Rolapitant hydrochloride hydrate (SCH619734 hydrochloride hydrate) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant hydrochloride hydrate does not interact with CYP3A4. Rolapitant hydrochloride hydrate shows potent anti-emetic activity in a ferret emesis model[1][2].
AGDV is the γ chain of fibrinogen. AGDV is critical for platelet aggregation[1][2].
Antifungal agent 34 (compound 6i) is a potent antifungal agent. Antifungal agent 34 shows a potent antifungal activity against Candida albicans, with a MIC of 4 µg/mL. Antifungal agent 34 shows significant inhibition on Candida albicans hyphae and biofilm development. Antifungal agent 34 exhibits no cytotoxicity to mammalian cells[1].
5-Methylcytosine-d4 is the deuterium labeled 5-Methylcytosine[1]. 5-Methylcytosine is a well-characterized DNA modification, and is also predominantly in abundant non-coding RNAs in both prokaryotes and eukaryotes. 5-Methylcytosine in mRNA is a new epitranscriptome marker inArabidopsis, and that regulation of this modification is an integral part of gene regulatory networks underlying plant development[2].
Limocitrin 3,7-diglucoside is a flavonoid isolated from Sedum sarmentosum.
Alosetron D3 (GR 68755 D3) is a deuterium labeled Alosetron. Alosetron is a serotonin 5HT3-receptor antagonist[1].
(Rac)-Rivastigmine-d6 ((Rac)-Rivastigmine-d6) is a labelled racemic Rivastigmine. Rivastigmine (S-Rivastigmine) is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM , 4.15 μM, respectively. Rivastigmine can pass the blood brain barrier (BBB). Rivastigmine is a parasympathomimetic or cholinergic agent used for the research of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease[1][2].
UCSF678 is a 42 nM arrestin-biased partial agonist at the 5-HT5AR with a more restricted off-target profile and decreased assay liabilities. UCSF678 is a selective probe with which to study the function of the 5-HT5AR[1].
Ko 143 is a potent and selective ATP-binding cassette sub-family G member 2 (ABCG2) inhibitor.
PF-5190457 is a potent and selective ghrelin receptor inverse agonist with a pKi of 8.36.
Lycopsamine, a pyrrolizidine alkaloid, is a potential antitumor agent isolated from Eupatorium maculatum L.[1].
Lucidin 3-O-glucoside is an anthraquinone analogue[1].
OMDM-6 is a hybrid agonist of vanilloid receptor type 1 (VR1, TRPV1) (EC50=75 nM) and cannabinoid receptor type 1 (CB1) (Ki=3.2 μM). OMDM-6 inhibits anandamide cellular uptake (ACU) with a Ki of 7.0 μM[1].
RH1 (NSC 697726) is a potent bioreductive agent with profound anti-cancer activity in vitro and in vivo.
Cannabisin B (Compound 7) is a compound isolated from the aerial part of Tetragonia tetragonioides (New Zealand spinach)[1].
ML179 (SR-1309) is a inverse LRH1 (Liver receptor homologue-1) agonist with IC50 of 320 nM. ML179 shows anti-proliferation activity in MDA-MB-231 cells. ML179 has the potential for the research of ER-negative breast cancer[1].
Gemifloxacin mesylate is an oral broad-spectrum quinolone antibacterial agent, used in the treatment of acute bacterial exacerbation of chronic bronchitis, and mild-to-moderate pneumonia.
Entadamide-A-β-D-glucopyranoside is one of the major components in the seeds of Entada phaseoloides. Entadamide-A-β-D-glucopyranoside has anti-complement activitie[1].
Fenbendazole-d3 is a deuterium labeled Fenbendazole. Fenbendazole is a benzimidazole anthelmintic. Fenbendazole is active against Giardia in vitro (IC50 = 0.3 μM). Fenbendazole (20 mg/kg) prevents infiltration of parasites into the brain in a rabbit model of E. cuniculi infection. Fenbendazole also activates HIF-1α and prevents oxidative stress-induced death in primary neurons in vitro.
Bis-aminooxy-PEG1 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
5-(2-Amino-2-oxoethyl)uridine is a purine nucleoside analogue. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Fluorescein Di-β-D-Glucuronide, a fluorescent probe, can be utilized to non-invasively image the intestinal bacterial β-glucuronidase activity in nude mice. Fluorescein Di-β-D-Glucuronide-based imaging reveals the in vitro and in vivo activity of intestinal bacterial β-glucuronidase, which would facilitate pharmacodynamic studies of specific bacterial β-glucuronidase inhibitors in animal studies[1].
Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50 of 13 μM and 370 μM, respectively.
Fumitremorgin C is a potent and selective ABCG2/BRCP inhibitor.
N-(Iodoacetamido)-Doxorubicin is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
3’-Deoxy-2’-thiouridine is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
PDE12-IN-3 is a phosphodiesterase 12 (PDE12) inhibitor with a pXC50 of 7.68. Antiviral activity[1].
ALK-IN-13 is an ALK inhibitor, extracted from patent US20130225528A1, example 19[1].
Isamoltane hemifumarate is a selective antagonist of 5-HT1B receptor, with an IC50 of 39 nM for inhibits the binding of [125I]ICYP to 5-HT1B recognition sites in rat brain membranes. Isamoltane hemifumarate is also a β-adrenoceptor ligand, with an IC50 of 8.4 nM. Isamoltane hemifumarate shows anxiolytic activity[1].
E6446 is a potent and orally acitve TLR7 and TLR9 antagonist, used in the research of deleterious inflammatory responses.