Organometallic Ligands

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.

NMDA glutamate receptor antagonist; anti-depressant

Tolvaptan is a vasopressin receptor antagonist. It binds to the V2 receptor in the cytosol and prevents it from activating the aquaporin 2 channel, which regulates water permeability. Inhibition of vasopressin receptors in the kidneys improves fluid and electrolyte balance. Tolvaptan has been shown to be effective for treating congestive heart failure, as well as other disorders that are associated with fluid retention, such as renal dysfunction and metabolic syndrome. Tolvaptan can also be used in combination therapy with other drugs to treat these conditions.

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.

Androgen receptor antagonist; therapy for endometriosis

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.

(±)-Vasicine is an alkaloid compound, which is a naturally occurring, organic molecule found primarily in the plant Adhatoda vasica. This alkaloid is extracted from the leaves of the plant, which is native to parts of Asia, particularly India and Pakistan. (±)-Vasicine is known for its bronchodilatory and respiratory stimulant activities.

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 PDE4 enzyme

Neu5Ac[1Me,4789Ac]a(2-3)Gal[246Bz]-b-MP is a synthetic glycan, which is a complex carbohydrate molecule modeled after naturally occurring glycoconjugates. This product is derived through chemical synthesis in the laboratory, allowing precise control over its structure and functional groups. It consists of sialic acid (Neu5Ac) linked to galactose (Gal), with several protective acetyl (Ac) and benzyl (Bz) groups that confer stability during synthesis and ensure high specificity in its interactions.

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.

CXCR2 antagonist