Nefazodone hydrochloride is an antidepressant drug.
ABT-546 (A-216546) is a potent, highly selective and active endothelin ETA receptor antagonist with a Ki of 0.46 nM for [125I]endothelin-1 binding to cloned human endothelin ETA. ABT-546 is ＞25,000-fold more selective for the ETA receptor than for the ETB receptor. ABT-546 blocks endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis with IC50 of 0.59 nM and 3 nM, respectively[1].
MK-6892 is a potent, selective, and full agonist for the high affinity nicotinic acid (NA) receptor GPR109A. Ki and GTPγS EC50 of MK-6892 on the Human GPR109A is 4 nM and 16 nM, respectively.
DNDS disodium is a potent erythrocyte sedimentation inhibitor[1].
Tesirine intermediate-1 is the intermediate of Tesirine (HY-128952). Tesirine (SG3249), a pyrrole benzodiazepine (PBD) dimer, is a DNA small channel crosslinker with strong cytotoxicity. Tesirine can be used to synthesize Antibody-Drug Conjugates (ADCs), the warhead component of the payload is SG3199 (HY-101161), which has strong anticancer cell activity.
Rupatadine (UR-12592) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 uM(rabbit platelet membranes/guinea pig cerebellum membranes).IC50 value:Target: PAF/H1 antagonistin vitro: Rupatadine competitively inhibited histamine-induced guinea pig ileum contraction (pA2 = 9.29 +/- 0.06) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4). It also competitively inhibited PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2 = 6.68 +/- 0.08) and in human platelet-rich plasma (HPRP) (IC50 = 0.68 microM), while not affecting ADP- or arachidonic acid-induced platelet aggregation [1]. The IC50 for rupatadine in A23187, concanavalin A and anti-IgE induced histamine release was 0.7+/-0.4 microM, 3.2+/-0.7 microM and 1.5+/-0.4 microM, respectively whereas for loratadine the IC50 was 2.1+/-0.9 microM, 4.0+/-1.3 M and 1.7+/-0.5 microM. SR-27417A exhibited no inhibitory effect [2].in vivo: Rupatadine blocked histamine- and PAF-induced effects in vivo, such as hypotension in rats (ID50 = 1.4 and 0.44 mg/kg i.v., respectively) and bronchoconstriction in guinea pigs (ID50 = 113 and 9.6 micrograms/kg i.v.). Moreover, it potently inhibited PAF-induced mortality in mice (ID50 = 0.31 and 3.0 mg/kg i.v. and p.o., respectively) and endotoxin-induced mortality in mice and rats (ID50 = 1.6 and 0.66 mg/kg i.v.) [1]. rupatadine treatment improved the declined lung function and significantly decreased animal death. Moreover, rupatadine was able not only to attenuate silica-induced silicosis but also to produce a superior therapeutic efficacy compared to pirfenidone, histamine H1 antagonist loratadine, or PAF antagonist CV-3988 [3].
3-Methylcytidine, a urinary nucleoside, can be used as a biomarker of four different types of cancer: lung cancer, gastric cancer, colon cancer, and breast cancer[1].
Cedeodarin is a taxifolin that can be isolated from Cedms deodara[1].
TT-10 (YAP-TEAD activator TT-10) is a small molecule activator that activates pro-proliferative YES-associated protein (YAP) and transcriptional enhancer factor domain (TEAD) activities in cardiomyocytes; promoted cardiomyocyte proliferation and simultaneously exerted antioxidant and antiapoptotic effects in vitro via nuclear translocation of YAP, activates YAP-TEADs activity and the Wnt/β-Catenin signaling pathway; ameliorates cardiac dysfunction, decreases ROS and DNA aamage and apoptosis after myocardial infarction (MI) in mice.
R-Phycoerythrin is a phycobiliproteins could be isolated from Heterosiphonia japonica. R-Phycoerythrin is a potent fluorescent probe contains four chromophore-carrying subunits that exhibits extremely bright red-orange fluorescence. (λex=496 nm, λem=578 nm)[1][2].
Zicronapine is an antipsychotic medication with a strong pro-cognitive effect in animal models and the potential to treat a number of neurological and psychiatric diseases. Zicronapine has potent antagonistic effects at dopamine D1/D2, and serotonin 5-HT2A receptors.
Suvizumab (KD-247) is an neutralizing antibody anti-HIV-1. Suvizumab reduces the viral load in HIV-infected patients. Suvizumab has good tolerance in human body and can be used to prevent HIV infection[1][2].
Magnolioside, isolated from Angelica gigas Nakai (Umbelliferae), exhibits significant neuroprotective activities against glutamate-induced toxicity[1].
Pendetide is a chelating agent, can be conjugated with Indium (111In) Capromab for further diagnostic use. Capromab pendetide is a FDA-approved imaging agent for the detection of soft tissue metastases in prostate carcinoma[1].
Autotaxin-IN-1 is a potent autotaxin inhibitor, which has favorable potency (IC50=2.2 nM), PK properties, and a robust PK/PD relationship. Autotaxin-IN-1 is used in treatment of osteoarthritis pain[1].
Auristatin PE is a novel synthetic Dolastatin 10 derivative and inhibitor of tubulin polymerization.
(R)-TCO-OH is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].
D-Mannitol-d1 is the deuterium labeled D-Mannitol.
4-Nitrophenyl β-D-galactopyranoside is a derivative of beta-D-galactoside and monosaccharide. 4-Nitrophenyl β-D-galactopyranoside can be used for affinity label[1].
Synstab A is a mitosis modulator to promote interactions between α- and β-tubulin. Synstab A can polymerizes microtubules from purified tubulin, and produces microtubule bundles in interphase cells[1][2].
Phenylbutazone-d10 (diphenyl) is the deuterium labeled Phenylbutazone. Phenylbutazone is an efficient reducing cofactor for the peroxidase activity of prostaglandin H synthase (PHS). Phenylbutazone, a hepatotoxin, is a nonsteroidal anti-inflammatory drug (NSAID). Phenylbutazone induces muscle blind-like protein 1 (MBNL1) expression and has the potential for ankylosing spondylitis research[1][2].
Efinopegdutide (JNJ-64565111) is a potent dual glucagon-like peptide-1 (GLP-1)/glucagon receptor (GluR) agonist, which activates both the GLP-1 and glucagon receptors. Efinopegdutide can be used in research of nonalcoholic steatohepatitis (NASH)[1].
Purvalanol A is a potent CDK inhibitor, which inhibits cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, cdk4-cyclin D1, and cdk5-p35 with IC50s of 4, 70, 35, 850, 75 nM, resepctively.
(+)-Cinchonaminone shows monoamine oxidase (MAO) inhibitory activity.
Interiorin D is a natural product[1].
Talatisamine, a aconitum alkaloid，is specific K+ channel blocker. Talatisamine attenuates beta-amyloid oligomers induced neurotoxicity in cultured cortical neurons[1].
Prezalumab (AMG 557) is a humanized IgG2 monoclonal antibody targets ICOSL and BAFF. Prezalumab demonstrates beneficial activities on the arthritis of systemic lupus erythematosus. Prezalumab can be used for the research of sjogren's syndrome cutaneous lupus erythematosus, psoriasis and systemic lupus erythematosus (SLE)[1].
Neladenoson dalanate is a potent, selective, orally acitve partial adenosine A1 receptor (A1AR) agonist (EC50=0.1 nM) for the treatment of chronic heart failure. Heart Failure Phase 2 Clinical
Dihydrexidine (DAR-100) is a high potent, selective and full efficacy D1 dopamine receptor agonist with an IC50 of 10 nM, and displays some affinity for the D2 receptor. Dihydrexidine (DAR-100) exhibits potent antiparkinsonian activity[1][2][3].
Brassicasterol, a metabolite of Ergosterol, plays a role in the inhibitory effect on bladder carcinogenesis promotion via androgen signaling[1]. Brassicasterol shows dual anti-infective properties against HSV-1 (IC50=1.2 µM) and Mycobacterium tuberculosis, and cardiovascular protective effect[2]. Brassicasterol exerts an anti-cancer effect by dual-targeting AKT and androgen receptor signaling in prostate cancer[3].