A novel potent, selective, orally active translocator protein 18 kDa (TSPO/PBR) antagonist with Ki of 0.33-9.3 nM for both rat and human TSPO; displays high selectivity over 98 other receptors, transporters, ion channels and enzymes; inhibits both neurosteroid accumulation and noradrenaline release in the brain of rats exposed to acute stress; suppresses conditioned fear stress-induced freezing behavior in rats with an efficacy equivalent to that of diazepam, but without not affect learning and memory. Irritable Bowel Syndrome Phase 2 Clinical
Br-DAPI is a water-soluble, cell-permeable, DNA-binding photosensitizer.
Pomiferin, a flavonoid from the fruits of Maclura pomifera, acts as an potential inhibitor of HDAC, with an IC50 of 1.05 μM, and also potently inhibits mTOR (IC50, 6.2 µM).
Undecanedioic acid is associated with intercellular matrix macromolecules and specifically with elastin.
CFTR corrector 12 (compound 17C) is a bithiazole derivative, serving as CFTR corrector. CFTR corrector 12 has the ability to correct some folding defective mutants of the channel responsible for the control of chloride transport across the plasma membrane. CFTR corrector 12 recovers the α-sarcoglycan (α-SG) content in mutant cells[1].
6-keto Prostaglandin F1α is an endogenous metabolite present in Cerebrospinal_Fluid, Urine and Blood that can be used for the research of Meningitis, Rheumatoid Arthritis and Cardiopulmonary Resuscitation[1][2][3][4].
HCGRP-(8-37) is a human calcitonin gene-related peptide (hCGRP) fragment and also an antagonist of CGRP receptor. Sequence: Val-Thr-His-Arg-Leu-Ala-Gly-Leu-Leu-Ser-Arg-Ser-Gly-Gly-Val-Val-Lys-Asn-Asn-Phe-Val-Pro-Thr-Asn-Val-Gly-Ser-Lys-Ala-Phe.
3-Phenoxybenzoic acid is an endogenous metabolite.
Anamorelin Fumarate is a novel ghrelin receptor agonist with EC50 value of 0.74 nM in the FLIPR assay.
Valinotricin is a fungal metabolite[1].
2',3',5'-Tri-O-benzoyl-2'-beta-C-methyl-6-azauridine 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].
Nln activator 1 is a first-in-class peptidomimetic neurolysin activator possessing enhanced brain penetration and stability.
DL-threo-Chloramphenicol D5 is a deuterium labeled DL-threo-Chloramphenicol. DL-threo-Chloramphenicol is the racemate of Chloramphenicol.
Clathrodin is a marine alkaloid that can be isolated from sponges of the genus, Agelas. Clathrodin is a modulator of voltage-gated sodium (NaV) channels. Clathrodin is a sodium channel neurotoxin influencing sodium channel ionic conductance[1][2].
5-Carboxytetramethylrhodamine can be used as a fluorescent probe of nucleic acids and proteins. 5-Carboxytetramethylrhodamine displays excitation maxima of 558 nm and an emission maximum of 586 nm[1][2][3].
Zapnometinib (PD0184264), an active metabolite of CI-1040, is a MEK inhibitor, with an IC50 of 5.7 nM. Zapnometinib exhibits antiviral activity against influenza virus and antibacterial activities[1][2][3].
15-keto-Prostaglandin F2α (15-keto-PGF2α) is a metabolite of Prostaglandin F2α. Prostaglandin F2α. Prostaglandin F2α is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist and plays a key role in the onset and progression of labour[1].
Myristoyl glutamic acid sodium is a common ingredient in cosmetics/creams. Myristoyl glutamic acid sodium, a surfactant belonging to the amino acid, has mild cleaning properties and is also foamy and mildly bacteriostatic[1].
4-Methylumbelliferyl oleate is a fluorogenic substrate for acid and alkaline lipases. 4-Methylumbelliferyl oleate is cleaved by lipases, liberating 4-Methylumbelliferyl (Ex/Em=320/450 nm)[1][2].
Fmoc-β-Ala-OH is an alanine derivative[1].
Ro 22-3581 (4'-(Imidazol-1-yl) acetophenone) is a selective thromboxane (Tx) synthetase inhibitor[1].
Jatrophane 5 is a natural product of Jatropha carcas L. Jatrophane 5 has powerful inhibition of P-gp, higher than R(+)-verapamil (HY-14275) and Tariquidar (HY-10550) in colorectal multi-drug resistant cells (DLD1-TxR)[1].
DiSC18(3) is a lipophilic carbocyanine dye for membrane labelling[1].
Momelotinib-d2 (CYT387-d2) is the deuterium labeled Momelotinib (HY-10961). Momelotinib (CYT387) is an orally active and ATP-competitive inhibitor of JAK1/JAK2 with IC50a of 11 nM and 18 nM,respectively, shows much less activity against JAK3[1][2].
HDAC6-IN-26 (compound 23) is a potent inhibitor of HDAC6[1].
L-Cystine is an amino acid and intracellular thiol, which plays a critical role in the regulation of cellular processes.
Chloropyramine hydrochloride is a histamine receptor H1 antagonist which can also inhibit the biochemical function of VEGFR-3 and FAK.
SKF83822 hydrobromide is a potent dopamine D1 receptor agonist. SKF83822 hydrobromide activates Gs/olf/adenylyl cyclase (AC)-coupled D1 receptors, but not phospholipase C (PLC)-coupled D1-like receptors[1].
Chimaphilin is an IGF-1R inhibitor (IC50: 0.086 μM). Chimaphilin has antifungal, antioxidant and anticancer activities. Chimaphilin inhibits the growth of both drug-sensitive and drug-resistant osteosarcoma cell lines. Chimaphilin can induce cancer cell apoptosis. Chimaphilin is a main component of pyrola[1][2].
LY-404187 is a potent, selective and centrally active positive allosteric modulator of AMPA receptors, with the EC50s of 5.65, 0.15, 1.44, 1.66 and 0.21 µM for GluR1i, GluR2i, GluR2o, GluR3i and GluR4i, respectively. LY-404187 has therapeutic potential in a number of psychiatric disorders and neurodegenerative diseases[1][2].