Piperidine Alkaloids

Kifunensine, a potent and selective inhibitor of class I α-mannosidases isolated from Actinomycete, prevents α-mannosidases I from trimming mannose residues on glycoproteins. Kifunensine inhibits ERAD.

Minoxidil (U10858) is an ATP-sensitive potassium (K_ATP) channel opener, a potent oral antihypertensive agent and a peripheral vasodilator that promotes vasodilation also affects hair growth. Minoxidil is also a potent inhibitor of soybean lipoxygenaseare with an IC₅₀ of 20 μM.

Halofuginone (RU-19110), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a K_i of 18.3 nM. Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca²⁺ channels. Halofuginone has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.

Reserpine is an inhibitor of the vesicular monoamine transporter 2 (VMAT2).

Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI).

Halofuginone hydrobromide (RU-19110 hydrobromide), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a K_i of 18.3 nM. Halofuginone hydrobromide is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone hydrobromide is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca²⁺ channels. Halofuginone hydrobromide has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.

Piperine is an alkaloid, can be isolated from pepper. Piperine can inhibit the activity of P-glycoprotein and CYP3A4. Piperine inhibits HeLa cells with an IC₅₀ of 61.94±0.054 μg/mL.

Piperine (Standard) is the analytical standard of Piperine. This product is intended for research and analytical applications. Piperine is an alkaloid, can be isolated from pepper. Piperine can inhibit the activity of P-glycoprotein and CYP3A4. Piperine inhibits HeLa cells with an IC₅₀ of 61.94±0.054 μg/mL.

Solasodine (Standard) is the analytical standard of Solasodine. This product is intended for research and analytical applications. Solasodine (Purapuridine) is a steroidal alkaloid that occurs in plants of the Solanaceae family. Solasodine has neuroprotective, antifungal, hypotensive, anticancer, antiatherosclerotic, antiandrogenic and anti-inflammatory activities.

Xestospongin C ((-)-Xestospongin C) is a selective, reversible inositol 1,4,5-trisphosphate receptor (IP3R) inhibitor. Xestospongin C acts as an inhibitor of the sarcoplasmic/endoplasmic reticulum Ca²⁺ ATPase (SERCA) pump of internal stores. Xestospongin C blocks IP3-induced Ca²⁺ release from cerebellar microsomes with an IC₅₀ of 358 nM. Xestospongin C is a valuable tool for investigating the structure and function of IP3Rs and Ca²⁺ signaling in neuronal and nonneuronal cells.

Oxymatrine, an alkaloid from Sophora flavescens Alt. with anti-inflammatory, antifibrosis, and antitumor effects, inhibits the iNOS expression and TGF-β/Smad pathway. Oxymatrine inhibits bocavirus minute virus of canines (MVC) replication, reduces viral gene expression and decreases apoptosis induced by viral infection.

Raloxifene hydrochloride (Keoxifene hydrochloride) is a second generation selective and orally active estrogen receptor modulator. Raloxifene hydrochloride produces estrogen-agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue.

Sinomenine, an alkaloid extracted from Sinomenium acutum, is a blocker of the NF-κB activation. Sinomenine also is an activator of μ-opioid receptor.

Evodiamine is an alkaloid isolated from the fruit of Evodia rutaecarpa Bentham with diverse biological activities including anti-inflammatory, anti-obesity, and antitumor.

Arecoline, a naturally brain-penetrant and orally active occurring psychoactive alkaloid, is a partial agonist of nicotinic and muscarinic acetylcholine receptor. Arecoline exhibits stimulation, alertness, anxiolysis and anti-parasitic effects. Arecoline also can induce oxidative stress.

Swainsonine (Tridolgosir) is an natural indolizidine alkaloid, a potent and reversible α-mannosidase inhibitor. Swainsonine induces apoptosis and cell cycle arrest at G2/M phase. Swainsonine shows anti-tumor activity.

Sinomenine hydrochloride (Cucoline hydrochloride), an alkaloid extracted from Sinomenium acutum, is a blocker of the NF-κB activation. Sinomenine also is an activator of μ-opioid receptor.

Vinpocetine (Ethyl apovincaminate) is a derivative of the alkaloid Vincamine that blocks voltage-gated Na⁺ channels. The IC₅₀ value of Vinpocetine on direct IKK inhibition in the cell-free system is 17.17 μM. Vinpocetine is a phosphodiesterase (PDE) inhibitor and inhibits NF-κB-dependent inflammatory responses by directly targeting IκB kinase complex (IKK), and has been widely used for the treatment of cerebrovascular disorders.

1-Deoxynojirimycin (Duvoglustat) is a potent and orally active α-glucosidase inhibitor. 1-Deoxynojirimycin suppresses postprandial blood glucose and is widely used for diabetes mellitus. 1-Deoxynojirimycin possesses antihyperglycemic, anti-obesity, and antiviral features.

Aloperine is an alkaloid in sophora plants such as Sophora alopecuroides L, which has shown anti-cancer, anti-inflammatory and anti-virus properties. Aloperine is widely used to treat patients with allergic contact dermatitis eczema and other skin inflammation in China. Aloperine induces apoptosis and autophagy in HL-60 cells.