OTAVAchemicals, Ltd - synthetic organic compounds for research and drug discovery
     
Home

Send us your structure for synthesis

Design your focused library

Newsletter Subscription

Stay updated with our new products and services. You can unsubscribe at any time.


hPreP Agonist Library

Human Presequence Protease Activators Library A neurotoxic peptide β-amyloid (Aβ) is linked to the beginning of Alzheimer’s disease (AD). The accumulation of amyloid-beta inside mitochondria boosts production of free radical and activation of the apoptotic pathway. Human Presequence Protease (hPreP, PITRM1) is a mitochondrial ATP-independent metalloprotease. It degrades toxic peptides, including mitochondrial presequences and β-amyloid. This enzyme is an attractive target for Alzheimer’s disease drug design because enhancement of it's activity increases the level of Aβ proteolysis.

Read more...
 
5-HT1B Receptor Targeted Library

GPCR focused libraries5-hydroxytryptamine receptors (serotonin receptors , 5-HT receptors) are a group of G protein-coupled receptors (GPCRs) and ligand-gated ion channels found in the central and peripheral nervous systems [1, 2]. They mediate both excitatory and inhibitory neurotransmission. The serotonin receptors are activated by the neurotransmitter serotonin, which acts as their natural ligand.

Read more...
 
SGLT2 Targeted Library

Sodium Glucose Cotransporter 2 Focused Library The sodium glucose cotransporter 2 (SGLT2) reabsorbs most of the glucose filtered by the kidneys. SGLT2 inhibitors reduce glucose reabsorption, thereby lowering blood glucose levels in patients with diabetes [1]. Type 2 diabetes is a chronic disease with disabling micro- and macrovascular complications that lead to excessive morbidity and premature mortality.

Read more...
 
HMGCR Targeted Library

HMG-CoA focused libraryThe enzyme 3-hydroxy-3-methyl-glutaryl-CoA reductase (3-hydroxy-3-methylglutaryl-coenzyme A, HMG-CoA, HMGCR) catalyzes the conversion of HMG-CoA to mevalonate, an early and rate-limiting step in cholesterol biosynthesis. The HMG-CoA reductase inhibitors, also known as statins, are the most effective class of drugs for lowering serum low-density lipoprotein cholesterol concentrations.

Read more...
 
Hsp90 Targeted Library

Hsp90 focused libraryHsp90 (heat shock protein 90) is a highly abundant and ubiquitous molecular chaperone which plays an important role in the folding of newly synthesized proteins or stabilizing and refolding denatured proteins after stress. Its expression is associated with many types of tumors including breast cancer, pancreatic carcinoma, human leukemia and others.

Read more...
 
Glycomimetic Focused Library

Glycomimetic Focused LibrarySeveral glycoprocessing enzymes and glycoreceptors have been recognized as important targets for therapeutic intervention. This concept has inspired the development of important classes of therapeutics, such as anti-influenza, anti-inflammatory, Gaucher’s disease, hepatitis and cancer drugs.

Read more...
 
GCR Antagonist Library

Glucocorticoid Receptor Antagoniat focused libraryGlucocorticoids (GCs) are secreted from the adrenal gland in response to exposure to emotional and physiologic stressors and are responsible for modulating essential metabolic, cardiovascular, immune, and behavioral functions [1–3]. The glucocorticoid receptor (GR) belongs to a family of nuclear hormone receptors that are ligand-dependent transcription factors.

Read more...
 
11β-HSD1 Targeted Library

11beta-hydroxysteroid dehydrogenase type I focused library11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1, cortisone reductase, HSD11B1, 11beta-hydroxysteroid dehydrogenase type 1,11beta-HSD1) is an enzyme that is involved in glucocorticoid regulation by catalyzing the conversion of inactive cortisone to its active form cortisol. These hormones regulate several physiological processes, and modulation of glucocorticoid action has been implicated as a potential treatment for a variety of diseases.

Read more...
 
Histamine Receptor Antagonist Library

Histamine receptor focused libraryIt is generally acknowledged that histamine is an important regulator of a plethora of (patho) physiological conditions and exerts its actions through the interaction with four histamine receptor subtypes. All these receptors belong to the family of heptahelical GPCR's and are considered as a promising molecular targets for drug development.

Read more...
 
HATs Targeted Library

Histone Acetyltransferase target-focused libraryPost-translational modifications, such as acetylation or phosphorylation, play a crucial role in the regulation of gene transcription in eukaryotes. Different subtypes of histone acetyltransferases (HATs) catalyze the acetylation of histones on specific lysine residues. 

Read more...
 
PARP-1 Targeted Library

PARP1 Focused Library Poly (ADP-ribose) Polymerase 1 (PARP-1) also known as NAD+ ADP-ribosyltransferase 1 or poly(ADP-ribose) synthase 1 is an enzyme that modifying nuclear proteins by poly ADP-ribosylation. PARP-1 is involved in modulating DNA repair, DNA replication, transcription, DNA methylation and chromatin remodeling through PARylation of downstream proteins. Also it is involved in differentiation, proliferation, tumor transformation and may participate in the pathophysiology of type I diabetes [1, 2].

Read more...
 
iPPI Focused Libraries

Protein-Protein Interaction Focused LibrariesTargeting protein protein interaction (PPI) is a new challenge to current drug discovery. Due to growing interest in PPI inhibitors we represent focused compound libraries covering chemical space of PPI inhibitors.

Read more...
 
DPP4 Targeted Library

DPP4 Focused LibraryDipeptidyl peptidase-4 (DPP4), also known as adenosine deaminase binding protein or cluster of differentiation 26 (CD26), is a serine exopeptidase able to recognizes an amino acid sequence having proline at the N-terminal penultimate position and inactivate this oligopeptides through the removal of N-terminal proline dipeptides [1, 2].

Read more...
 
Calcium Channel Blockers

Calcium Channel Blockers focused libraryCalcium channel blockers (CCBs) disrupt the movement of calcium (Ca2+) through calcium channels. They are used as antihypertensive drugs, i.e., as medications to decrease blood pressure in patients with hypertension. CCBs are particularly effective against large vessel stiffness, one of the common causes of elevated systolic blood pressure in elderly patients.

Read more...
 
Potassium Channel Blockers

Kv1.5 Potassium Channel BlockerAtrial fibrillation is the most common sustained cardiac rhythm disorder, and confers a substantial mortality and morbidity from stroke, thromboembolism, heart failure, and impaired quality of life. With the increasingly elderly population in the developed world, the prevalence of atrial fibrillation is increasing, resulting in a major public-health problem.

Read more...
 
HCN Channel Blocker Library

HCN Channel BlockerThe current produced by hyperpolarization-activated cyclic nucleotide-gated (HCN) channels (termed If, cardiac pacemaker “funny” current, and Ih in neurons) is also considered a “pacemaker current” because it plays a key role in controlling the rhythmic activity of cardiac pacemaker cells and spontaneously firing neurons.

Read more...
 
Solubility Fragment Library

Solubility Fragment Library

The Solubility Fragment Library consists of about 957 low molecular fragments with "Rule-of-Three" compliance and assured solubility in both DMSO (200mM) and PBS buffer (1mM). The library design included diversity filtering in order to provide chemical structure variety for your fragment screening program.

 

 

Read more...
 
CREBBP Targeted Library

CREBBP focused libraryCREB Binding Protein (CREBBP) is a coactivator of transcription factor CREB that activates genes in cAMP transcriptional pathway. The coactivator binds to transcription factor activation domains positions histone acetyltransferases near specific nucleosomes in target gene promoter regions, recognizing the acetylated lysine residue.

Read more...
 
Halogen-Enriched Fragments

Halogen-Enriched Fragment LibraryOur Halogen-Enriched Fragment Library comprises 708 brominated fragments that can explore binding sites for favorable halogen bond interactions to identify unique binding modes that are complementary to those obtained from classical fragment-based screening.
 

Read more...
 
Chelator Fragment Library

Chelator Fragments LibraryFragment-based lead design (FBLD) could be used to identify new metal-binding groups for metalloenzyme inhibitors. Several small-molecule chelators have been shown to effectively inhibit metalloproteins, therefore the design,

Read more...
 
«StartPrev1234NextEnd»

SSL