IL-17 modulator 5 (compound 26) is a IL-17 inhibitor, with an IC50 of 1 nM[1].
Pseudocoptisine acetate, a quaternary alkaloid with a benzylisoquinoline skeleton, is isolated from the tubers of Corydalis turtschaninovii. Pseudocoptisine acetate shows anti-inflammatory properties[1].
Quercetin-3-glucoside is a naturally occurring polyphenol that has antioxidant, anti-proliferative, and anti-inflammatory properties.Quercetin-3-glucoside alleviates ethanol-induced hepatotoxicity, oxidative stress, and inflammatory responses via the Nrf2/ARE antioxidant signaling pathway[1].Quercetin-3-glucoside regulates the expression of nitric oxide synthase 2 (NO2) via modulating the nuclear factor-κB (NF-κB) transcription regulation system. Quercetin-3-glucoside has high bioavailability and low toxicity, is a promising candidate agent to prevent birth defects in diabetic pregnancies[2].
Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range[1][2][3].
α-Viniferin is an anti-inflammatory compound from Caragana chamlagu root[1].
Artemisinic acid (Qing Hao acid), an amorphane sesquiterpene isolated from Artemisia annua L., possesses a variety of pharmacological activity, such as antimalarial activity, anti-tumor activity, antipyretic effect, antibacterial activity, allelopathy effect and anti-adipogenesis effect[1].
RORγt/DHODH-IN-2 (compound 1) is a potent dual RORγt/DHODH inhibitor. RORγt/DHODH-IN-2 can be used for inflammatory bowel disease (IBD) research[1].
Tyrphostin AG 1433 is a specific and potent inhibitor of PDGFR-β and of KDR/Flk-1. Tyrphostin AG 1433 acts as an angiogenesis inhibitor[1].
GDC-0834 Racemate is the racemate form of GDC-0834, which is a potent and selective BTK inhibitor with in vitro IC50s of 5.9 and 6.4 nM in biochemical and cellular assays, respectively.IC50 value: 5.9 nM/6.4 nM(biochemical/cellular assay) [1]Target: BTKin vitro: GDC-0834 inhibited BTK with an in vitro IC(50) of 5.9 and 6.4 nM in biochemical and cellular assays, respectively, and in vivo IC(50) of 1.1 and 5.6 μM in mouse and rat, respectively [1].in vivo: Administration of GDC-0834 (30-100 mg/kg) in a rat collagen-induced arthritis (CIA) model resulted in a dose-dependent decrease of ankle swelling and reduction of morphologic pathology [1]. GDC-0834 exhibited low clearance in PXB chimeric mice with humanized liver. Uncertainty in human pharmacokinetic prediction and high interest in a BTK inhibitor for clinical evaluation prompted an investigational new drug strategy, in which GDC-0834 was rapidly advanced to a single-dose human clinical trial. GDC-0834 plasma concentrations in humans were below the limit of quantitation (<1 ng/ml) in most samples from the cohorts dosed orally at 35 and 105 mg [2].
Toosendanin, a triterpenoid extracted from the bark of fruit of Melia toosendan Sieb et Zucc, possesses analgesic, insecticidal and anti-inflammatory activities[1].
TATP hapten is a hapten made from acetone, hydrogen peroxide, and 7-oxo octanoic acid. TATP hapten coupled with bovine serum albumin can raise an immune response against TATP. TATP hapten can coupled directly to BSA and HRP via N-hydroxysuccinimide chemistry to produce haptenated proteins[1].
Cletoquine-d4 is deuterium labeled Cletoquine. Cletoquine (Desethylhydroxychloroquine) is a major active metabolite of Hydroxychloroquine. Cletoquine is produced in the liver by CYP2D6, CYP3A4, CYP3A5, and CYP2C8 isoenzymes. Cletoquine is also a Chloroquine derivative and has the ability to against the chikungunya virus (CHIKV). Cletoquine has antimalarial effects and has the potential for autoimmune diseases treatment[1][2].
Icariside E4 is an antinociceptive agent, and can be isolated from Tabebuia roseo-alba. Icariside E4 has peripheral analgesic activity by ATP-sensitive K+ channel-dependent mechanisms. Icariside E4 also has anti-oxidant, anti-Alzheimer and anti-inflammatory effects[1][2].
Tepilamide fumarate (XP-23829) is an oral fumaric acid ester, acts as a prodrug of monomethyl fumarate, and is used in the research of moderate to severe chronic plaque psoriasis[1].
Methyl α-D-mannopyranoside could target macrophages in anti-tuberculosis inhalation therapy[1].
Ammonium glycyrrhizinate is a triterpenoid saponin, acting as a direct HMGB1 antagonist, with anti-inflammatory， anti-tumor, anti-diabetic activities[1][2][3].
3'-Sialyllactose (3'-SL) is a prebiotic, maintains immune homeostasis and exerts anti-inflammatory and anti-arthritic effects. 3'-Sialyllactose can be used for the research of inflammation[1][2].
Isoscutellarein 8-O-β-D-glucuronide is a flavonoid antioxidant, can be isolated from Theobroma grandiflorum seeds[1][2].
10-Nitrolinoleic acid is a potent peroxisome proliferator-activated receptor γ (PPARγ) agonist. 10-Nitrolinoleic acid competes with [3H]Rosiglitazone for binding to PPAR-γ, with an IC50 of 0.22 μM[1].
AHK is a bioactive peptide with antioxidant effect and has been reported used as a cosmetic ingredient[1].
Resolvin D3 (RvD3) is a docosahexaenoic acid (DHA) derived mediator. Resolvin D3 is dysregulated in arthritis and reduces arthritic inflammation[1][2].
Caplacizumab (Cablivi) is a humanized anti-von Willebrand factor (vWF) nanobody. Caplacizumab inhibits the vWF-mediated platelet adhesion and prevents further microthrombi formation. Caplacizumab can be used for the research of thrombotic thrombocytopenic purpura (TTP)[1].
Benzoyloxypaeoniflorin, isolated from the root of Paeonia suffruticosa, is a tyrosinase inhibitor against mushroom tyrosinase with IC50 of 0.453 mM. Benzoyloxypaeoniflorin is NF-κB Inhibitor and contributes to improving blood circulation through its inhibitory effect on both platelet aggregation and blood coagulation[1][2][3].
(E/Z)-Teriflunomide ((E/Z)-A77 1726) is the active metabolite of Leflunomide (HY-B0083). Leflunomide is an immunomodulatory agent that may exert effects by inhibiting the mitochondrial enzyme dihydroorotate dehydrogenase (DHODH). Leflunomide can be used for the research of rheumatoid arthritis (RA)[1].
Isomagnolone is isolated from Illicium burmanicum and has anti-inflammatory activity[1].
Serelaxin (RLX-030), a recombinant form of human gene-2 relaxin targeting the RLN receptor, is a vasoactive peptide hormone with an antifibrotic activity[1][2][3].
Pterosin B, a indanone found in bracken fern (Pteridium aquilinum), is an inhibitor of salt-inducible kinase 3 (Sik3) signaling. Pterosin B prevents chondrocyte hypertrophy and osteoarthritis in mice by inhibiting Sik3[1][2].
MRT67307 dihydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively[1]. MRT67307 dihydrochloride also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 dihydrochloride also blocks autophagy in cells[2].
T-kinin (Ile-Ser-bradykinin) is a peptide containing bradykinin. T-kinin can be used for the research of inflammation[1][2].