FPH2 induces of functional proliferation of primary human hepatocytes and may lead to the development of new therapeutics for liver diseases.
A potent, selective sodium-coupled citrate transporter (NaCT or SLC13A5) with IC50 of 0.51 uM, >20-fold selectivity over NaDC1 and NaDC3; demonstrates dose-dependent inhibition of radioactive [(14)C]citrate uptake in liver and kidney in vivo, reduces fasting plasma glucose concentrations with suitable in vivo pharmacokinetic profile.
Taurolithocholic acid sodium salt, a potent cholestatic agent, is a potent Ca2+ agonist[1].
Essential oils, Melaleuca alternifolia is extracted from the leaves of Melaleuca alternifolia, has bactericidal and anti-inflammatory activies[1].
(Rac)-Modipafant (UK-74505) is an orally active, selective, long-acting irreversible platelet activating factor receptor (PAFR) antagonist. (Rac)-Modipafant prevents dengue infection[1][2][3].
CPI-169 racemate is the racemate of CPI-169. CPI-169 is a novel and potent EZH2 inhibitor.
Securitinine is a Securinega alkaloid. Securitinine can be derived from the wood of Japanese medicinal plant Securinega suffruticosa var[1].
Uridine triphosphate 13C9,15N2 (UTP 13C9,15N2) sodium is a labeled Uridine triphosphate sodium. Uridine triphosphate sodium can be used in nucleic acid synthesis.
Noopept (GVS-111) is a medication promoted and prescribed in Russia and neighbouring countries as a nootropic.IC50 Value:Target: in vitro: Nooglutil exhibits pharmacologically significant competition with a selective agonist of AMPA receptors ([G-3H]Ro 48-8587) for the receptor binding sites (with IC50 = 6.4 +/- 0.2 microM), while the competition of noopept for these receptor binding sites was lower by an order of magnitude (IC50 = 80 +/- 5.6 microM) [1]. GVS-111 significantly increased neuronal survival after H(2)O(2)-treatment displaying a dose-dependent neuroprotective activity from 10 nM to 100 microM, and an IC(50) value of 1.21+/-0.07 microM. GVS-111 inhibited the accumulation of intracellular free radicals and lipid peroxidation damage in neurons treated with H(2)O(2) or FeSO(4), suggesting an antioxidant mechanism of action [2].in vivo: N-Phenylacetyl-L-prolylglycine ethyl ester (GVS-111) administered intravenously at a dose of 0.5 mg/kg/day, for the first time 1 h after ischaemic lesion and then for 9 post-operative days, with the last administration 15 min before testing, attenuated the deficit [3]. GVS-111 itself was not found in rat brain 1 h after 5 mg/kg i.p. administration up to limit of detection (LOD) under high performance liquid chromatography (HPLC) conditions [4]. The most pronounced antiinflammatory effect of dipeptide was observed on the model of adjuvant arthritis in rats, where the drug administered over 25 days in a daily dose of 0.5 mg/kg (i.m.) or 5 mg/kg (p.o.) significantly reduced the chronic immune inflammation (on the 12th day, by 94.0 and 74.1%, respectively) [5].Toxicity: Noopept administered in this dose range induced no irreversible pathologic changes in the organs and systems studied and exhibited no allergenic, immunotoxic, and mutagen activity [6]. Clinical trial: Discontinued
C3bot(154-182) is a C3 peptide enhances recovery from spinal cord injury by improving regenerative growth of descending fiber tracts. C3bot(154-182) represents a promising tool to foster axonal protection and/or repair, as well as functional recovery after traumatic CNS injury[1].
S-15535 is a highly selective 5-HT1A receptor ligand. S-15535 is an antagonist of postsynaptic 5-HT1A receptors and an agonist of presynaptic 5-HT1A receptors. S-15535 can be used in research on psychiatric disorders, such as anti-anxiety[1].
BI-99179 is a potent and selective inhibitor of type I fatty acid synthase (FAS) with IC50 of 79 nM; demonstrates potent cellular activity (inhibition of 14C-acetate incorporation) with IC50 of 0.6 uM in the mouse N-42 cellular assays, shows no significant LDH release in the cytotoxicity assay at >30 uM; BI-99179 is a tool compound suitable for the in vivo validation of FAS as a therapeutic target.
Fmoc-Lys(Me)2-OH HCl is a lysine derivative[1].
Antitumor agent-40 is an antitumor agent. Antitumor agent-40 can be used for the research of cancer[1].
Priliximab (CEN 000029) is an anti-CD4 humanized monoclonal antibody. Priliximab binds to CD4 on the surface of T cells, resulting in a significant and sustained reduction in circulating CD4+ T cells. Priliximab can be used in research of rheumatoid arthritis (RA)[1].
CDK7-IN-1, an analog of YKL-5-124, is a cyclin-dependent kinase 7 (cdk7) inhibitor, with an IC50 of less than 100 nM, extracted from patent WO 2016105528 A2, Compound 215[1].
N2-iso-Butyroyl-3’-O-methylguanosine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7)[1].
Wnt pathway inhibitor 4 (compound 16D) is an anticancer agent that has anti-proliferative activity[1].
2-tert-Butylamino-d9-4-chloro-6-cyclopropylamino-1,3,5-triazine is the deuterium labeled 2-tert-Butylamino-4-chloro-6-cyclopropylamino-1,3,5-triazine[1].
Antituberculosis agent-1 (Compound 8a) is an antituberculosis agent with an MIC of 3.84 µg/mL against M. tuberculosis H37Rv[1].
Forrestiacids J is an ATP-citrate lyase (ACL) inhibitor with an IC50 of 2.6 μM[1].
Lys-(Des-Arg9,Leu8)-Bradykinin is a bradykinin B1 receptor antagonist[1].
Potassium acetate is a potassium salt employed to replenish electrolytes, for restoration of water-electrolyte balance. Potassium acetate can employ in DNA and protein purification. Potassium acetate has been used to prepare neutralizing solution for alkaline lysis of bacteria[1][2].
CD532 is a potent Aurora A kinase inhibitor with an IC50 of 45 nM. CD532 has the dual effect of blocking Aurora A kinase activity and driving degradation of MYCN. CD532 also can directly interact with AURKA and induces a global conformational shift. CD532 can be used for the research of cancer[1][2].
3′-Azido-2′,3′-dideoxy-5-hydroxyuridine 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].
Tubeimoside II(Tubeimoside-B) is a natural analogue of oleanane type of triterpenoid saponin; show anti-inflammatory, antitumor, and antitumor-promoting effects.IC50 value:Target:The anti-inflammatory, anti-tumor, and anti-tumorigenic activities of tubeimoside II are stronger than those of tubeimoside I, and the acute toxicity of tubeimoside II is lower than that of tubeimoside I; the anti-inflammatory, anti-tumor, and anti-tumorigenic activities of tubeimoside III are stronger than those of tubeimoside II, and the acute toxicity of tubeimoside III is also stronger than that of tubeimoside II.
HIV-1 inhibitor-26 (compound 9a) is a potent HIV-1 reverse transcriptase (RT) inhibitor with an IC50 value of 1.4 μM. HIV-1 inhibitor-26 has low cytotoxicity with a CC50 of 1486 μM in PBMCs. HIV-1 inhibitor-26 can be used for researching AIDS[1].
Desmethyl-YM-298198 hydrochloride is a high-affinity, selective, and noncompetitive mGluR1 antagonist (IC50: 16 nM). Desmethyl-YM-298198 hydrochloride has analgesic effect in Streptozotocin (HY-13753)-induced hyperalgesic mice[1].
Palmitoylglycine, a novel endogenous lipid, acts as a modulator of calcium influx and nitric oxide production in sensory neurons. Palmitoylglycine induces transient influx of calcium followed by nitric oxide production via calcium-sensitive nitric-oxide synthase enzymes. Palmitoylglycine potently inhibits heat-evoked firing of nociceptive neurons in rat dorsal horn[1].
TCO-PEG8-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].