LY404039 is an inhibitor for mGluR1(Ki=149 nM) and mGluR2(Ki= 92 nM), which can also inhibit dopamine receptor.IC50 Value:149 nM(Ki for mGlu2); 92 nM(Ki for mGlu3)[1]Target: mGluR1; mGluR2Metabotropic glutamate (mGlu) receptors have been shown to mediate a number of behaviors including emotionality and responsivity to stress as demonstrated by efficacy in preclinical and clinical studies.in vitro: Similar to LY354740, LY404039 is a nanomolar potent agonist at recombinant human mGlu2 and mGlu3 receptors (K(i) = 149 and 92, respectively) and in rat neurons expressing native mGlu2/3 receptors (Ki = 88). LY404039 is highly selective for mGlu2/3 receptors, showing more than 100-fold selectivity for these receptors, versus ionotropic glutamate receptors, glutamate transporters, and other receptors targeted by known anxiolytic and antipsychotic medications[1].in vivo: LY404039 attenuated amphetamine- and phencyclidine-induced hyperlocomotion (3-30 and 10 mg/kg, respectively). LY404039 (3-10 mg/kg) inhibited conditioned avoidance responding. LY404039 also reduced fear-potentiated startle in rats (3-30 microg/kg) and marble burying in mice (3-10 mg/kg), indicating anxiolytic-like effects. Importantly, LY404039 did not produce sedative effects or motor impairment as measured by rotarod performance and lack of escape failures in the conditioned avoidance task (at doses up to 30 and 10 mg/kg, respectively). LY404039 (10 mg/kg) also increased dopamine and serotonin release/turnover in the prefrontal cortex [3].Clinical trial: An Absolute Bioavailability Study of LY-2140023 and LY-404039 in Healthy Subjects Using the Intravenous Tracer Method. Phage1
trans-Zeatin-d5 is deuterium labeled trans-Zeatin. trans-Zeatin is a plant cytokinin, which plays an important role in cell growth, differentiation, and division; trans-Zeatin also inhibits UV-induced MEK/ERK activation.
3-Aminobutanoic acid is a β-amino acid. 3-Aminobutanoic acid can protect plant against a challenge infection with P. infestans. 3-Aminobutanoic acid has various levels of susceptibility for the pathogen[1].
Fenticonazole is an imidazole derivative with antibacterial and antifungal activity. Fenticonazole has the potential for the research of mixed vaginitis[1][2].
Lomitapide (AEGR-733; BMS-201038) is a potent inhibitor of microsomal triglyceride-transfer protein (MTP) with an IC50 of 8 nM in vitro.
Synstatin (92-119) is an anti-tumor agent that inhibits angiogenesis and cancer cell invasion. Synstatin (92-119) down-regulates integrin α?β3 and reduces the activation of angiogenic growth factors VEGF and FGF-2[1][2].
AL 8697 is a selective p38 MAPK inhibitor with IC50s of 6 nM and 82 nM for p38α and p38β, respectively[1].
Sheng Gelieting (CGT-8012) is a dipeptidy peptidase-IV enzyme (DP-IV) inhibitor. Sheng Gelieting has great DP-IV inhibition activity with an IC50 value of 87 nM. Sheng Gelieting can be used for curing or preventing diseases relevant to the dipeptidy peptidase-IV enzyme, such as the diabetes, particularly the II-type diabete[1].
Phthalide is a promising chemical scaffold with a potent anti-inflammatory efficacy. Phthalide can be used to synthesize a variety of phthalide derivatives including anti-inflammatory agent, antimicrobial, antioxidant[1][2][3].
HsTX1, from the scorpion Heterometrus spinnifer, is a 34-residue, C-terminally amidated peptide cross-linked by four disulfide bridges. HsTX1, an the inhibitor of potassium channel, with IC50 for Kv1.3 of 12 pM inhibits TEM cell activation and attenuates inflammation in autoimmunity[1][2][3].
Ornoprostil is a prostaglandin E1 analogue. Ornoprostil is orally active and can be used for gastric ulcer research[1].
Etzadroxil (Ethyl 2-Ethylbutyrate) is a volatile ester compound. Sulopenem Etzadroxil is an orally available ester prodrug form of Sulopenem, an antibiotic with broad-spectrum activities against Gram-positive and Gram-negative bacteria[1][2].
LKBtide is a biological active peptide. (This is a peptide substrate that is phosphorylated by Serine/Threonine kinase 11 (STK11), also known as LKB1. LKBtide is derived from sucrose non-fermenting 1 (SNF1) protein kinase, which is normally activated by the LKB1/AMP-activated protein kinase (AMPK) signaling pathway.)
CORM-401 is an oxidant-sensitive CO-releasing molecule, can be used in the research of inflammatory and oxidative stress-mediated pathologies.
Butyryltimolol, an effective prodrug of Timolol, improves the corneal penetration of Timolol[1]. Butyryltimolol is a β-adrenergic blocker[2].
Bis-(N,N’-amine-PEG3)-Cy5 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Zatonacaftor is a modulator of cystic fibrosis transmembrane regulator (CFTR) protein. Zatonacaftor can be used for research of cystic fibrosis[1][2].
Fmoc-Ser(tBu)-ODhbt is a serine derivative[1].
Human PD-L1 inhibitor IV, a polypeptide, is a competitive human PD-1 protein inhibitor with a Kd value of 1.38 μM. Human PD-L1 inhibitor IV inhibit the interaction of hPD-1/hPD-L1[1].
Sarmentocymarin can be isolated from the air-dried powd. roots of Cryptolepis buchanani Roem[1].
Kaempferide is an O-methylated flavonol, a type of chemical compound. It can be found in Kaempferia galanga (aromatic ginger). The enzyme kaempferol 4'-O-methyltransferase uses S-adenosyl-L-methionine and kaempferol to produce S-adenosyl-L-homocysteine and kaempferide. P-glycoproteins.
HIV-1, HIV-2 Protease Substrate is the substrate of HIV-1, HIV-2 protease. And there are 4 residues for conservative substitutions of the substrate binding residues of HIV-1 and HIV-2 protease[1].
SG3199-Val-Ala-PAB is an intermediate of Tesirine synthesis. Tesirine is a drug-linker conjugate for ADC which can be used for the research of several cancers[1].
Heparastatin is a heparanase inhibitor.
Futoamide is an active compound. Futoamide can be isolated from Piper futokadzura SIEB. et ZUCC[1].
EC1167 is the linker for EC1169. EC1169 is prostate-specific membrane antigen targeting-tubulysin conjugate. EC1169 has the potential to treat recurrent metastatic, castration-resistant prostate cancer (MCRPC)[1].
TAMRA azide, 5-isomer is a click chemical containing azide groups that can be used as a linker for the orange dye TAMRA. The azide group of TAMRA Azide, 5-isomer enables copper-catalyzed click chemical reactions with alkynes, DBCO, and BCN[1][2].
Epitizide, a benzothiadiazine, commonly found in combination Triamterene, is used to produce diuresis[1].
GV-196771A is the sodium salt form of GV196771, is an NMDA receptor antagonist.