(±)-Acetylcarnitine chloride (Acetyl dl-carnitine chloride) is a weak cholinergic agonist with cholinergic properties. (±)-Acetylcarnitine chloride is an important intermediate in lipid metabolism[1][2].
RTI-7470-44 is a potent, selective human trace amine-associated receptor subtype 1 (hTAAR1) antagonist with IC50 of 8.4 nM in vitro cAMP functional assay.RTI-7470-44 exhibits a Ki of 0.3 nM in a radioligand binding assay, and shows species selectivity (>90-fold) for hTAAR1 over the rat and mouse orthologues.RTI-7470-44 displays good blood–brain barrier permeability, moderate metabolic stability, and a favorable preliminary off-target profile.RTI-7470-44 increased the spontaneous firing rate of mouse VTA dopaminergic neurons and blocked the effects of the known TAAR1 agonist RO5166017.
AMTB hydrochloride is a selective TRPM8 channel blocker. AMTB hydrochloride inhibits icilin-induced TRPM8 channel activation with a pIC50 of 6.23. AMTB hydrochloride can be used for the research of the overactive bladder and painful bladder syndrome. AMTB hydrochloride is a non-selective inhibitor of voltage-gated sodium channels (NaV)[1][2].
Osteocalcin (1-49) (human) is a vitamin K-dependent bone specific protein. Osteocalcin (1-49) (human) is chemotactic for several of the cell types frequently found at bone remodeling surfaces[1][2].
Oleoyl proline is a novel N-acyl amine compound[1].
N-(((9H-Fluoren-9-yl)methoxy)carbonyl)-N-methyl-D-leucine is a leucine derivative[1].
4'-Hydroxy-3'-methylacetophenone, a phenolic volatile compound, is isolated from Hawaiian green coffee beans (Coffea Arabica L.). 4'-Hydroxy-3'-methylacetophenone has potent antioxidant activities. 4'-Hydroxy-3'-methylacetophenone also can be used to synthesize heterocyclic compounds which have antimycobacterial activity[1][2].
Epelsiban (GSK 557296) is a potent, selective and orally bioavailable oxytocin receptor antagonist, with a pKi of 9.9 for human oxytocin receptor.
N4-Benzo yl-5’-O-(4,4’-dimethoxytrityl)-aracytidine 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].
SB-216641A (SB-216641 hydrochloride) is a selective antagonist of 5-HT1B/D receptor. SB-216641A shows high affinity and selectivity for h5-HT1B receptors over h5-HT1D receptors. SB-216641A blocks SKF-99101H from functioning in vivo[1][2].
10-Deacetyl-13-oxobaccatin III is an taxane that can be isolated from Taxus sumatrana. 10-Deacetyl-13-oxobaccatin III (30 μg/mL) shows cytotoxicity against A498, NCI-H226, A549, PC-3 cells, with inhibition a rate of 29.7%, 49.2%, 43.9%, 65.3%[1].
Bistrifluron has insecticidal effects on the larval stage, and also has an effect on adult longevity, reproduction, and hatchability. Bistrifluron is used for the control of a variety of Lepidopterous pests[1].
Syringaldehyde is a polyphenolic compound belonging to the group of flavonoids and is found in different plant species like Manihot esculenta and Magnolia officinalis[1]. Syringaldehyde moderately inhibits COX-2 activity with an IC50 of 3.5 μg/mL[2]. Anti-hyperglycemic and anti-inflammatory activities[1].
RC-3095 TFA is a bombesin/gastrin releasing peptide receptor antagonist[1].
SPDP-PEG4-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
CC214-1 is a potentially efficacious mTOR inhibitor that induces autophagy [1],with an IC50 is 0.002 μM. CC214-1 proved to be useful as an in vitro tool compound for the exploration of mTOR kinase biology. CC214-1 can be used for Glioblastoma study[2].
KIN1408 is an antiviral small molecule compound, as agonists of the RLR pathway.Target: KIN1408 activate IRF3 through MAVS, thereby inhibiting infection by viruses of the families Flaviviridae (West Nile virus, dengue virus and hepatitis C virus), Filoviridae (Ebola virus), Orthomyxoviridae (influenza A virus), Arenaviridae (Lassa virus) and Paramyxoviridae (respiratory syncytial virus, Nipah virus) .
DBCO-PEG1-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
PF-03654746 is a potent and selective histamine H3 receptor antagonist with high brain penetration.PF-03654746 reduces allergen-induced nasal symptoms, might be a novel therapeutic strategy to further explore allergic rhinitis[1].PF-03654746 improves cognitive efficacy and disease-modifying effects in Alzheimer's disease (AD)[2].
Glucocorticoid receptor agonist-1 phosphate Gly-Glu (TFA) is a cleavable linker, that can be used to synthesize Antibody-Drug Conjugates (ADCs).
Reboxetine Mesylate is a norepinephrine reuptake inhibitor use in the treatment of unipolar depression.Target: OthersReboxetine is a drug of the norepinephrine reuptake inhibitor class. Reboxetine dose-dependently and potently inhibits locus coeruleus neuronal firing in rats with ED50 of 191 μg/kg. Reboxetine inhibition of the locus coeruleus neurons is reversible by the α2 antagonist piperoxan (1.5 mg/kg, IV). Reboxetine dose-dependently reverses reserpine-induced blepharospasm and hypothermia in the mouse. Reboxetine is also found to antagonize clonidine-induced hypothermia dose-dependently in mice. Reboxetine reverses reserpine-induced blepharospasm and hypothermia in rats with ED50 of 10 mg/kg and 3 mg/kg (p.o.), respectively [1]. Reboxetine is associated with a markedly lower relapse rate than placebo (22% vs. 56%) and a greater cumulative probability of a maintained response during long-term treatment in patients with recurrent DSM-III-R major depression. Reboxetine effectively prevents recurrence of depressive symptoms following episode resolution [2]. Acute systemic administration of Reboxetine (0.3 mg/kg-20 mg/kg) dose-dependently increases extracellular norepinephrine in the rat frontal cortex while having no effect on extracellular serotonin. Reboxetine (20 mg/kg) also increases extracellular dopamine in the rat frontal cortex. Chronic administration of Reboxetine for 14 days results in elevated basal concentrations of extracellular norepinephrine and dopamine and a greater net increase of extracellular norepinephrine and dopamine, but not serotonin in the rat frontal cortex [3].
Napabucasin is a STAT3 inhibitor which blocks stem cell activity in cancer cells.
C646 is a selective and competitive histone acetyltransferase p300 inhibitor with Ki of 400 nM, and is less potent for other acetyltransferases.
MK2-IN-4 is a MAPKAPK2 (MK2) inhibitor with an IC50 value of 45 nM. MK2-IN-4 can be used in the research of cancer, inflammation, immunology[1].
X-GalNAc is a chromogenic substrate for for N-acetyl-β-galactosidase, used to determine the presence or absence of a cloned DNA insert in bacteria growing on agar plates[1].
4-Iodo-SAHA (1k) is an orally active class I and class II histone deacetylase (HDAC) inhibitor with EC50s of 1.1, 0.95, 0.12, 0.24, 0.85 and 1.3 μM for Skbr3, HT29, U937, JA16 and HL60 cell lines, respectively. 4-Iodo-SAHA (1k) can be used for the research of cancer[1].
Manninotriose is a novel and important player in the RFO(Raffinose family oligosaccharides) metabolism of red dead deadnettle; potential to improve the side effects of MTX for ALL treatment.
Bufarenogin induces intrinsic apoptosis via Bax and ANT cooperation[1].
D-(+)-Melezitose hydrate ((+)-Melezitose hydrate) can be used to identify clinical isolates of indole-positive and indole-negative Klebsiella spp[1].
Chrysanthemic acid (NSC 11779) is an organic compound that is associated with a variety of natural and synthetic insecticides for the prevention of insect-borne diseases, among others[1].