Gout

Probenecid is a potent and selective agonist of transient receptor potential vanilloid 2 (TRPV2) channels. Probenecid also inhibits pannexin 1 channels.

Dapansutrile is a potent, orally active and selective NLRP3 inflammasome inhibitor. Dapansutrile has anti-inflammatory activity and decreases immune factor levels. Dapansutrile can be used for research of inflammatory diseases.

Lithospermic acid ((+)-Lithospermic acid) is a plant-derived polycyclic phenolic carboxylic acid isolated from Salvia miltiorrhiza, and has the anti-oxidative and hepatoprotective activity on carbon tetrachloride (CCl₄)-induced acute liver damage in vitro and in vivo.

Adrenocorticotropic hormone (ACTH; Adrenocorticotrophic hormone) is a polypeptide tropic hormone produced by the anterior pituitary gland. Adrenocorticotropic hormone stimulates cortisol secretion from the adrenal cortex via the hypothalamic-pituitary-adrenal (HPA) axis. Adrenocorticotropic hormone regulates cortisol and androgen production. Adrenocorticotropic hormone can promote the development of spermatogenesis. Adrenocorticotropic hormone can relieve acute inflammation in gout models by inhibiting the polarization of macrophages to M1 type, inhibiting ROS and proinflammatory factor production and protecting mitochondrial function. Adrenocorticotropic hormone can be used for the researches of inflammation, endocrinology, metabolic disease, such as gout and nephrotic syndrome.

PP121 is a multi-targeted kinase inhibitor with IC₅₀s of 10, 60, 12, 14, 2 nM for mTOR, DNK-PK, VEGFR2, Src, PDGFR, respectively.

NLRP3-IN-99 is an orally active NLRP3 inflammasome inhibitor, IC₅₀ = 0.019 μM. NLRP3-IN-99 binds to the NLRP3 NACHT domain with a human K_d value of 6.9 nM, blocking inflammasome assembly and activation. NLRP3-IN-99 blocks ASC oligomerization and the assembly of NLRP3 with ASC and NEK7, inhibiting NLRP3-driven IL‑1β secretion. NLRP3-IN-99 can be used for research on NLRP3-related diseases, such as gout.

GPR84 antagonist 9 is an orally active GPR84 antagonist with an IC₅₀ value of 12 nM. By antagonizing the GPR84 receptor, GPR84 antagonist 9 blocks immune cell migration, M1 polarization, and the release of inflammatory factors (IL1β/TNFα) induced by medium-chain free fatty acids (MCFFAs) and other substances, thereby comprehensively inhibiting inflammatory and fibrotic responses. GPR84 antagonist 9 can be used in the research of inflammation-driven pain disorders, including neuropathic pain disorders, Fabry disease, gout, and bladder pain syndrome.

Z1456467176 is an allosteric inhibitor of P2X7R. Z1456467176 binds to P2X7R, prevents ATP-induced channel opening and receptor activation, and blocks ATP-induced activation of the NLRP3-caspase-1-IL-1β pathway. Z1456467176 inhibits ATP-induced P2X7R pore formation in macrophages, as well as IL-1β secretion induced by ATP or BzATP. Z1456467176 alleviates gouty joint inflammation in rats. Z1456467176 can be used for the research of gouty arthritis.

Uricase, Microorganism (Uox, Microorganism) is a uricase (urate oxidase) derived from Microorganism. Uricase, Microorganism converts uric acid into allantoin. The absence of Uricase in mammals causes kidney diseases resulting from uric acid accumulation. Uricase, Microorganism can be used for research on chronic refractory gout and hyperuricemia.

Adrenocorticotropic hormone (ACTH; Adrenocorticotrophic hormone) TFA is a polypeptide tropic hormone produced by the anterior pituitary gland. Adrenocorticotropic hormone TFA stimulates cortisol secretion from the adrenal cortex via the hypothalamic-pituitary-adrenal (HPA) axis. Adrenocorticotropic hormone TFA regulates cortisol and androgen production. Adrenocorticotropic hormone TFA can promote the development of spermatogenesis. Adrenocorticotropic hormone TFA can relieve acute inflammation in gout models by inhibiting the polarization of macrophages to M1 type, inhibiting ROS and proinflammatory factor production and protecting mitochondrial function. Adrenocorticotropic hormone TFA can be used for the researches of inflammation, endocrinology, metabolic disease, such as gout and nephrotic syndrome.

Phellodendrine chloride is an orally active plant alkaloid. Phellodendrine chloride inhibits the proliferation of KRAS-mutated pancreatic cancer cells by suppressing macropinocytosis and glutamine metabolism, inducing ROS accumulation and mitochondrial apoptosis. Phellodendrine chloride promotes autophagy by activating the AMPK/mTOR pathway, alleviating intestinal damage in ulcerative colitis. Phellodendrine chloride can alleviate gouty arthritis by inhibiting the IL-6/STAT3 signaling pathway. Phellodendrine chloride suppresses allergic reactions by altering the conformation of MRGPRB3/MRGPRX2 protein, thereby inhibiting the activation of PKC and subsequent downstream MAPK and NF-κB signaling. Phellodendrine chloride inhibits the AKT/NF-κB pathway and down-regulates the expression of COX-2, thereby protecting zebrafish embryos from oxidative stress. Phellodendrine chloride has an anti-major depressive disorder (MDD) effect by down-regulating CHRM1, HTR1A, and the PI3K/Akt signaling pathway.

Ulodesine (BCX4208) is a purine nucleoside phosphorylase (PNP) inhibitor, with an IC₅₀ of 2.293 nM against human PNP, and low nanomolar IC₅₀ values against mouse, rat and monkey PNP. Ulodesine blocks the production of uric acid precursors, reduces serum uric acid levels, clears accumulated uric acid in the blood, and elevates the levels of purine nucleosides including guanosine. Ulodesine reduces the counts of total lymphocytes, T lymphocytes and lymphocyte subsets, inhibits the proliferation of cancer cells and activated lymphocytes, and enhances vaccine immune responses. Ulodesine can be used in research related to hyperuricemia and gout.

Allopurinol sodium is a potent and orally active xanthine oxidase inhibitor with an IC₅₀ value of 0.2-50 μM. Allopurinol sodium can be used in the research of hyperuricemia and gout. Allopurinol sodium decreases the expression of HIF-1α and HIF-2α protein. Allopurinol sodium shows anti-depressant and anti-nociception activity. Anti-leishmanial effect.

Antrafenine (Stakane) is a derivative of 2-(quinolin-4-ylamino) benzoate, and is an orally active anti-inflammatory and analgesic agent. Antrafenine protects mammalian epithelial cells from cell death upon exposure to influenza A virus A/WSN/33 (H1N1). Antrafenine inhibits carrageenan-induced paw swelling in rats, and reduces exudate volume and total leukocyte infiltration in carrageenan- and calcium pyrophosphate dihydrate crystal-induced pleurisy in rats. Antrafenine can be used in studies related to influenza and pseudogout.

Uricase (Recombinant) (Uox (Recombinant)) is a uricase (urate oxidase). Uricase (Recombinant) converts uric acid into allantoin. The deficiency of Uricase in mammals causes kidney diseases resulting from uric acid accumulation. Uricase (Recombinant) can be used for research on chronic refractory gout and hyperuricemia.

Strictinin is an orally active phenolic compound. Strictinin reduces xanthine oxidase activity, uric acid production, and the activation of ERK1/2, JNK, NF-κB, and NLRP3 inflammasome components in hepatocytes treated with Xanthine (HY-W017389). Strictinin decreases elevated serum uric acid levels and enhanced xanthine oxidase activity in mice treated with potassium oxonate. Strictinin acts as a ROR1 inhibitor and exhibits anticancer activity against highly aggressive non-androgen-dependent prostate cancer. Strictinin induces cancer cell apoptosis (apoptosis), arrests cell cycle, and inhibits cancer cell migration, invasion, and epithelial-mesenchymal transition. Strictinin modulates gut microbiota, inhibits bacterial growth and biofilm formation, accelerates small intestinal transit, and blocks viral entry and replication. Strictinin can be used in research related to hyperuricemia, androgen receptor-negative non-androgen-dependent prostate cancer, triple-negative breast cancer, bacterial infections, constipation, coronavirus infections, dental caries, and infections caused by influenza A, influenza B, and human parainfluenza virus type 1.

Xininurad is a potent orally active URAT1 inhibitor with an IC₅₀ of 7.17 nM. Xininurad inhibits URAT1 activity to reduce serum uric acid levels and increase urinary uric acid excretion. Xininurad can be used for the research of hyperuricemia and gout.

Uricase, candida utilis (Uox, candida utilis) is a uricase (urate oxidase) derived from Candida utilis. Uricase, candida utilis converts uric acid into allantoin. The absence of Uricase in mammals causes kidney diseases resulting from uric acid accumulation. Uricase, candida utilis can be used for research on chronic refractory gout and hyperuricemia.

7DG (7-Desacetoxy-6,7-dehydrogedunin) is a PKR inhibitor, P2X7 purinergic receptor inhibitor, and skin-lightening agent. 7DG binds outside the ATP-catalytic domain of PKR, blocks the kinase activity-independent protein-protein interactions of PKR, inhibits the phosphorylation and activity of PKR, disrupts ASC assembly and caspase-1 activation, and suppresses the activation of the NLRP1 inflammasome. 7DG inhibits pyroptosis, suppresses the ATP-P2X7 signaling pathway, and abolishes ATP-induced increases in the expression levels of MITF, tyrosinase, PMEL/gp100, and melanin content. 7DG exerts skin-lightening effects in cultured skin in vitro. 7DG can be used in research related to chronic obstructive pulmonary disease, gout, type 2 diabetes, Alzheimer's disease, and hyperpigmentary skin disorders.

Benziodarone is a potent inhibitor of S-arylglutathione transferase enzyme system. Benziodarone catalyzes BSP conjugation with GSH. Benziodarone inhibits biliary excretion of synthetic BSP-GSH conjugates.