Organometallic Ligands

Angiotensin II receptor antagonist

Pan-class I phosphatidylinositide 3-kinase (PI3K) inhibitor (IC50 = 3, 33, 3 and 75 nM at catalytic subunits p110α, p110β, p110δ and p110γ respectively). Inhibits proliferation in several cancer cell lines, such as glioblastoma, breast and prostate cancer cells. Has synergistic anti-cancer effect in combination with MEK/ERK kinase inhibitor GDC-0973 (cobimetinib).

Regaloside D is a natural product derived from plant sources, specifically isolated from certain species known for their bioactive properties. It functions as a glycoside, a compound in which a sugar is bound to a non-carbohydrate moiety, potentially influencing a variety of cellular processes through its interaction with specific molecular targets.

Roflumilast is a selective phosphodiesterase-4 inhibitor that is used for the treatment of exacerbations in patients with chronic obstructive pulmonary disease (COPD). It is also used to treat plaque psoriasis. This drug has anti-inflammatory and immunomodulatory effects as it aids in increasing levels of cAMP.

A brain-penetrant inhibitor of leucin-rich repeat kinase 2 (LRRK2) with IC50 = 0.76 nM and anti-parkinsonian activity. Gain-of-function mutations in LRRK2 gene lead to increased familial and idiopathic risk of developing the disease. The inhibitors of the kinase activity have therapeutic potential against Parkinson’s disease.

AZD9567 is a selective glucocorticoid receptor modulator (SGRM), which is a synthetic pharmaceutical compound. Its source is rooted in medicinal chemistry efforts to design ligands that selectively interact with glucocorticoid receptors. The mode of action of AZD9567 involves binding to glucocorticoid receptors with high specificity, modulating their activity to trigger anti-inflammatory and immunomodulatory responses while minimizing common side effects associated with traditional glucocorticoids.

alpha-adrenoceptor agonist; nasal decongestant

As a synthetic trifluorinated glucocorticoid receptor agonist, Fluticasone exhibits anti-inflammatory properties. When binding to and activating glucocorticoid receptors, Fluticasone initiates the activation of lipocortin which inhibits cytosolic phospholipase A2. Consequently, the cascade of inflammatory mediator synthesis reactions are inactivated and the production of inflammatory cells namely mast cells, dendritic cells, macrophages and eosinophils and the cytokines that they produce are greatly reduced.It is this anti-inflammatory role which has enabled Fluticasone to successfully treat conditions such as asthma, emphysema, allergic rhinitis and atopic dermatitis. It has also been seen to increase anti-inflammatory effects of annexoin-1 and mitogen-activated kinase phosphatase-1; reduce mucus gland secretions and increase the number of beta-2 receptors on smooth muscles of the airways.
Fluticasone 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.

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.

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.

γ-secretase inhibitor; inhibits notch signaling

Selective TRPM8 channel blocker. Inhibits icillin-induced store-operated Ca2+ entry, hence TRPM8 activation, in pulmonary vasculature. Reduces frequency of volume-induced contraction of bladder. Reduces micturition and nociceptive reflex actions in the bladder, suggesting therapeutic potential for bladder hypersensitivity disorders.

Histamine (H2) receptor antagonist