Metabolism

<p>LY 517717 is an orally active inhibitor of coagulation factor Xa with antithrombotic activity for the study of venous thromboembolism (VTE).</p>

<p>AC-261066 is an orally available and isoform-selective agonist of RARβ2 with a pEC50 of 8.0.</p>

<p>Verofylline (Verofyllinum) is an orally available, long-acting, multiacting, methylxanthine-substituted bronchodilator with inhibitory effects on PDE4 for the</p>

<p>Isomazole is a novel orally available phosphodiesterase (PDE) inhibitor with calcium-sensitizing properties that inhibits PDE3 and PDE4.</p>

<p>alphaSYN-IN-NAB2: a NAB2 gene protein guarding neurons against alpha-SYN harm; aids endosomal transport, cell processes, and can study various diseases.</p>

<p>VU0155069, a selective PLD1 inhibitor (IC50: 46 nM), halts cancer cell migration in transwell assays.</p>

<p>CYP1B1-IN-1 is a selective and potent cytochrome P450 1B1 (CYP1B1) inhibitor with potential anticancer and antitumor activity for breast cancer research.</p>

<p>IPN60090: potent oral GLS1 inhibitor, IC50 of 31 nM, potential for anticancer and immunomodulation.</p>

<p>K-111 is a PPAR alpha agonist. K-111 improves insulin resistance, reducing bodyweight, and ameliorating atherogenic dyslipidemia.</p>

<p>Aleplasinin (PAZ 417) is a selective and orally active inhibitor of Plasminogen activator inhibitor-1(PAI-1) and a key negative regulator of the fibrinolytic</p>

<p>4-Hydroxymephenytoin ((+/-)-4'-Hydroxymephenytoin) is the metabolism of an antiepileptic drug mephenytoin. Mephenytoin is used as a CYP2C19 substrate.</p>

<p>Ch55, a potent HL60 cell differentiator (EC50=200nM), binds well to RAR-α/β, useful for cancer research.</p>

<p>Vatanidipine (AE0047) is a novel dihydropyridine (DHP)-type calcium channel blocker with slow-onset pharmacological actions.A slow-onset and long-lasting</p>

<p>Isolithocholic Acid, a bile acid isomer, forms through microbial metabolism of Lithocholic acid or its 3α-sulfate.</p>

<p>Salnacedin (G-201) treats immune, skin, and musculoskeletal issues, suitable for acne, dermatitis, and psoriasis research.</p>

Clozic (ICI 55897) exhibits reversible anti-proliferative effects and can be used in studies about serving as a potential anti-arthritic agent.

<p>CYP1B1-IN-5: selective CYP1B1 inhibitor, IC50 = 4.7 nM, useful for metabolism disease research.</p>

GSK205 is a selective TRPV4 antagonist (IC50: 4.19 μM) for inhibiting TRPV4-mediated Ca2+ influx.

<p>Dirlotapide (CP742033), an intestinal MTP inhibitor, cuts weight in diabetic dogs by lowering food intake and raising peptide YY.</p>

<p>IHVR-17028 is a potent broad-spectrum ERα-glucosidase I (α-glucosidase? I) inhibitor with IC50 of 0.24 μM and antiviral activity.</p>

<p>C75 is an inhibitor synthetic fatty-acid synthase (FASN) and inhibits prostate cancer cells PC3 (IC50: 35 μM).</p>

<p>Phosphatase-IN-1 is a phosphatidic acid phosphatase (Pah) inhibitor with antifungal activity for the study of rice blast and ruderalia.</p>

<p>5(S)-HETrE, made by 5-LO from mead acid, has unknown biological activity and metabolic fate.</p>

<p>(Rac)-Lonafarnib is a racemic FTase inhibitor, effective against H-ras, K-ras, N-ras (IC50: 1.9, 5.2, 2.8 nM), and has anti-HDV properties.</p>

<p>(R)-IDO/TDO-IN-1 (compound 25), an indoleamine-2,3-dioxygenase (IDO) inhibitor, demonstrates good pharmacokinetic properties and exerts anti-tumor effects in the MC38 xenograft model. This compound exhibits synergy when combined with the anti-PD-1 monoclonal antibody (SHR-1210) [1].</p>

<p>Antiviral agent 46, also known as compound 4, is a cannabidiol (CBD) derivative exhibiting anti-SARS-CoV-2 activity (IC50: 1.90 μM) and ACE2 inhibition (IC50: 1.37 μM) [1].</p>

<p>AKB-6899 is an inhibitor of prolyl hydroxylase domain 3 (PHD3) and increases the soluble form of the VEGF receptor (sVEGFR-1) production from GM-CSF-treated</p>

<p>17(S)-HpDHA, primarily produced by the 15-Lipoxygenase (LOX) isoenzymes h15-LOX-1 and h15-LOX-2 from docosahexaenoic acid (DHA), is a key regulator in epoxide synthesis through allosteric modulation. Additionally, it effectively inhibits platelet aggregation, demonstrating an EC50 of approximately 1 μM [1].</p>

<p>PF-04937319 activates glucokinase (EC50=154.4μM) with low hypoglycemia risk, researched for type 2 diabetes treatment.</p>

BAY-7081 is a cyanopyridone-based compound that functions as a potent, selective, and orally active PDE9A inhibitor, demonstrating an inhibition concentration (

<p>"113-O12B is an ionizable cationic lipidoid containing a disulfide bond, utilized in the generation of lipid nanoparticles (LNPs) for mRNA delivery [1]."</p>

<p>ICMT-IN-25 (compound 37) serves as a potent inhibitor of isoprenylcysteine carboxyl methyltransferase (ICMT), exhibiting an IC50 value of 0.025 μM [1].</p>

<p>BMS-986318: potent FXR agonist, EC50=53/350 nM, good ADME, effective in liver disease models, for nonalcoholic steatohepatitis research.</p>

<p>IDH1 Inhibitor 7 is an IDH1 inhibitor with an IC 50 of less than 100 nM .</p>

<p>HIF-2α-IN-13 (18) acts as a HIF-2α inhibitor and exhibits an IC 50 value of 2.7 μM.</p>

<p>JGB-1-155, serving as a positive allosteric modulator (N-PAMs), effectively enhances the activity of nicotinamide phosphoribosyltransferase (NAMPT) with an EC 50 of 3.29 μM. It mitigates oxidative stress by elevating NAD+ levels in THP-1 human monocytes and reduces TNFα-induced reactive oxygen species (ROS) in HT-22 cells [1].</p>

<p>AZD6605 is a potent, reversible inhibitor of, MMP2, MMP9, MMP12 and MMP13.</p>

<p>Yonkenafil, a PDE5 inhibitor, may reduce stroke damage and aid in Alzheimer's treatment.</p>

<p>9(E),11(E)-Conjugated Linoleic Acid (9(E),11(E)-CLA) belongs to a group of eight geometric isomers of linoleic acid, characterized by adjacent double bonds. This specific isomer, 9,11 all-trans linoleic acid, was first discovered in ground beef and is found in various dairy products as well. Notably, it has been shown to decrease mammary tumors in rats with dietary inclusion as minimal as 0.1%. [Matreya, LLC. Catalog No. 1181]</p>

<p>AZD 4017 is an inhibitor of 11β-Hydroxysteroid Dehydrogenase Type 1(11β-HSD1) (IC50: 7 nM).</p>

<p>Diflumidone sodium is a non-steroidal agent with anti-inflammatory activity.</p>

<p>3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid) (Dehydrolithocholic acid) is a bile acid metabolite and inhibits the differentiation of TH17 cells by directly</p>

<p>LMPTP INHIBITOR 1 hydrochloride is a selective inhibitor of low molecular weight protein tyrosine phosphatase ( LMPTP ), with an IC 50 of 0.8 μM for LMPTP-A.</p>

<p>RORγt agonist 3 is a potent agonist of RORγt.</p>

<p>Branched fatty acid esters of hydroxy fatty acids (FAHFAs) are a class of endogenous lipids whose levels are modulated by fasting and high-fat diets and are linked to insulin sensitivity. These compounds typically consist of a C-16 or C-18 fatty acid, such as palmitoleic, palmitic, oleic, or stearic acid, esterified to a hydroxylated C-16 or C-18 lipid. One specific form of FAHFA, known as 9-OAHSA, involves the esterification of oleic acid to 9-hydroxy stearic acid. Within the FAHFA family, OAHSAs notably represent the predominant form found in the serum of glucose-tolerant AG4OX mice, which uniquely overexpress the Glut4 glucose transporter in adipose tissue.</p>

PDE5-IN-42 is a selective inhibitor of second-generation phosphodiesterase type 5 (PDE5).

<p>Gisadenafil (UK-369003) is a selective inhibitor of phosphodiesterase 5 (PDE5) with an IC50 of 3.6 nM and prevents degradation of cGMP.</p>

FTI-2153 inhibits farnesyltransferase with 1.4 nM IC50, >3000x more effective on H-Ras than Rap1A.

<p>N-Methyl Palbociclib is an impurity of the orally active selective CDK4 and CDK6 inhibitor Palbociclib (PD 0332991).</p>

<p>ICMT-IN-9 (compound 47) is a potent ICMT inhibitor with an IC50 value of 0.16 μM [1].</p>