IDO1/2-IN-1 hydrochloride (compound 4t) is the first potent IDO1/IDO2 dual inhibitor with IC50s of 28 nM and 144 nM for IDO1 and IDO2, respectively. IDO1/2-IN-1 hydrochloride exhibits antitumor activies. Orally active[1].
Metoprolol-d5 is the deuterium labeled Metoprolol[1]. Metoprolol is an orally active, selective β1-adrenoceptor antagonist. Metoprolol shows anti-inflammation, antitumor and anti-angiogenic properties[2][3][4].
HN37 as a potent and chemically stable antiepileptic drug candidate, with an EC50 of 37 nM for KCNQ2[1].
γ-bag cell peptide is a peptide. γ-bag cell peptide is located near the N-terminus of the egg laying prohormone, the vesicle is released upon insulin stimulation. γ-bag cell peptide can be used for the research of the central and peripheral nervous systems[1].
Lapaquistat-d9 acetate (TAK-475-d9) is the deuterium labeled Lapaquistat acetate. Lapaquistat acetate (TAK-475) is a squalene synthase inhibitor, blocking the conversion of farnesyl diphosphate (FPP) to squalene in the cholesterol biosynthesis pathway[1]. Lapaquistat acetate is effective at lowering low-density lipoprotein cholesterol, but it might cause liver damage. Lapaquistat acetate is used for hypercholesterolemia and mevalonate kinase deficiency (MKD) research[2].
4,4'-Oxydianiline-d12 is the deuterium labeled 4,4'-Oxydianiline[1].
(R)-NODAGA-tris(t-Bu ester) ((R)-NODAG) is a NODAGA derivative. (R)-NODAGA-tris(t-Bu ester) can be used to label peptides, antibodies, etc., and subsequently radiolabeled for PET imaging[1].
Fmoc-Lys(2-Cl-Z)-OH is a lysine derivative[1].
Benzamide Derivative 1 is a benzamide derivative from patent EP0213775A1, compound 18. Benzamide Derivative 1 may be useful in treatment of gastrointestinal disorders.
Pregnenolone monosulfate acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, reduces several effects of tetrahydrocannabinol (THC).
Tetrahydrodeoxycorticosterone-d3 is the deuterium labeled Tetrahydrodeoxycorticosterone. Tetrahydrodeoxycorticosterone, an neurosteroid, is a potent positive allosteric modulator (PAM) of GABAA receptor. Tetrahydrodeoxycorticosterone has potent neuroinhibitory properties[1][2][3].
Suzetrigine is a blocker of sodium channel protein type 10 subunit alpha. Suzetrigine acts as an analgesic[1].
Cariprazine is a novel antipsychotic drug candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
N-trans-Feruloylputrescine is an alkaloid that can be isolated from Magnolia officinalis[1].
MC-Val-Cit-PAB-clindamycin has a bioreversible linkage based on a quaternary ammonium for targeted delivery and it can improve pharmacokinetics and the therapeutic index. MC-Val-Cit-PAB-clindamycin is used for the antibody-drug conjugates (ADC) that are effective and stable in vitro and in vivo to treat various diseases or disorders[1].
Nusinersen is an antisense oligonucleotide drug that modifies pre–messenger RNA splicing of the SMN2 gene and thus promotes increased production of full-length SMN protein[1].
MK-4688 is an efficient inhibitor of the HDM2-p53 protein-protein interaction.
Isopropyl 4-hydroxybenzoate-d4 is the deuterium labeled Isopropyl 4-hydroxybenzoate[1].
Apramycin sulfate is an aminoglycoside antibiotic mproduced by a strain of Streptomyces tenebrarius, used in veterinary practice.
Anticancer agent 122, an inhibitor of human lactate dehydrogenase A enzyme (hLDHA), has good anticancer activities and can be used for anticancer research[1].
Trimethadione is an oxazolidinedione anticonvulsant; commonly used to treat epileptic conditions.
CDK9-IN-15 (compound 50) is a potent CDK9 inhibitor[1].
(-)-GSK598809 is an isomer of GSK598809. GSK598809 is a potent and selective dopamine D3 Receptor (DRD3) antagonist.
LMP7-IN-1 is an inhibitor of immunoproteasome (LMP7), may used in the research of inflammatory and autoimmune diseases, neurodegenerative diseases, proliferative diseases and cancer[1].
Protodeltonin is a steroidal saponin from Dioscorea zingiberensis Wright, with anti-proliferation activity[1].
Ac-Leu-Leu-Norleucinol (ALLN) is a calpain inhibitor, can be used for research of Acetaminophen (HY-66005) induced acute liver damage, and lowers glutamic-oxalacetic transaminease (ALT) and glutamic-pyruvic transaminase (AST)[1].
Denopamine ((R)-(-)-Denopamine) is an orally active, selective β1-adrenergic agonist. Denopamine prolongs survival in a murine model of congestive heart failure induced by viral myocarditis: suppression of tumor necrosis factor-α production in the heart. Cardiovascular effects[1].
GC 14 is a thyroid hormone antagonist.
Benzyl-PEG2-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Rasagiline(AGN1135;TVP1012) is a new MAO-B inhibitor for the treatment of idiopathic Parkinson's disease. Target: Monoamine Oxidase (MAO)-BRasagiline (N-propargyl-1-(R)-aminoindan) is a novel, highly potent irreversible monoamine oxidase (MAO)-B inhibitor, anti-Parkinsonian drug. Rasagiline is effective as monotherapy or adjunct to L-Dopa for patients with early and late Parkinson's disease (PD) [1]. Rasagiline inhibits MAO-B more potently than selegiline and has the advantage of once-daily dosing. In several large, randomized, placebo-controlled trials, rasagiline has demonstrated efficacy as monotherapy in early PD and as adjunctive therapy in advanced PD. In addition, rasagiline has been shown to have neuroprotective effects in in vitro and in vivo studies. The recently completed delayed-start ADAGIO (Attenuation of Disease Progression with Azilect Given Once-daily) trial suggests a potential disease-modifying effect for rasagiline 1 mg/day, though the clinical import of this finding has yet to be established [2]. Rasagiline has been found to be well tolerated and effective in the treatment of early PD and as adjunctive treatment in motor fluctuations. Whether rasagiline is associated with clinically significant neuroprotection (ie, disease modification) in PD is the subject of ongoing clinical trials [3].