Fluphenazine dimaleate is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine dimaleate blocks neuronal voltage-gated sodium channels. Fluphenazine dimaleate acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine dimaleate can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine dimaleate can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2[1][2][3][4][6].
AMG 837 is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.IC50 value: 13 nM (EC50) [1]Target: GPR40 agonistAMG 837 displayed the expected two-fold increase in potency on GPR4 (EC50 = 13 [±7] nM) compared to the racemic compound and its activity crossed over to the rat and mouse forms of GPR40 (EC50 = 23 and 13 nM, respectively). AMG 837 was found to be a partial agonist on GPR40 with maximal activity 85% of that shown by DHA under our standard assay conditions. AMG 837 is a highly potent stimulator of insulin secretion in MIN6 cells with an EC50 comparable to that seen in the aequorin Ca2+-flux assay. showedno significant activity in cell-based assays against PPARα, δ, and γ. An external panel of 64 receptors also revealed no significant activity with the exception of weak inhibition (IC50 = 3 uM) on the a2-adrenergic receptor. Overall, AMG 837 was both highly potentand selective in vitro.
Fomc-Gly-Gly-Phe-Gly-OH (compound D5) can be used as an intermediate in the synthesis of ADC dual-drug-linker. Fomc-Gly-Gly-Phe-Gly-OH synthetic intermediate GGFGE further forms an important ADC dual-drug link assembly unit[1].
Mirtazapine-d4 is deuterium labeled Mirtazapine. Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively[1][2].
Thyminose-13C-2 is the 13C labeled Thyminose. Thyminose is an endogenous metabolite[1].
Fmoc-D-Asp(OtBu)-OH is an aspartic acid derivative[1].
GCN2-IN-7 (compound 39) is an orally active and selective general control nonderepressible 2 (GCN2) inhibitor (IC50=5 nM). GCN2-IN-7 shows anti-tumor activity in vivo[1].
cis-Ned19 is a chemical probe. cis-Ned19 blocks NAADP signaling and fluorescently labeled NAADP receptors in cell[1].
Vipivotide tetraxetan Linker is a useful peptide linker for synthesis of Vipivotide tetraxetan (PSMA-617). Vipivotide tetraxetan (PSMA-617) is a ligand used to synthesize 177Lu-PSMA-617, which is a radioactive molecule for the treatment of prostate cancer[1].
Neurotensin, a gut tridecapeptide, acts as a potent cellular mitogen for various colorectal and pancreatic cancers which possess high-affinity neurotensin receptors (NTR).
CY5-N3 is a Cy5-azide, which is a fluorescent dye.
Palonosetron Hcl is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV).IC50 Value:Target: 5-HT ReceptorPalonosetron is the most effective of the 5-HT3 antagonists in controlling delayed CINV nausea and vomiting that appear more than 24 hours after the first dose of a course of chemotherapy.
BCR-ABL-IN-8 (compound 26f) is a BCR-ABL inhibitor containing trimethoxy group[1].
Enalaprilat D5 Sodium Salt is the deuterium labeled Enalaprilat(MK-422), which is an angiotensin-converting enzyme (ACE) inhibitor.
AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor with IC50 of 5 nM, 4 nM and 1 nM for Aurora A, B and C, respectively.
L-Citrulline-13C is the 13C-labeled L-Citrulline. L-Citrulline is an amino acid derived from ornithine in the catabolism of proline or glutamine and glutamate, or from l-arginine via arginine-citrulline pathway.
Closantel is a salicylanilide anthelmintic compound; exhibits different anthelmintic spectra and apparent toxicity in mammals.
Sudocetaxel zendusortide is an antineoplastic[1].
Methyl-D-alanine is an alanine derivative[1].
Fmoc-β-HoLeu-OH is a leucine derivative[1].
RFRP-3 (rat) is a neuropeptide. RFRP-3 (rat) inhibits gonadotropin secretion, causing a marked increase in ghrelin mRNA and plasma growth hormone levels[1].
Nortriptyline-d3 (Desmethylamitriptyline-d3) hydrochloride is the deuterium labeled Nortriptyline hydrochloride. Nortriptyline hydrochloride (Desmethylamitriptyline hydrochloride) is a tricyclic antidepressant and the main active metabolite of Amitriptyline, and used to relieve the symptoms of depression[1].
NF-κB-IN-3 (Compound 2) is a NF-κB inhibitor with an IC50 of 0.70 µM. NF-κB-IN-3 can be used as an antitumor agent[1].
Ethidium monoazide bromide is a DNA intercalating fluorescent dye that enters bacteria with damaged membranes. Ethidium monoazide bromide can be covalently linked to DNA by photoactivation. Ethidium monoazide bromide stains only dead cells[1].
(2-Chlorophenyl)diphenyl-methanol-d5 is the deuterium labeled (2-Chlorophenyl)diphenylmethanol[1].
RP-001 is a picomolar short-acting S1P1 (EDG1) selective agonist, with an EC50 of 9 pM. RP-00 induces internalization and polyubiquitination of S1P1. RP-001 has little activity on S1P2-S1P4 and only moderate affinity for S1P5[1].
MOG (35-55), human is a component of CNS myelin. MOG (35-55), human is different from mMOG (35-55) by a proline for serine substitution at position 42. MOG (35-55), human is also immunogenic, but not encephalitogenic, and is only partially cross-reactive with mMOG35–55. MOG (35-55), human induces minimal clinical signs of EAE relative to the rodent peptide[1].
MG 1 is an α1 adrenergic receptor antagonist.
Demethyl linezolid is a impurity of linezolid. Demethyl linezolid is a useful antimicrobial agent extracted from patent WO1995007271A1, example 9, effective against a number of human and veterinary pathogens[1].