Ligands organométalliques

AR-R 17779 is a selective agonist for α7 nicotinic acetylcholine receptors (nAChRs) (Ki value = 190 nM for rat α7 receptor). This compound has use as a tool to study the function of α7 nicotinic receptors. One such study revealed a role for α7 nicotinic receptors in nicotine-mediated excitatory effects on hippocampal learning and memory. AR-R17779 reduces formation of atherosclerotic plaques and abdominal aortic aneurysms in apolipoprotein E-deficient mice.

DNA alkylating agent; highly potent metabolite of nemorubicin

Inhibits JAK1 and JAK2 kinases

Potent inverse agonist of peroxisome proliferator-activated receptor PPARβ and PPARδ with IC50 value of 27 nM. In mouse myoblasts, DG 172 enhanced recruitment of transcriptional corepressor and down-regulated transcription of PPARβ/δ target gene Angptl4. DG 172 also possess a PPARβ/δ-independent activity on bone marrow cells and promotes dendritic cell differentiation.

Receptor tyrosine kinase inhibitor; anti-angiogenesis; anti-oncogenesis

L-type calcium channel blocker

Synthetic antineoplastic agent

Inhibits DNA topoisomerase II; antineoplastic; immunomodulatory; antimicrobial

Sorafenib is a drug that belongs to the class of multikinase inhibitors. It inhibits a number of kinases, including the Mcl-1 protein, which is involved in apoptosis along with blocking picolinic acid (PA), an endogenous metabolite involved in apoptosis signal transduction. Sorafenib also binds to epidermal growth factor receptor (EGFR) on the surface of cancer cells, inhibiting the production of proteins that are required for angiogenesis, thus blocking the formation of new blood vessels. Sorafenib may also inhibit P-glycoprotein (Pgp) activity. Overall, these cytotoxic effects give Sorafenib anti-tumor properties, inhibiting angiogenesis and cellular transformation, which are the two main processes of tumor growth and metastasis. Sorafenib has been shown to be effective against a range of solid tumors such as breast, prostate and lung cancers and is also used for the treatment of metastatic colorectal cancer and renal cell carcinoma. A combination therapy group found that sorafenib was more effective when used with interferon alfa-2b for the treatment of advanced renal cell carcinoma. Sorafenib also has the potential for drug interactions with other drugs that are metabolized by cytochrome P450 enzymes. Sorafenib 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.

Padsevonil is an investigational antiseizure medication, which is a synthetic pharmaceutical compound. It is derived from extensive medicinal chemistry research aiming to address complex seizure disorders resistant to conventional treatments. Padsevonil functions by exhibiting a dual mechanism of action. It binds to synaptic vesicle protein 2A (SV2A) with high affinity, similar to levetiracetam but with additional modulation of the benzodiazepine-sensitive gamma-aminobutyric acid-A (GABA-A) receptor. This combined activity potentiates its efficacy in stabilizing neuronal hyperactivity and dampening excitatory neurotransmission, providing a novel angle to tackle refractory seizures.

Sparteine hydroiodide is the salt form of sparteine. This compound acts as an inhibitor of voltage-gated sodium channels. In organic chemisty, it is used for chiral synthesis.

Cyamemazine is a neuroleptic medication, which is a member of the phenothiazine class of compounds. It is synthesized from derivatives of phenothiazine, a group of agents primarily found in pharmaceuticals. The mode of action of cyamemazine involves antagonism at dopamine D2 receptors in the central nervous system. This inhibition of dopamine activity is the principal mechanism through which it exerts its antipsychotic effects. Due to its receptor activity, cyamemazine is used primarily in the management of various psychotic disorders, including schizophrenia and acute psychoses. It also exhibits anxiolytic properties, making it effective in treating anxiety associated with these conditions. By modulating neurotransmitter pathways, cyamemazine helps to alleviate symptoms such as hallucinations, delusions, and agitation, offering therapeutic benefit in complex neuropsychiatric cases. As an atypical antipsychotic, it provides an option for patients who may not respond adequately to other treatments. Although primarily used in a clinical setting, ongoing research continues to investigate potential wider applications and efficacy in treating other mental health issues.

Partial inverse agonist of benzodiazepine sites of the GABAA receptors with anxiogenic properties. FG 7142 is a pharmacological stressor which generates anxiety in humans and in experimental animals such as rhesus monkeys and rodents. FG 7142 also reduces food intake and frequency of feeding in male and female rats.

Selective and potent inhibitor of glucose transporter GLUT1 with IC50 of 2 nM. The compound limits glucose uptake and is able to block basal as well as stress-regulated glycolysis in ovarian cancer cells. It supresses proliferation, viability and tumorigenicity of ovarian cancer cells.