Protéine de transport membranaire

Dothiepin is a tricyclic antidepressant used to treat depression in patients who are not responding to alternative therapies. This drug inhibits the reuptake of norepinephrine and serotonin, increasing available neurotransmitter levels at the synaptic cleft. It also exhibits anticholinergic, antihistamine and central sedative properties.

Lofepramine is a psychoactive drug that belongs to the class of tricyclic antidepressants. It is used to treat depression and anxiety disorders. This drug works by inhibiting the reuptake of neurotransmitters such as serotonin and norepinephrine and as a result these neurotransmitters remain active in the brain for a longer period, which can help improve mood and alleviate symptoms of depression.

Inhibits P-gp transporters ; modulates P-gp-mediated multidrug resistance

GABA reuptake inhibitor

Inhibits urate anion exchanger 1 (URAT1); therapeutic use in gout

Inhibitor of sulphonylurea receptor SUR1; hypoglycemic agent

Inhibitor of sodium-glucose cotransporter SGLT2

Rabeprazole is a proton pump inhibitor drug that is used to treat symptoms of GERD, heal gastrointestinal ulcers and eradicate Helicobacter pylori. This antiulcer drug suppresses gastric acid by inhibiting the gastric H+/K+ ATPase at the parietal cell.

AZD3965 is a potent, selective and orally available monocarboxylate transporter 1 (MCT1) inhibitor with binding affinity of 1.6 nM, 6-fold selective for MTC1 over MCT2.

Serotonin uptake inhibitor; anti-depressant

A serotonin reuptake inhibitor with anticholinergic activity and mild inhibitory activity on noradrenaline reuptake. Paroxetine has been used for the treatment of depression, anxiety disorders, post-traumatic stress disorder, premenstrual dysphoric disorder and obsessive-compulsive disorder.  Also inhibits nitric oxide synthase and cytochrome isoenzyme P450 2D6.

Inhibitor of lactate uptake and efflux via monocarboxylate transporter MCT1. The blockade of lactate transport with BAY 8002 leads to accumulation of lactate and pyruvate in cells. The MCT1 inhibition decreased tumour growth most effectively in diffuse large B-cell lymphoma cell lines and in subsets of solid tumour models.

Maprotiline is a tetracyclic antidepressant that is used for the treatment of major depressive disorder and anxiety that is associated with depression. This drug inhibits noradrenaline reuptake and has anticholinergic properties. Additionally, Maprotiline inhibits the amine transporter which allows for a delay in the reuptake of noradrenaline.

Inhibitor of CETP exchange protein

Inhibits protein translocation from ER to Golgi; fungal metabolite

Inhibitor of CETP exchange protein

Fluvoxamine is a selective serotonin reuptake inhibitor that is used in the treatment of depression and obsessive-compulsive disorder. It blocks the reuptake of serotonin, enhancing its effects.

Potent inhibitor of the sodium-coupled citrate cotransporter SLC13A5 (NaCT, INDY). The compound is not structurally related to citrate and is selective for SLC13A over other related transporters.

Amitryptylline is a tricyclic antidepressant that is used to treat depression and to relieve depression associated anxiety. Although its mechanism is not fully understood, it is suggested that this drug inhibits norepinephrine and serotonin thus increasing their concentrations at the synaptic clefts. Additionally, Amitryptylline has shown to have anticholinergic properties.

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.

Furosemide is a potent loop diuretic that is used in the treatment of hypertension, liver cirrhosis, renal disease and heart failure. This drug acts on the kidney to increase water loss from the body. It inhibits electrolyte reabsorption. Furosemide also exerts vasodilatory effects.

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.

Clomipramine is a tricyclic antidepressant drug that inhibits the reuptake of serotonin, norepinephrine, and dopamine. It is used to treat obsessive compulsive disorder, panic disorders and cataplexy. Additionally, Clomipramine is shown to modulate immune activation and shows constant anti-inflammatory properties at therapeutic concentrations by consistently decreasing pro-inflammatory cytokines.

Elacridar is an inhibitor of ATP-dependent transport, which is mediated by P-glycoprotein (P-gp). Functioning as an oral bioenhancer, Elacridar addresses multiple drug resistance in tumors, a common challenge in cancer treatment often linked to changes in the expression of protein inhibitors. Inhibition of P-gp by Elacridar is a key mechanism behind its effectiveness. P-glycoprotein, a well-characterized human ABC transporter of the MDR/TAP subfamily, acts as an ATP-dependent efflux pump with broad substrate specificity. Its increased expression in the intestines can hinder drug absorption, leading to reduced bioavailability and inadequate therapeutic plasma concentrations. Elacridar addresses this challenge by inhibiting P-gp, thereby increasing the bioavailability of coadministered drugs. Overall, Elacridar emerges as a promising option for the treatment of solid tumors, offering a strategic approach to overcoming multidrug resistance in cancer therapy.

P-glycoprotein (MDR1) inhibitor; non-immunosuppressive cyclosporin A analog

Methyl-d3-magnesium iodide solution, 1.0 M in diethyl ether, is a specialized organometallic reagent used extensively in synthetic chemistry. This compound is a labeled Grignard reagent, where the methyl group is fully deuterated. It is sourced through the synthesis involving the reaction of deuterated methyl iodide with magnesium in an anhydrous diethyl ether solvent.

Potent P-glycoprotein (P-gp) inhibitor

A potent inhibitor of CETP that inhibits transfer of cholesteryl esters and triglycerides. Raises HDL cholesterol levels whilst lowering LDL cholesterol. Reduces cardiovascular events in patients with atherosclerotic vascular disease that receive statin treatment.