CP12; CP 12; P3-450; Aryl hydrocarbon hydroxylase; Dioxin inducable P3 45; Flavoprotein linked monooxygenase; microsomal monooxygenase; P450 4; P450 form 4; P450 P3; P450(PA); Xenobiotic monooxygenase; P450 1A2.
Cat. No.: HY-P705910
Purity: ≥ 90%, as determined by reducing SDS-PAGE .
Synonyms: CYP3A5; Flavoprotein-Linked Monooxygenase; Cytochrome P450 Family 3 Subfamily A Member 5; Aryl Hydrocarbon Hydroxylase; P450PCN3; Alternative Protein CYP3A5; CP35; microsomal Monooxygenase; PCN3; Xenobiotic Monooxygenase; Cytochrome P450, Subfamily IIIA (Niphedipine Oxidase), Polypeptide 5; Unspecific Monooxygenase; Cytochrome P450, Family 3, Subfamily A, Polypeptide 5; Cytochrome P450 HLp2; Cytochrome P450-PCN3; Cytochrome P450 3A; Cytochrome P450 3A5; Cytochrome P-450; CYPIIIA5; DKFZp686I18188; Uncharacterized Protein DKFZp686I18188
Species:
Human
Source:
E. coli
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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
