Proteínas

Androgen receptor antagonist

Acitretin is a synthetic retinoid that can be used to treat skin conditions such as acne, psoriasis, and eosinophilic fasciitis. It has been shown to be an active inhibitor of squamous cell carcinoma in the laboratory. Acitretin works by inhibiting the excessive cell growth and keratinisation seen in psoriasis therefore reducing the thickening of the skin, plaque formation and scaling.

LGD 3303 is an investigational selective androgen receptor modulator (SARM), which is a compound designed to selectively interact with androgen receptors in the body. SARMs like LGD 3303 are researched for their potential to mimic anabolic activity with reduced androgenic effects compared to traditional anabolic steroids. LGD 3303 acts by binding to androgen receptors, and it is believed to promote muscle growth and bone health without significantly affecting other tissues.

Full antagonist to the estrogen beta receptor (ERβ) with 36-fold selectivity for the β over α receptor. ERβ is a tumour suppressor and PHTPP is a useful tool to study the biology of estrogen-dependent tumours.

Estrogen receptor degrader; therapeutic use in breast cancer

Endogenous non-toxic agonist of the aryl hydrocarbon receptor (AhR) with immunosuppressive activity. The compound also inhibits the nuclear translocation of Smad2/3/4 leading to aberrant Transforming Growth Factor-β1 (TGFβ1) signaling. It inhibits myofibroblast differentiation and is a potential anti-scarring agent.

PPARα transcription factor agonist

Pioglitazone is a thiazolidinedione drug that is used in combination with diet change and exercise to treat glycemic levels in patients with type 2 diabetes mellitus. This drug is an agonist of peroxisome proliferator-activated receptor-gamma and increases glucose uptake. In animal studies, Pioglitazone has shown to have anti-inflammatory properties.

Ciprofibrate is a fibrate drug that is used as a lipid-lowering agent. This drug reduces both LDL and VLDL cholesterol levels in the blood. Ciprofibrate works by reducing the production of triglycerides in the liver and increasing the removal of triglycerides from the blood. This drug is an agonist of peroxisome proliferator-activated receptor alpha.

Rho/MRTF/SRF mediated gene transcription inhibitor

Inhibitor of HIF1-α transcription factor and repressor of HIF1-α-regulated genes in adult and embryonic stem cell models as well as in tumoral cell lines. FM19G11 inhibits the expression of undifferentiating factors Oct4, Sox2, Nanog, and Tgf-α at transcriptional and protein level. FM 19G11 affects also epigenetic events by reducing histone acetylation and leading to repression of p300, a HIF-transcription activation co-factor.

Spironolactone is an aldosterone receptor antagonist that is used to treat hypertension, heart failure and edema. This drug binds to mineralocorticoid receptors and acts as an aldosterone antagonist. Spironolactone promotes sodium and water excretion and potassium retention. It also activates pro-inflammatory pathways.

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.

Androgen receptor antagonist; therapy for endometriosis

PPARγ antagonist

Eplerenone is a drug known as an aldosterone antagonist. It is a type of potassium-sparing diuretic that is used to treat chronic heart failure and high blood pressure, particularly for patients with resistant hypertension due to elevated aldosterone. It does this by blocking the activity of the enzyme that produces aldosterone, which increases levels of sodium and water in the body. This leads to a decrease in blood pressure.

Glucocorticoid; anti-inflammatory; anti-asthmatic agent

Bexarotene is a retinoid and antineoplastic agent that is used for the treatment of solid tumours and t-cell lymphomas. It inhibits the growth in vitro of some tumor cell lines of hematopoietic and squamous cell origin and research has shown that it induces tumor regression in vivo in some animal models.