Ciwujianoside D1 is a natural product that can inhibit histamine release induced by anti-immunoglobulin E from rat peritoneal mast cells[1].
2"-O-Galloylquercitrin (Compound 6) is isolated from the natural Acer ginnala. 2"-O-Galloylquercitrinhas health benefits. 2"-O-Galloylquercitrin has the activity of free radical scavenger [1].
NRD167 is a potent and selective SIRT5 inhibitor.
Atracurium Besylate is a neuromuscular blocking agent with ED95 of 0.2 mg/kg. Target: nAChRAtracurium besylate is a neuromuscular-blocking drug or skeletal muscle relaxant in the category of non-depolarizing neuromuscular-blocking drugs, used adjunctively in anesthesia to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation. Atracurium is classified as an intermediate-duration non-depolarizing neuromuscular-blocking agent [1]. A 14C radiolabeled metabolism study in cats confirmed the lack of hepatic or renal involvement in the metabolism of atracurium: radioactivity eliminated in bile and urine was predominantly from metabolites rather than the unchanged parent drug [2].
Dihydrodeoxyuridine (H2dUrd) 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].
N-Nitrosodiethylamine-d4 is the deuterium labeled N-Nitrosodiethylamine[1]. N-Nitrosodiethylamine (Diethylnitrosamine) is a potent hepatocarcinogenic dialkylnitrosoamine. N-Nitrosodiethylamine is mainly present in tobacco smoke, water, cheddar cheese, cured, fried meals and many alcoholic beverages. N-Nitrosodiethylamine is responsible for the changes in the nuclear enzymes associated with DNA repair/replication. N-Nitrosodiethylamine results in various tumors in all animal species. The main target organs are the nasal cavity, trachea, lung, esophagus and liver.
Ro 48-8071 is an inhibitor of OSC (Oxidosqualene cyclase) with IC50 of appr 6.5 nM.
1,4,7-Triazonane (1,4,7-Triazacyclononane), an intermediate in the synthesis of 1,4,7-trifunctionalized derivatives, is a possible reagent for compleximetric titrations with high cation-binding selectivity[1][2].
HA15-Biotin is a chemical probe that consists of HA15 and biotin attached on the amide part of HA15. HA15-Biotin exhibits similar levels of activity to HA15. HA15-Biotin can be used for proteomic analysis[1].
SB-328437 is a potent, selective non-peptide CCR3 antagonist with an IC50 of 4.5 nM[1].
MCOPPB is an orally active and selective agonist of Nociceptin/Orphanin FQ–Receptor. MCOPPB inhibits signaling through the NOP receptor in the mouse brain. MCOPPB is used in anxiety disorders research[1].
H-Ser-Tyr-OH is a dipeptide consisting of glutamic acid, glycine and histidine. H-Ser-Tyr-OH can form a copper(II) complex with copper ions to form a strong free radical scavenging activity. H-Ser-Tyr-OH also increases the intracellular uptake of the delta opioid receptor ligand deltorphin[1].
Tryptamine-d4 hydrochloride is the deuterium labeled Tryptamine hydrochloride. Tryptamine hydrochloride, a monoamine alkaloid, similar to other trace amines, is believed to play a role as a neuromodulator or neurotransmitter[1].
Niraparib metabolite M1 is a metabolite of niraparib, and the latter one acts as a novel poly(ADP-Ribose) polymerase (PARP) inhibitor.
Hydroxy Bezafibrate-d6 is the deuterium labeled Hydroxy Bezafibrate[1].
Encequidar (HM30181) mesylate hydrochloride is a potent and selective inhibitor of P-glycoprotein (MDR1). Encequidar mesylate hydrochloride improves anti-tumor efficacy of Paclitaxel (HY-B0015) in mouse tumor models[1][2][3].
PERK-IN-3 is a potent PERK inhibitor with an IC50 of 7.4 nM[1].
ZK 93423 is a potent benzodiazepine GABAA receptor agonist with a certain cooling effect on rodents[1].
Loperamide D6 hydrochloride (R-18553 D6 hydrochloride) is a deuterium labeled Loperamide hydrochloride. Loperamide hydrochloride is an opioid receptor agonist for the treatment of diarrhea[1].
15:0 SM (d18:1/15:0)-d9 is deuterium labeled 15:0 SM (d18:1/15:0).
Fmoc-N-Me-Val-OH is a modified peptide.
Carbodenafil is a Sildenafil (UK-92480) related compound found in health foods. Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM[1].
2,5-Dihydroxyacetophenone, isolated from Rehmanniae Radix Preparata, inhibits the production of inflammatory mediators in activated macrophages by blocking the ERK1/2 and NF-κB signaling pathways[1].
PD176252 is a potent antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide-preferring (BB2) receptor with Kis of 0.17 nM and 1 nM for human BB1 and BB2 receptors, and 0.66 nM, 16 nM for Rat BB1 and BB2 receptors, respectively; PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC50s of 0.31 and 0.66 μM in HL-60 cells.
Siguazodan (SKF 94836) is a potent, selective and orally active phosphodiesterase III (PDE-III) inhibitor with an IC50 of 117 nM. Siguazodan increases cAMP accumulation in intact platelets with an EC50 of 18.88 μM. Siguazodan also inhibits phenylephrine-induced 5-HT release with an IC50 value of 4.2 μM[1][2][3].
Bavisant Hcl hydrate(JNJ-31001074) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD. IC50 Value: Target: H3 receptorin vitro: Bavisant completed a phase II ADHD trial, but no results have been reported [1].in vivo: Mean change from baseline in the total ADHD-RS-IV score at day 42 (primary efficacy endpoint) was -8.8 in the placebo group versus -9.3, -11.2 and -12.2 in the bavisant 1?mg/day, 3?mg/day and 10?mg/day groups, respectively; the change in the 10?mg/day group was not statistically superior to placebo (p=0.161), and hence statistical comparisons of the 1?mg/day and 3?mg/day groups with placebo based on a step-down closed testing procedure were not performed [2].Clinical trial: A Study to Characterize the Pharmacokinetics and Effect of Food on JNJ-31001074 in Healthy Volunteers. Phase 2
Farnesyl acetate is a sesquiterpene isolated from the leaves of Amomum gagnepainii. Farnesyl acetate has significant toxicity against red palm weevil larvae with a LD50 of 7867 ppm[1][2].
Fargesone A is a potent and selective FXR agonist. Fargesone A shows anti-inflammatory activity[1].
Fmoc-His(3-Me)OH derives Histidine-associating compounds with biological activity. Fmoc-His(3-Me)OH, with Fmoc-citrulline-OH, Fmoc-His(1-Me)-OH together, forms tri-peptides and shows vasodilating effect with EC50s of 2.7-4.7 mM in 1.0 mM Phenylephrine (PE)-contracted aorta rings. Fmoc-His(3-Me)OH (resin) also makes Methyl-His-Gly-Lys (His(3-Me)-Gly-Lys), thus acts as an [Ca2+]i inhibitor. Fmoc-His(3-Me)OH methylates NAHIS02, making it unable to block the Alzheimer's Aβ channel[1][2][3].