Metabolism

RPR132595A (NPC) hydrochloride, an active metabolite of CPT-11, is produced via cytochrome P-450 3A4 (CYP3A4) metabolism and is ultimately eliminated via

Enniatin A, a Fusarium toxin, blocks rat liver ACAT with 22 μM IC50.

Quinaprilat: active form of quinapril; treats heart failure, hypertension.

CETP-IN-4 is a cholesteryl ester transfer protein (CETP) inhibitor.

α-Hydroxyphenazolam is a metabolite of Phenazolam.

16(S)-HETE, a CYP450 byproduct of arachidonic acid, halts kidney ATPase by 60% at 2µM when angiotensin II is present.

cis-5-Tetradecenoic acid, found in blood, helps study Long Chain 3-Hydroxyacyl-CoA Dehydrogenase Deficiency.

Etherolenic acid, a divinyl ether oxylipin from linolenic acid via 13-lipoxygenase, turns into 13(S)-HpOTrE, then to divinyl ether.

all-trans-5,6-epoxy Retinoic Acid can be used in related research in the field of life sciences. Its product number is T36382 and CAS number is 13100-69-1.

DOTA-XYIMSR-01 is a molecular probe targeting CAIX, capable of being labeled with 177Lu for the treatment and localization of malignant gliomas. The uptake of [177Lu]Lu-XYIMSR-01 in U87MG tumors is 6.19% injected dose per gram (% ID/g), with a tumor-to-muscle uptake ratio of 20.14. In an orthotopic glioma model, co-administration with temozolomide significantly enhances survival rates and inhibits tumor growth in mice. DOTA-XYIMSR-01 shows potential for research in the field of cancer treatment.

(+)-Geodin, a fungal metabolite, boosts fibrinolysis in BAECs (50-150 μM) and glucose uptake in rat adipocytes (1-100 μg/ml).

PDE1-IN-5 (Compound 10c) is a selective PDE1C inhibitor with an IC50 of 15 nM, exhibiting anti-inflammatory properties through the inhibition of iNOS, TNF-α, IL

Insulin sensitizer C59 is an orally available insulin sensitizer that improves glucose uptake and can be used to study insulin-stimulated GLUT4 translocation.

BtGH84 Activator I is a BtGH84 activator. It is the small molecule activator of a glycoside hydrolase.

DPPE-MPEG(2000) is a polyethylene glycol (PEG) derivative of 1,2-dipalmitoyl-rac-glycero-3-phosphoethanolamine (DPPE), characterized as a PEGylated phospholipid.

Histamine glutarimide is a novel QPCT inhibitor that targets inflammatory processes like eosinophil migration, showing anti-asthmatic effects in animal models.

Mycophenolate Mofetil: Non-competitive, selective inhibitor of IMP dehydrogenase I/II, IC50: 39/27 nM.

α-Glucosidase-IN-79 (Compound 4d9) is a non-competitive α-glucosidase inhibitor with an IC50 of 2.11 μM, demonstrating greater inhibitory potency than the existing α-glucosidase inhibitors Acarbose (IC50 of 327.0 μM) and HXH8r (IC50 of 15.32 μM). It exhibits no cytotoxicity on normal human liver cells (LO2) and shows good metabolic stability in rat plasma. α-Glucosidase-IN-79 holds promise for research in type 2 diabetes.

YM44781: non-peptide antagonist with strong NK1 (pKi=9.09) and NK2 (pKi=9.94) receptor affinity.

8-iso-13,14-dihydro-15-keto Prostaglandin F2α (8-iso-13,14-dihydro-15-keto PGF2α) is a metabolite of the isoprostane, 8-isoprostane (8-iso PGF2α), in rabbits,

α-Amylase-IN-4 (Compd 10y) exhibits the highest level of amylase inhibition, demonstrating an IC50 value of 17.83 ± 0.14 μg/mL [1].

ISM012-042 is an orally active inhibitor of PHD1 and PHD2, with IC50 values of 1.9 and 2.5 nM, respectively. At a concentration of 2.5 μM, ISM012-042 protects Caco-2 cells from DSS-induced barrier damage. Additionally, in LPS-induced bone marrow-derived dendritic cells (BMDC) from mice, ISM012-042 exhibits anti-inflammatory properties by dose-dependently reducing the expression of IL-12 subunit IL-12p35 and TNF. It also restores intestinal barrier function and alleviates intestinal inflammation in various experimental colitis models. ISM012-042 is useful for studying intestinal mucosal repair and immune disorders.

Plipastatin A1, a lipopeptide isolated from B.

hCAII/XII-IN-1 (compound 4l) is a potent inhibitor of hCAXII and hCAII, with Ki values of 8.4 nM and 9.4 nM, respectively. It plays a significant role in cancer research.

CAIX/VEGFR-2-IN-3 (Compound 6i) is an inhibitor of Carbonic Anhydrase IX and VEGFR-2, with IC50 values of 41 and 48 nM, respectively. It exhibits anticancer activity by inhibiting the growth of MCF-7 breast cancer cells (IC50 of 22.33 μM) and mouse fibroblast cell line 3T3, where cell viability is reduced to below 40% at a concentration of 100 μM. This compound is applicable for research in the field of cancer treatment.

hCAI/II-IN-10 (Compound 5d) is an inhibitor of human carbonic anhydrase I and II (hCA I and hCA II), with IC50 values of 4.32 nM and 3.89 nM, respectively.

Lysinoalanine, (S,R)- is a bioactive chemical.

LDHA-IN-8, an inhibitor, inhibits the proliferation of pancreatic and lung cancer cells, decreasing the intracellular lactate content and increasing ROS levels.

1,3-Dipalmitoyl-2-eicosapentaenoyl glycerol reduces mice liver triglycerides.

18-Hydroxycorticosterone is a corticosteroid and corticosterone derivative, which can lead to serious electrolyte imbalances.

ROC-0929 (13a) is a selective sPLA2 inhibitor with IC50 of 80 nM, targeting hGX and blocking ERK1/2, p-38 phosphorylation for inflammation research.

DSPE-PEG1000-APRPG is a PEG compound composed of DSPE and the APRPG peptide. It is applicable for drug delivery.

Compound 13, an AChE activator 1, is a non-pyridinium oxime that reactivates paraoxon-inhibited acetylcholinesterase (AChE) [1].

Impurity C of Calcitriol is an impurity of Calcitriol.Impurity C of Calcitriol is used in the synthesis of vitamin D3.

RXP 407 selectively inhibits ACE N-domain, preserving acetyl-Ser-Asp-Lys-Pro and not affecting angiotensin I in vivo.

NF-κB/HIF-1α-IN-1 (compound 9c) effectively inhibits the NF-κB activation pathway and demonstrates selective antifibrotic activity. This compound exhibits no significant cytotoxicity in NCI tumor cell lines. In rat models, NF-κB/HIF-1α-IN-1 successfully ameliorates liver fibrosis, suppresses the expression levels of NF-κB and HIF-1α, and induces Nrf2.

Hexaglutamate folate, a natural folic acid form, requires deconjugation for absorption; its deficiency can lead to anemia and numerous chronic diseases.

CalB-10X, also known as Candida antarctica lipase B (CALB), functions as a catalyst for polymer synthesis.

Neotheaflavin, from black tea, inhibits pancreatic lipase.

Pepsin A is a protease and endopeptidase in the stomach, capable of breaking down proteins in food into small peptide fragments.

ICDH, an enzyme in the citric acid cycle, converts isocitrate to α-ketoglutarate and reduces NAD(P)+, vital for metabolism.

16,16-dimethyl PGA2, a stable analog of PGA2, greatly reduces Sendai virus growth and helps mice survive influenza and cancer.

Obeversen is a DGAT-2 synthesis reducer [1] .

Seco Rapamycin, a ring-opened Rapamycin derivative, does not affect mTOR function.

FPPS-IN-2 (compound 4a) is an effective orally active HFPPS inhibitor with an IC50 value of 1.108 µM, showing potential for use in osteoporosis research.

5-Methoxyresorcinol (Flamenol) is a chemical intermediate.