4'-Hydroxy diclofenac D4 is the deuterium labeled 4'-Hydroxy diclofenac. 4'-Hydroxy diclofenac is an orally active metabolite of Diclofenac (HY-15036) by cytochrome P450 2C9 (CYP2C9). 4'-Hydroxy diclofenac has anti-inflammatory and analgesic properties[1][2].
Drotrecogin alfa activated (DrotAA) is recombinant human activated protein C (APC). Drotrecogin alfa activated prevents smoke-induced increases in pulmonary microvascular permeability and proinflammatory cytokine IL-1β in rats. Drotrecogin alfa activated inhibits coagulation and inflammation and promotes fibrinolysis. Drotrecogin alfa activated can be used for severe sepsis reaearch[1][2].
ODN 21158 is a potent G-modified TLR3 andTLR9inhibitor. ODN 21158 shows no cytotoxic. ODN 21158 nhibits IFN-α secretion in a dose dependent manner[1].
Indomethacin (Indometacin) sodium is a potent, orally active COX1/2 inhibitor with IC50 values of 18 nM and 26 nM for COX-1 and COX-2, respectively. Indomethacin sodium has anticancer activity and anti-infective activity. Indomethacin sodium can be used for cancer, inflammation and viral infection research.[1][2][3].
Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon sodium inhibits CCR9-mediated Ca2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon sodium is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 µM for all). Vercirnon sodium is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively[1].
Cimetidine sulfoxide (Cimetidine sulphoxide) is a sulfoxide metabolite of Cimetidine. Cimetidine is a histamine H2-receptor antagonist. Cimetidine has the potential for peptic ulcer disease and upper gastrointestinal haemorrhage treatment[1].
Terreic acid, a quinone epoxide antibiotic, acts as an effective Btk inhibitor. Terreic acid blocks the interaction between PKC and the pleckstrin homology domain of Btk. Terreic acid inhibits the binding of GST-BtkPH to PKC in lysates of HMC-1 human mast cells with an IC50 of approximately 100 μM[1].
ent-16-Kaurene-3b,15b,18-triol is a ent-kaurene diterpene. ent-16-Kaurene-3b,15b,18-triol has significant antiallergic activity on β-hexosaminidase release induced by Polyginseng antigen[1].
WRNA10 is a potent HIV-1 TAR RNA binder with an IC50 of 10 µM and an CC50 of 40 µM[1].
BMY-25271 is a histamine H2 receptor antagonist.
Argininosuccinic acid disodium participates in the fourth step of the urea cycle and is cleaved into arginine and fumarate by argininosuccinate lyase (ASL). Argininosuccinic acid disodium reduces reduced glutathione (GSH) concentrations and increases reactive oxygen species production in the cerebral cortex and striatum. Argininosuccinic acid disodium causes lipid peroxidation and protein oxidation and also induces oxidative stress in the developing rat brain[1][2].
Revdofilimab (ABBV-368) is a human IgG1 agonist monoclonal antibody against OX40. Among them, OX40 is a member of the TNF receptor superfamily expressed on activated and memory T cell subsets and T regulatory cells[1].
Azathioprine (BW 57-322) sodium is an orally active immunosuppressive agent. Azathioprine can be converted in vivo to the active metabolite 6-mercaptopurine (6-MP). Azathioprine has myelosuppressive effects and induces apoptosis[1][3].
(3R,5R)-3,5-Diacetoxy-1-(3,4-dihydroxyphenyl)-7-(4-hydroxyphenyl)heptane, a diarylheptanoid from the rhizomes of Curcuma kwangsiensis, possesses a variety of biological and pharmacological activities including antioxidant, antihepa totoxic, anti-inflammatory, antiproliferative, antiemetic, and antitumor activities[1].
cFMS-IN-2 is a FMS kinase inhibitor with an IC50 of 0.024 μM.
JAK3/BTK-IN-6 (compound 14h) is a potent BTK and JAK3 dual inhibitor, with IC50 values of 0.6 and 0.4 nM, respectively. JAK3/BTK-IN-6 shows good metabolic stability in human liver microsome. JAK3/BTK-IN-6 can be used for hematological and immune diseases research[1].
PNF21 is a new transdermal corticosteroid with anti-inflammatory activity.
L-m-Tyrosine is an unnatural amino acid, that has potential in the research of Parkinsons disease, Alzheimers disease, and arthritis[1].
Cassiaside is a naphthopyrone glucoside, shows mixed-type inhibition against BACE1 (IC50=4.45 μM; Ki=9.85 μM). Cassiaside possesses potential anti- Alzheimer's disease (AD) activity[1].
Etrasimod (APD334) is a potent, selective and orally available antagonist of the sphingosine-1-phosphate-1 (S1P1) receptor with an IC50 value of 1.88 nM in CHO cells.
diABZI STING agonist-1 is a selective stimulator of interferon genes (STING) receptor agonist.
KZR-616 (KZR616) is a potent, selective dual immunoproteasome subunit LMP7/LMP2 inhibitor with IC50 of 39 nM/139 nM, weakly inhibits β5, MECL-1 and no acitivty against β1 subunit; shows no inhibition at 10 uM against a broad selectivity panel of 20 serine, metallo-, cysteine and aspartyl proteases and 11 hydrolases; demonstrates efficacy in the anti-collagen antibody induced arthritis (CAIA) models. Other Indication Phase 2 Clinical
Berberrubine chloride is an active metabolite of berberine, attenuates ulcerative colitis in mice model[1].
GLPG1205 is potent, selective and orally active GPR84 (a G-protein-coupled receptor) antagonist with a favorable PK/PD profile. GLPG1205 has anti-inflammatory activity and is used for the treatment of pulmonary fibrosis[1][2].
Ro 24-4383 is a carbamate-linked dual action antibacterial agent[1].
Cavα2δ1&NET-IN-1 (Compound 59S) is a dual inhibitor of the α2δ‑1 subunit of voltage-gated calcium channels (Cavα2δ-1) and the norepinephrine transporter (NET). Cavα2δ1&NET-IN-1 inhibits Cavα2δ-1 with a Ki of 112 nM. Cavα2δ1&NET-IN-1 inhibits NET with a Ki of 383 nM and IC50 of 67 nM. Cavα2δ1&NET-IN-1 can be used for research of pain[1].
Re 80 is an anti-angiogenic agent and is a synthetic retinoid[1].
Flurbiprofen is a nonsteroidal anti-inflammatory agent (NSAIA) with antipyretic and analgesic activity.Target: PGE synthaseFlurbiprofen, a propionic acid derivative, is a nonsteroidal anti-inflammatory agent (NSAIA) with antipyretic and analgesic activity. Oral formulations of flurbiprofen may be used for the symptomatic treatment of rheumatoid arthritis, osteoarthritis and anklylosing spondylitis. Flurbiprofen may also be used topically prior to ocular surgery to prevent or reduce intraoperative miosis. Flurbiprofen is structurally and pharmacologically related to fenoprofen, ibuprofen, and ketoprofen. Flurbiprofen may have unique pharmacological properties that reduce the accumulation of unfolded proteins and may represent a new class of drug for the fundamental treatment of obesity [1]. Flurbiprofen and its enantiomers selectively lower Aβ42 levels in broken cell γ-secretase assays, indicating that these compounds directly target the γ-secretase complex that generates Aβ from APP. Of the compounds tested, meclofenamic acid, racemic flurbiprofen, and the purified R and S enantiomers of flurbiprofen lowered Aβ42 levels to the greatest extent [2].
IRAK inhibitor 3 is an interleukin-1 (IL-I) receptor-associated kinase (IRAK) kinase modulator extracted from patent WO2008030579 A2.