5 hydroxy 6 methoxy (s) duloxetine

5-hydroxy-6-methoxy (S)-Duloxetine is a metabolite of (S)-duloxetine . It is formed from (S)-duloxetine via a 5- or 6-hydroxy duloxetine intermediate, which is formed by the cytochrome P450 (CYP) isoforms CYP1A2 and CYP2D6, and a catechol duloxetine intermediate. 5-hydroxy-6-methoxy (S)-Duloxetine binds to the serotonin (5-HT), norepinephrine, and dopamine transporters with Ki values of 266, 920, and 2,814 nM, respectively.

(S)-5-hydroxy-6-methoxy Duloxetine, an active metabolite of the (S)-duloxetine, functions as a serotonin (5-HT) and norepinephrine reuptake inhibitor. Its formation occurs through the cytochrome P450 (CYP) isoforms CYP1A2 and CYP2D6 via a 5- or 6-hydroxy duloxetine intermediate, followed by a catechol duloxetine intermediate. This compound effectively inhibits the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT) across lipid membranes, with inhibition constants (Kis) of 266, 920, and 2,814 nM, respectively, for human transporters.

Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6 15 2 3 3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.

Rutin (Quercetin 3-O-rutinoside), a flavonoid, has a variety of biological activities including antiallergic, anti-inflammatory, antiproliferative, and anticarcinogenic properties.

Acetylcysteine (NAC) is an N-acetyl derivative of cysteine, a ROS inhibitor and mucolytic agent. Acetylcysteine induces apoptosis, can be used to reduce mucus thickness, and has anti-influenza viral activity.

Corticosterone (Kendall's compound B) is an adrenocortical steroid with salocorticoid and glucocorticoid activity that is orally active. Corticosterone is involved in the regulation of energy, immune responses, and stress responses in the body.

Resveratrol (SRT 501) is a polyphenolic natural product, a plant antitoxin with antioxidant and chemopreventive activities. Resveratrol has a wide range of targets including COX, SIRT, LOC, etc. Resveratrol induces autophagy and apoptosis.

Kainic acid is an excitatory amino acid receptor agonist (EC50=16.2 μM). Kainic acid is an effective excitatory toxic agent. Kainic acid induces epileptic seizures.

Empagliflozin (BI 10773) is an SGLT-2 inhibitor (IC50=3.1 nM) that is potent and selective, with more than 300-fold selectivity for SGLT-1 4 5 6. Empagliflozin is used for the treatment of type 2 diabetes.

3-Methyladenine (3-MA) is a PI3K inhibitor that selectively inhibits class IB PI3Kγ (IC50 = 60 μM) and class III VPS34 (IC50 = 25 μM). 3-Methyladenine inhibits autophagy.

LDN193189 (LDN-193189) (DM 3189) is a selective BMP signaling inhibitor, inhibiting the transcriptional activity of ALK2 and ALK3 (IC50s: 0.8 0.8 5.3 16.7 nM for ALK1 2 3 6).

Citronellol ((±)-β-Citronellol) is used in insect repellents and perfumes and as a mite attractant.

Balsalazide sodium hydrate (Balsalazide disodium) is an anti-inflammatory compound used in the treatment of Inflammatory Bowel Disease.Balsalazide sodium hydrate is a new 5-aminosalicylic acid (5-ASA) containing prodrug. High dose Balsalazide sodium hydrate(3.0 g twice daily) was superior in maintaining remission in patients with ulcerative colitis compared with a low dose (1.5 g twice daily) or a standard dose of mesalazine (0.5 g three times daily). All three treatments were safe and well tolerated [1]. Balsalazide sodium hydrate is approved for the treatment of mild-to-moderate active UC. It is efficacious for the induction of remission in mild to moderate UC and has a favorable safety profile, with the added advantages of greater efficacy of remission induction and rapidity of onset [2].

Prostaglandin E2 (PGE2) is a natural hormone-like substance involved in various physiological functions, including the contraction and relaxation of smooth muscles, dilation and constriction of blood vessels, regulation of blood pressure, and modulation of inflammation. It can be used to induce neuropathic pain models.

Marimastat (BB2516) (BB-2516) is a potent, broad spectrum matrix metalloprotease (MMP) inhibitor. MMP-9 (IC50=3 nM), MMP-1 (IC50=5 nM), MMP-2 (IC50=6 nM), MMP-14 (IC50=9 nM)and MMP-7 (IC50=13 nM).

Salvianolic acid A (Dan Phenolic Acid A) is a natural product and an inhibitor of matrix metalloproteinase 9 (MMP-9). Salvianolic acid A has antioxidant and anti-inflammatory activity and protects the blood-brain barrier.

Phorbol 12-myristate 13-acetate (PMA) is a natural phorbol ester that acts as an activator of PKC, SphK, and NF-κB, and is commonly used to induce differentiation of THP-1 cells and establish dermatitis models.

5HT6-ligand-1 is an orally active ligand of 5-HT6 receptor (Ki = 1.43 nM).

5-A-RU (5-Amino-6-(D-ribitylamino)uracil) is an early intermediate in riboflavin biosynthesis and is found in a variety of bacteria and yeast as well as plants. 5-A-RU is also a mucosal-associated invariant T (MAIT) cell activator that forms potent MAIT-activating antigens through non-enzymatic reactions with small molecules from other metabolic pathways.

5-A-RU hydrochloride (5-Amino-6-(D-ribitylamino)uracil hydrochloride) is an intermediate of bacterial riboflavin that activates mucosal-associated invariant T cells (MAIT).5-A-RU is used in the study of breast and prostate cancer.

6-Methyl-5-azacytidine is a potent DNMT (DNA methyltransferase) inhibitor.

ACY-957 (HDAC Inhibitor C001) is an orally active and selective inhibitor of HDAC1 and HDAC2 (IC50s: 7 nM, 18 nM, and 1300 nM against HDAC1 2 3) and shows no inhibition on HDAC4 5 6 7 8 9.

Asperphenamate is a fungal metabolite of Aspergillus flatiipes. The IC50s for T47D cells, MDA-MB-231 cells, and HL-60 cells are 92.3 μM, 96.5 μM, and 97.9 μM. Asperphenamate shows an anticancer effect.

JHU395 is an orally-bioavailable prodrug of a lipophilic glutamine antagonist (GA), 6-diazo-5-oxo-L-norleucine (DON). It demonstrates delivery of DON to malignant peripheral nerve sheath tumor (MPNST) both in vitro and in vivo, resulting in significant antitumor activity in MPNST. Additionally, JHU395 exhibits plasma stability.