Organometallic Ligands

Nilutamide is an antineoplastic agent that is used to treat prostate cancer. This drug is an androgen receptor antagonist and binds with androgen receptors thus blocking its action and resulting in growth arrest.

Fluvastatin is a statin that lowers blood cholesterol and triglycerides by inhibiting HMG-CoA reductase, an enzyme that plays a critical role in the synthesis of cholesterol. Fluvastatin has also been shown to reduce the incidence of myocardial infarction, and to reduce atherosclerotic lesions in animal models, reducing the incidence of cardiovascular disease. Fluvastatin also has been shown to inhibit the activation of toll-like receptor 4 (TLR4) by lipopolysaccharide (LPS), which may be related to its anti-inflammatory effects. Furthermore, through lowering blood cholesterol, Fluvastatin also inhibits tubulointerstitial injury and prevents renal damage caused by high concentrations of the lipid.

GC 376 is an inhibitor of the main protease Mpro (3CLpro) in coronaviruses as well as picornaviruses. This broad-spectrum antiviral compound has been used as investigational veterinary drug for treatment of feline infectious peritonitis virus (FIPV) infections. Recent studies also showed that GC 376 inhibits the main protease Mpro (3CLpro) from SARS-CoV-2 with IC50 of 0.03 μM and EC50 of 3.37 μM.

Polmacoxib is a non-steroidal anti-inflammatory drug (NSAID), which is derived through synthetic chemical processes. It functions as a selective cyclooxygenase-2 (COX-2) inhibitor. By selectively inhibiting the COX-2 enzyme, polmacoxib reduces the conversion of arachidonic acid to prostaglandins that mediate inflammation and pain, while sparing the COX-1 enzyme that protects gastric mucosa and maintains platelet function.

Selective antagonist of the serotonin receptors 5-HT2A with subnanomolar affinity. The compound has clozapine-like anti-psychotic properties and more favourable CNS safety profile than traditional anti-psychotics. MDL 100907 has been used in studies on antisocial behaviour in mice and shown that the blockage of 5-HT2A receptors leads to decreased post-traumatic aggression and bradycardia.

Pitolisant is a selective histamine H3 receptor inverse agonist, originating from chemical research into histaminergic pathways. It works by binding to histamine H3 receptors in the brain, functioning primarily as an antagonist/inverse agonist. This action leads to increased release of neurotransmitters such as histamine, acetylcholine, and norepinephrine, which play crucial roles in wakefulness and attention.

SR 4835 is a synthetic compound, which is an advanced molecular entity derived from extensive medicinal chemistry efforts. This compound exhibits a novel mechanism of action, targeting specific cellular pathways implicated in disease processes. SR 4835 functions by modulating enzyme activity, thus influencing intracellular signaling cascades that play a critical role in pathophysiological conditions.

Pitolisant is an inverse agonist and antagonist of the histamine (H3) receptor. It acts as an allosteric modulator of the H3 receptor to increase the activity of histamine at the M1 receptor. Pitolisant has been used in the treatment of narcolepsy, schizophrenia and Alzheimer's disease. Its mechanism of action involves binding to the amide group on histamine, which increases its affinity for the H3 receptor and enhances its activity at this site. Pitolisant has been shown to improve cognitive ability and reduce fatigue in patients with Alzheimer's disease.

Nilotinib is a kinase inhibitor that is used for the treatment of Chronic Myeloid Leukemia (CML). This drug is also used for the treatment of CML that is resistant to imatinib. Nilotinib inhibits the tyrosine kinase activity of the BCR-ABL protein. It also inhibits PDGFR and c-kit.

Levetiracetam is a modulates the activity of the synaptic vesicle protein 2A (SV2A) in the brain and is used to treat epilepsy.It is not clear exactly how Levetiracetam affects the activity of SV2A and if this is through inhibiting the release of neurotransmitters. However, it is thought to work by binding to a specific site on SV2A, which interferes with its normal function and ultimately leads to changes in exocytosis. One of the postulated mechanisms of action is that this modulates glutamate release. Levetiracetam is used to treat certain types of seizures in people with epilepsy.
Levetiracetam is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready-to-use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.

ERKtide Substrate Peptide.

H-FERQHM-OH peptide, corresponding to RNase A 8-13 (Chain A of bovine pancreatic ribonuclease) is a non-amyloidogenic peptide, that can be used as a negative control in amyloid formation experiments together with CRB1001320.

Candesartan is a drug that belongs to the class of angiotensin II receptor antagonists and is used to treat hypertension. It is used in combination therapy with other drugs, such as hydrochlorothiazide and amlodipine, to lower blood pressure. Candesartan inhibits the formation of angiotensin II, the receptor which causes vasoconstriction and increased blood pressure.

Inhibitor of HMG-CoA reductase

Proprotein convertase subtilisin/kexin type 9 (PCSK9) is negative regulator of hepatic low-density lipoprotein (LDL) receptors by promoting their degradation. This leads to an increase in plasma levels of cholesterol-LDL (LDL-c). PCSK9 binds to the LDL receptor at the epidermal growth factor precursor homology domain A (EGF-A) which leads the receptor to be targeted for degradation. Natural loss of function mutations in PCSK9 have been linked to improved coronary health and lower cholesterol levels with reduced risk of coronary heart disease. This has led to further study to find inhibitors of PCSK9 with the hope that they may be clinically relevant in the future.As discussed, PCSK9 binds to EGF-A on the LDL receptor. A peptide named pep 2-8 is a mimic of EGF-A and binds PCSK9 in the same manner observed with the LDL receptor. Pep 2-8 is a potent selective competitive inhibitor of PCSK9. Pep 2-8 restores LDL receptor function and LDL uptake of PCSK9-treated HepG2 cells. This is still an active area of research to optimise inhibition of PCSK9 for cholesterol regulation.Pep 2-8 has also been utilised as an anchor peptide in phage-display experiments to bind an extension peptide library to the groove site.Peptide Ac-TVFTSWEEYLDWV-NH2 is a Research Peptide with significant interest within the field academic and medical research. This peptide is available for purchase at Cymit Quimica in multiple sizes and with a specification of your choice.

Riluzole is a glutamate antagonist that is used for the treatment of amyotrophic lateral sclerosis. This drug is also used as an anticonvulsant. Although a complete mechanism of action is unknown, it has an inhibitory effect on glutamate release and it inactivates voltage dependent sodium channels.

Vinpocetin or Vinpocetine is a synthetic derivative of a vinca alkaloid that is used to treat symptoms of cerebrovascular diseases such as stroke and dementia. It blocks sodium channels, reduces cellular calcium influx and has shown to have antioxidant activity. Studies have also suggested that vinpocetin can inhibit phosphodiesterase- 1 (PDE-1) in isolated rabbit aorta.

A chemical probe for the dual bromodomains of human transcription-initiation-factor TFIID subunit 1 (TAF1). GNE 371 binds TAF1 with an IC50 of 10 nM and is selective over other bromodomain family members. Exerts anti-proliferative effects in synergy with BET inhibitor JQ1.

Potent agonist of a1β1γ1 5′-adenosine monophosphate-activated protein kinase (AMPK). It binds to the allosteric drug and metabolite (ADaM) site at the α- and β- subunit interface of AMPK. It has potential for the treatment of diabetic nephropathy. PF 06409577 reduces infections caused by flaviviruses, mediated by changes in the metabolism of lipids in host cells.