A novel potent, selective, allosteric and orally active dopamine D1 receptor potentiator with Kb of 26 nM; induces a 21-fold leftward shift in the cAMP response to dopamine in HEK293 cells, 30-fold less potent at rat and mouse D1 receptors and is inactive at the human D5 receptor; robustly (∼10-fold) increases locomotor activity in habituated hD1 mice (3-20 mg/kg), also acts synergistically with L-DOPA to reverse the strong hypokinesia caused by reserpine.
Naloxone is an antagonist of Opioid receptor. Naloxone alleviates opioid-overdose-induced respiratory depression. Naloxone may cause pulmonary edema and cardiac arrhythmias[1].
NS3861 is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding Ki values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively[1].
Aloe emodin is a hydroxyanthraquinone present in Aloe vera leaves, has a specific in vitro and in vivo antitumor activity.IC50 value:Target:in vitro: aloe-emodin treatment led to the dissociation of heat shock protein 90 (HSP90) and ER α and increased ER α ubiquitination. Protein fractionation results suggest that aloe-emodin tended to induce cytosolic ER α degradation [1]. Aloe-emodin, a natural compound found in aloe, inhibited both proliferation and anchorage-independent growth of PC3 cells. Protein content analysis suggested that activation of the downstream substrates of mTORC2, Akt and PKCα, was inhibited by aloe-emodin treatment. Pull-down assay and in vitro kinase assay results indicated that aloe-emodin could bind with mTORC2 in cells and inhibit its kinase activity [2]. Of three anthraquinone derivatives, aloe-emodin, with a lower cytotoxicity showed concentration-dependently reducing virus-induced cytopathic effect and inhibiting replication of influenza A in MDCK cells. Galectin-3 also inhibited influenza A virus replication. Proteomic analysis of treated cells indicated galectin-3 up-regulation as one anti-influenza A virus action by aloe-emodin. Since galectin-3 exhibited cytokine-like regulatory actions via JAK/STAT pathways, aloe-emodin also restored NS1-inhibited STAT1-mediated antiviral responses in transfected cells: e.g., STAT1 phosphorylation of interferon (IFN) stimulation response element (ISRE)-driven promoter, RNA-dependent protein kinase (PKR) and 2'5',-oligoadenylate synthetase (2'5',-OAS) expression [3]. AE downregulated mRNA expression and promoter/gelatinolytic activity of Matrix Metalloproteinase (MMP)-2/9, as well as the RhoB expression at gene and protein level. AE suppressed the nuclear translocation and DNA binding of NF-κB [4].in vivo: Aloe-emodin also exhibited tumor suppression effects in vivo in an athymic nude mouse model [2].
BI-0252 is an orally active, selective MDM2-p53 inhibitor with an IC50 of 4 nM. BI-0252 can induce tumor regressions in all animals of a mouse SJSA-1 xenograft, with concomitant induction of the tumor protein p53 (TP53) target genes and markers of apoptosis[1].
D75-4590, a pyridobenzimidazole derivative and a β-1,6-glucan synthesis inhibitor, possesses antifungal activity[1].
3-epi-Vitamin D3 (Epicholecalciferol) (Compound 4), a Vitamin D3 analogue, is a Hedgehog pathway inhibitor with an IC50 of 39.2 μM measured in U87MG cells[1].
Deracoxib-d3 is the deuterium labeled Deracoxib. Deracoxib, a selective cyclooxygenase-2 inhibitor, is a non-narcotic, non-steroidal anti-inflammatory drug (NSAID).
VU591 is a potent, selective renal outer medullary potassium channel (ROMK or Kir1.1) inhibitor, with an IC50 of 0.24 μM[1].
6-((4-Hydroxybutyl)amino)hexyl 2-hexyldecanoate is a lipid, it can be used to synthesis nanomaterials. 6-((4-Hydroxybutyl)amino)hexyl provides the use of the nano-lipid particle as the key component in nucleic acid delivery, including the components of the delivery carrier[1].
hDHODH-IN-1 is a human dihydroorotate dehydrogenase (hDHODH) inhibitor. hDHODH-IN-1 has anti-inflammatory effect[1].
4-Methylthiophene is an intermediate used in the synthesis of the aromatic sulfur compounds[1].
Coenzyme Q6 (Ubiquinone 30) is an isoprenylated benzoquinone lipid. Coenzyme Q6 exhibits functions in respiratory electron transport and as a lipid antioxidant. Coenzyme Q6 also has antioxidant effects, which can prevent the production of free radicals and oxidative damage[1].
Nilofabicin is an enoyl-(acyl-carrier protein) reductase (FabI) inhibitor. Nilofabicin had an MIC(90) of 0.5 microg/ml for Staphylococcus aureus strains and was more potent than either linezolid or vancomycin[1].
SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 dihydrochloride inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes[1][2][3][4].
Triamcinolone is a long-acting synthetic corticosteroid.Target: Glucocorticoid ReceptorDimethyl fumarate is an anti-inflammatory. It is indicated for multiple sclerosis patients with relapsing forms and is also being investigated for the treatment of psoriasis. The mechanism of action of dimethyl fumarate in multiple sclerosis is not well understood. It is thought to involve dimethyl fumarate degradation to its active metabolite monomethyl fumarate (MMF) then MMF up-regulates the Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) pathway that is activated in response to oxidative stress [1]. The mean duration of follow-up was 40 months. The rate of decline in the FEV1 after bronchodilator use was similar in the 559 participants in the triamcinolone group and the 557 participants in the placebo group (44.2+/-2.9 vs. 47.0+/-3.0 ml per year, P= 0.50). Members of the triamcinolone group had fewer respiratory symptoms during the course of the study (21.1 per 100 person-years vs. 28.2 per 100 person-years, P=0.005) and had fewer visits to a physician because of a respiratory illness (1.2 per 100 person-years vs. 2.1 per 100 person-years, P=0.03). Those taking triamcinolone also had lower airway reactivity in response to methacholine challenge at 9 months and 33 months (P=0.02 for both comparisons) [2].
N-Nitroso-3-azabicyclo[3.3.0]octane-d4 is the deuterium labeled N-Nitroso-3-azabicyclo[3.3.0]octane[1].
5-HT3 antagonist 1 is a potent and selective antagonist of serotonin 3 (5-HT3) receptor.
Ulixertinib (VRT752271) is a reversible, ATP-competitive inhibitor of ERK1 and ERK2 kinases, with IC50 of <0.3 nM against ERK2.
Saponin PE is a saponin compound isolated from aerial part of Clematis tangutica[1].
Loxoprofenol-SRS tromethamine (HR1405-01), an active metabolite of Loxoprofen, is a Safe intravenous non-steroidal anti-inflammatory drug (NSAID) with superior anti-inflammatory and analgesic activities[1].
Isoasiaticoside is a pentacyclic triterpene saponin that can be isolated from Centella asiatica. Isoasiaticoside has potential neuroprotective effects in the 6-OHDA (HY-B1081)-induced PC12 cell model[1].
RNF114 ligand 1 is a E3 Ubiquitin ligase binder[1].
Tricyclazole is a pentaketide-derived melanin biosynthesis inhibitor and a unique fungicide for control of Pyricularia oryzae on rice[1][2].
Enfenamic acid is a nonsteroidal anti-inflammatory agent. Enfenamic acid suppresses wound healing[1][2].
1-Methylisatin is a potent and selective CE (carboxylesterases) inhibitor, with Kis of 38.2 and 5.38 µM for hiCE and hCE1, respectively. 1-Methylisatin interacts with Hb (human adult hemoglobin) by hydrophobic binding and electrostatic attraction. 1-Methylisatin can be used in the study of regulation of drug metabolism in vivo[1][2].
Terbutaline sulfate is a β2-adrenergic receptor agonist; a fast-acting bronchodilator and a tocolytic to delay premature labor.
Quetiapine (hemifumarate)-d8 is the deuterium labeled Quetiapine hemifumarate[1]. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects[2].
H-Val-Thr-Cys-Gly-OH is a cell attachment peptide. H-Val-Thr-Cys-Gly-OH is a bioactive molecule used for cell adhesion or other cell interactions[1].
1-Chlorohexadecane-d33 is the deuterium labeled 1-Chlorohexadecane[1].