Bleomycin A5 (Pingyangmycin) is an orally active glycopeptide antibiotics. Bleomycin A5 has a role as an antineoplastic agent, an Apoptosis inducer and a bacterial metabolite[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].
WRNA10 is a potent HIV-1 TAR RNA binder with an IC50 of 10 µM and an CC50 of 40 µM[1].
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].
diABZI STING agonist-1 is a selective stimulator of interferon genes (STING) receptor agonist.
Berberrubine chloride is an active metabolite of berberine, attenuates ulcerative colitis in mice model[1].
TLR7 agonist 16 (compound 16d) is a highly potent TLR7 agonist with an EC50 of 18 nM. TLR7 agonist 16 potently induces the activation of mouse macrophages and hPBMCs at low-nanomolar concentrations[1].
Bromfenac (sodium hydrate) is a nonsteroidal anti-inflammatory drug (NSAID), which has anti-inflammatory activity(1) Bromfenac (sodium hydrate) (1 mg/kg, i.v.) is metabolited into an unusual conjugate, bromfenac N-glucoside, in rats bile(2) Bromfenac (sodium hydrate) permeation was found to be 1.62-fold higher through ChS-CS-NPs
IMMH001, also called SYL930, is an orally active, potent and selective S1P1 (sphingosine-1-phosphate receptor 1) agonist. IMMH001 decreased levels of both chemokines and proinflammatory cytokines, including IL-1β, IL-5, IL-18, IP10, CCL3, and CCL5. IMMH001 can be used for rheumatoid arthritis (RA) research[1][2].
Amaroswerin is a bioactive secoiridoid glucoside from Swertia mussotii. Amaroswerin has anti-inflammatory, antidiabetic, antiviral, anticholinergic and immunomodulatory activities. Amaroswerin inhibits NO release with an IC50 value of 5.42 μg/mL in RAW264.7 cells[1].
BLXA-4 is used potentially to treat gingival diseases.
Ki-20227 is a highly selective c-Fms tyrosine kinase(CSF1R) inhibitor with IC50 value of 2 nM; 6 fold and > 100 fold selectivity over VEGFR2(IC50=12 nM) and c-Kit/PDGFRβ(IC50=451/217 nM), respectively.IC50 value: Target: CSF1Rin vitro: Ki20227 did not inhibit other kinases tested, such as fms-like tyrosine kinase-3, epidermal growth factor receptor, or c-Src (c-src proto-oncogene product). Ki20227 was also found to inhibit the M-CSF-dependent growth of M-NFS-60 cells but not the M-CSF-independent growth of A375 human melanoma cells in vitro [1]. Ki20227 inhibited M-CSF-dependent reactions, such as lipopolysaccharide-induced tumor necrosis factor-alpha production, which were enhanced by M-CSF in vitro [2]. in vivo: Ki20227 decreased the number of tartrate-resistant acid phosphatase-positive osteoclast-like cells on bone surfaces in ovariectomized (ovx) rats [1]. In addition, the number of CD11b(+), Gr-1(+), and Ly-6G(+) cells in the spleen decreased in the Ki20227-treated mice, and the CII-induced cytokine production in splenocytes isolated from the Ki20227-treated arthritic mice was also reduced [2]. Ki20227 treatments inhibited the turn-over/expansion of myeloid cells provoked by the immunization and subsequent MOG-specific T cell responses in our EAE animal model [3].
L-Lysine-13C6,d9,15N2 dihydrochloride is the deuterium, 13C-, and 15-labeled L-Lysine hydrochloride. L-lysine hydrochloride is an essential amino acid for humans with various benefits including treating herpes, increasing calcium absorption, reducing diabetes-related illnesses and improving gut health.
7-Hydroxyflavone is a flavonoid isolated from M. indica, with anti-inflammatory activity. 7-Hydroxyflavone protects renal cells from nicotine (NIC)-associated cytotoxicity via the ERK/Nrf2/HO-1 pathway[1][2].
Ebrotidine(FI 3542) is a competitive H2-receptor antagonist (Ki= 127.5 nM) with a potent antisecretory activity and evidenced gastroprotection.IC50 Value: 127.5 nM (Ki)[1]; 0.21mg/kg (ED50, histamine- stimulated acid secretion) [2]Target: H2 receptorin vitro: Ebrotidine displaced 3H-thiotidine specific binding to histamine H2-receptors (Ki: 127.5 nmol/l), showing a higher affinity (p < 0.05) than ranitidine (Ki: 190.0 nmol/l) and cimetidine (Ki: 246.1 nmol/l) [1]. in vivo: Following intravenous administration to rats, ebrotidine inhibited histamine- and pentagastrin-stimulated acid secretion in a dose-dependent manner, ED50 being 0.21 and 0.44 mg/kg, respectively [2]. The mean number of gastric erosions seen at endoscopy after treatment with ebrotidine plus ASA (2.0 +/- 0.3) was significantly lower than that after placebo plus ASA (3.7 +/- 0.2). This reduction in lesion core by ebrotidine was accompanied by a significant increase in gastric blood flow (by 15% in corpus and 26% in antrum), by a rise in transmucosal potential difference (by 12%), and by a decrease of mucosal microbleeding [3]. Results of macroscopic assessment revealed that ebrotidine at doses of 50mg and higher/kg body weight effectively prevented mucosal injury, and that the maximal protective effect was achieved by 1h. Physicochemical analysis established that ebrotidine evoked 30% increase in mucus gel dimension, and showed 20% increase in phospholipids, and the content of sulfo- (18%) and sialomucins (21%) [4].
Dipterocarpol is a dammarane-type triterpenoid. Dipterocarpol is substrate of the bacterial steroid-hydroxylase CYP106A2[1].
Etalocib (LY293111), an orally active leukotriene B4 receptor antagonist, inhibits the binding of [3H]LTB4, with a Ki of 25 nM. Etalocib (LY293111) prevents LTB4-induced calcium mobilization with an lC50 of 20 nM. Etalocib (LY293111) induces apoptosis[1][2][3].
PLP(139-151) is a fragment of myelin proteolipid protein, induce experimental autoimmune encephalomyelitis (EAE).
Danshenol A, an abietane-type diterpenoid, is an aldose reductase (AR) inhibitor with an IC50 of 0.1 μM. Danshenol A can protect endothelial cells from oxidative stress by directly scavenging ROS. Danshenol A has anti-inflammatory and antitumor properties. Danshenol A can be used for atherosclerosis research[1][2][3][4].
Abrilumab is a fully human monoclonal antibody directed against α4β7. Abrilumab selectively binds the α4β7 integrin heterodimer. Abrilumab can be used for the research of inflammatory bowel disease (IBD)[1].
4,6-Dichloroguaiacol induces biochemical and morphological changes in human peripheral blood lymphocytes in vitro[1].
Eprazinone dihydrochloride is a gent with mucolytic, secretolytic, antitussive, and bronchial antispasmodic properties. Eprazinone dihydrochloride is a neurokinin 1 receptor (NK1R) ligand. Eprazinone dihydrochloride has the potential for chronic bronchitis treatment that improved pulmonary function and arterial partial pressure of oxygen[1][2].
Phenidone, an orally active dual inhibitor of cyclooxygenase (COX) and lipoxygenase (LOX), ameliorates rat paralysis in experimental autoimmune encephalomyelitis. Phenidone is a potent hypotensive agent in the spontaneously hypertensive rat[1][2]. Phenidone is used as a photographic developer[3].
CLP-3094 is a potent BF3 (binding function 3)-directed inhibitor of the androgen receptor (AR). CLP-3094 inhibits AR transcriptional activity (IC50=4 μM)[1]. CLP-3094 is a selective, potent GPR142 antagonist[2].
Polyinosinic-polycytidylic acid sodium (Poly(I:C) sodium) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid sodium can directly trigger cancer cells to undergo apoptosis[1][2].
Cortistatin-14, a neuropeptide have structural similarity to somatostatin-14, binds and exerts its function via the somatostatin receptors (sst1-sst5). Cortistatin-14 shows anticonvulsive, neuroprotective effect and remarkable anti-inflammatory properties[1][2][3][4].
Palmitoyl serinol-d5 is the deuterium labeled Palmitoyl serinol[1]. Palmitoyl serinol (N-Palmitoyl serinol) is an analog of the endocannabinoid N-palmitoyl ethanolamine (PEA). Palmitoyl serinol improves the epidermal permeability barrier in both normal and inflamed skin[2][3].
4-Phenyl-7,8-dihydroxycoumarin is a coumarin derivative and can be used for bronchiectasiss research[1].