Sculponeatin N is a ent-kaurane diterpene derivative compound isolated from the plant Isodon sculponeata[1].
Mianserin hydrochloride is a H1 receptor inverse agonist and is a psychoactive agent of the tetracyclic antidepressant.Target: H1 receptorMianserin is a psychoactive drug of the tetracyclic antidepressant (TeCA) therapeutic family. It is classified as a noradrenergic and specific serotonergic antidepressant (NaSSA) and has antidepressant, anxiolytic (anti-anxiety), hypnotic (sedating), antiemetic (nausea and vomiting-attenuating), orexigenic (appetite-stimulating), and antihistamine effects. It is not approved for use in the US, but its analogue, mirtazapine, is. Mianserin was the first antidepressant to reach the UK market that was less dangerous than the tricyclic antidepressants in overdose.Mianserin is an antagonist/inverse agonist of the H1, 5-HT1D, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT6, 5-HT7, α1-adrenergic, and α2-adrenergic receptors, and also inhibits the reuptake of norepinephrine. As a high affinity H1 receptor inverse agonist, mianserin has strong antihistamine effects (sedation, weight gain, etc.). Contrarily, it has negligible affinity for the mACh receptors, and thus lacks any anticholinergic properties. It was recently found to be a potent kappa opioid receptor agonist. In addition, mianserin also appears to be a potent antagonist of the neuronal octopamine receptor. What implications this may have on mood are currently unknown, however octopamine has been implicated in the regulation of sleep, appetite and insulin production and therefore may theoretically contribute to the overall side effect profile of mianserin.
Biotin-PEG2-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Apoptotic agent-1 (Compound 8a) is an apoptotic agent with high antiproliferative activity against cancer cells and low cytotoxic effect. Apoptotic agent-1 induces over-expression of Fas receptor and Cyto C genes[1].
2,4-PDCA (2,4 pyridine dicarboxylic acid) is a broad-spectrum inhibitor of 2OG oxygenase, including JmjC domain-containing family of histone demethylases (JHDMs). 2,4-PDCA is a target chemical in the field of bio-based plastics[1][2][3].
H-Arg-4MβNA is a substrate for cathepsin H, used for the detection of enzyme activity in gel electrophoresis.
TUG-770 is a highly potent free fatty acid receptor 1 (FFA1/GPR40) agonist with EC50 of 6 nM for hFFA1.IC50 Value: 6 nM (hFFA1, EC50) [1]Target: GPR40in vitro: TUG-770 (Compound 22) displayed excellent physicochemical and in vitro ADME properties, with good aqueous solubility, good chemical stability, low lipophilicity, and decreased plasma protein binding (PPB). TUG-770 furthermore showed excellent stability toward human liver microsomes (HLM), no inhibition of selected CYP-enzymes implicated in drug-drug interactions, no P-glycoprotein (P-gp) inhibition, and good permeability in the Caco-2 cell assay [1].in vivo: Examination of TUG-770 in an acute intraperitoneal glucose tolerance test (IPGTT) in normal mice revealed a good dose dependent response with maximal reduction in glucose level reached at 50 mg/kg. The effect of TUG-770 was fully sustained after 29 days of daily oral treatment. Additional evaluation of TUG-770 in rats confirmed a significant glucose lowering effect for the high doses already after 10 min and for all doses after 30 min [1].Clinical trial:
P7C3 is a NAMPT activator. P7C3 can enhance learning and memory in aged rats. Protects newborn neurons in the dentate gyrus by mitigating cell death. In vitro: Administration of active P7C3 chemicals to cells treated with doxorubicin, which induces NAD depletion, led to a rebound in intracellular levels of NAD and concomitant protection from doxorubicin-mediated toxicity. In vivo: P7C3 is orally bioavailable, crosses the blood-brain barrier, and is non-toxic at doses several fold higher than the efficacious dose.An easily administered pro-neurogenic compound. The administration of P7C3 is 10mg/ kg( IP) in rats. Administration of P7C3 to normal mice, as well as npas3-/- mice, enhance survival of neurons subsequent to their birth in the SGZ.
S1P1 agonist 6 (Compound I) is a S1P1 agonist that reduces autoimmune ability by blocking the transportation of lymphocytes. S1P1 agonist 6 can be used as an immunosuppressive agent in the study of various autoimmune diseases research[1].
Carbamic acid, N-[2,4-dimethyl-6-(4-morpholinyl)-3-pyridinyl]-, phenylmethyl ester is a new invention for treating, one or more disorders or conditions wherein the dopaminergic system is disrupted, such as one or more disorders or conditions independently selected from the group consisting of: schizophrenia and other psychotic states; mood disorders ADHD; aggression; movement disorders.
Riluzole hydrochloride is an anticonvulsant drug and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.
BI 7446 is a cyclic dinucleotide (CDN)-based potent and selective stimulator of interferon genes (STING) agonist. BI 7446 can activate all five STING variants in cells and induce tumor-specific immune-mediated tumor rejection. BI 7446 can be used for immuno-oncology research[1].
SIRT5 inhibitor 2 (compound 49) is a potent SIRT5 inhibitor with an IC50 value of 2.3 μM. SIRT5 inhibitor 2 has inhibitory activity against the SIRT5-dependent desuccinylation. SIRT5 inhibitor 2 can be used for researching cancer and neurodegenerative diseases[1].
CK2-IN-9 is a potent and selective inhibitor of CK2 kinase with an IC50 of 3 nM. CK2-IN-9 reduces Wnt reporter activity with an IC50 of 75 nM. CK2-IN-9 has low exposure (AUC=0.36 μM/h) and high clearance (CL=65 mL/min/kg) properties in rat[1].
DBCO-PEG12-TCO cantains a TCO and a DBCO moiety. TCO group can specifically react with terrahydrazine.
H-Lys-Trp-Lys-OH is a small molecule peptide which displays antibacterial and antiviral activities extracted from patent CN 104072579 A, Compound AMP12. Sequence: H-Lys-Trp-Lys-OH.
Triptorelin acetate is a Gonadotropin-releasing hormone (GnRH) receptor agonist[1].
Cardionogen 1 (CDNG1/vuc230) is a Wnt signaling pathway inhibitor that slows down Myc-induced liver tumorigenesis. Cardionogen 1 treatment of zebrafish embryos before gastrulation inhibits cardiomyocyte formation, whereas treatment during or after gastrulation induces cardiomyocyte formation. Cardionogen 1 has potential in research into cancer and cardiovascular disease[1][2].
Boc-aminooxy-amide-PEG4-propargyl is a non-cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
MF63 is a selective mPGES-1 inhibitor with an IC50 of 0.9 nM and 1.3 nM for pig mPGES-1 and human mPGES-1 enzyme, respectively. IC50 value: 0.9 nM ( pig mPGES-1); 1.3 nM (human mPGES-1)Target: mPGES-1MF63 potently inhibited the human mPGES-1 enzyme with a high degree (>1000-fold) of selectivity over other prostanoid synthases. In rodent species, MF63 strongly inhibited guinea pig mPGES-1 but not the mouse or rat enzyme. When tested in the guinea pig and a knock-in (KI) mouse expressing human mPGES-1, the compound selectively suppressed the synthesis of PGE(2), but not other prostaglandins inhibitable by nonsteroidal anti-inflammatory drugs (NSAIDs), yet retained NSAID-like efficacy at inhibiting lipopolysaccharide-induced pyresis, hyperalgesia, and iodoacetate-induced osteoarthritic pain.
Sanguinarine (Sanguinarin) gluconate, a benzophenanthridine alkaloid, can stimulate apoptosis via activating the production of reactive oxygen species (ROS). Sanguinarine-induced apoptosis is associated with the activation of JNK and NF-κB[1].
Yttrium (90Y) anditixafortide is a diagnostic imaging agent[1].
Pyridoclax is a potential Mcl-1 inhibitor.
C6-NBD Sphinganine is a sphinganine analog and can be used as fluorescent dye for labeling fatty acid[1].
N1-Glutathionyl-spermidine disulfide is a substrate of trypanothione reductase[1].
Promazine (hydrochloride) is a D2 dopamine receptor antagonist, belongs to the phenothiazine class of antipsychotics, used to treat schizophrenia.
m-PEG4-NH-DBCO is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
(E)-Alprenoxime is the isomer of the Alprenoxime. Alprenoxime is a site-activated ocular β-blocker.
Glucagon is a peptide hormone that helps regulate the blood sugar (glucose) levels in the body.
Lerodalcibep (LIB003) is a recombinant fusion protein of a PCSK9-binding domain (adnectin) and human serum albumin. Lerodalcibep is a Lipid-lowering agent. Lerodalcibep can be used for the research of hypercholesterolemia and cardiovascular diseases[1].