An alkaloid with diverse biological activities; an inhibitor of Nav1.7 (IC50= 47.2 µM) and hERG (IC50 = 43.7 µM); increases the latent period of coughs

Peimine – 50 mg

Brand:
Cayman
CAS:
23496-41-5
Storage:
-20
UN-No:
Non-Hazardous - /

Peimine is an alkaloid that has been found in Fritillaria and has diverse biological activities, including ion channel inhibitory, anti-tussive, anticancer, and anti-inflammatory properties.{53420,56003,56004,56005,56006} It is an inhibitor of voltage-gated sodium channel 1.7 (Nav1.7; IC50= 47.2 µM) and human-ether-a-go-go (hERG), also known as Kv11.1 (IC50 = 43.7 µM).{56003,56004} It increases the latent period of coughs, decreases the number of coughs, and has expectorant activity in a mouse model of ammonia liquor-induced cough when administered at a dose of 3 mg/kg.{53420} Peimine (2.5, 5, and 10 µM) inhibits the growth of DU145, LNCaP, and PC3 prostate cancer, but not RWPE-1 non-cancerous, cells.{56005} It also induces phosphorylation of calcium/calmodulin-dependent protein kinase II (CaMKII) in, and apoptosis of, PC3 cells and inhibits PC3 cell invasion, migration, and epithelial-to-mesenchymal transition. Peimine (10, 20, or 50 mg/animal) reduces tumor growth in a PC3 mouse xenograft model. It decreases IL-1β-induced nitric oxide (NO) and prostaglandin E2 (PGE2; Item No. 14010) production and reduces inducible NO synthase (iNOS) and COX-2 protein levels in primary mouse articular chondrocytes in vitro.{56006} It also decreases the severity of osteoarthritis-associated histopathological alterations in a mouse model of osteoarthritis when administered at a dose of 20 mg/kg.  

 

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Description

An alkaloid with diverse biological activities; an inhibitor of Nav1.7 (IC50= 47.2 µM) and hERG (IC50 = 43.7 µM); increases the latent period of coughs, decreases the number of coughs, and has expectorant activity in a mouse model of ammonia liquor-induced cough at 3 mg/kg; inhibits the growth of DU145, LNCaP, and PC3 prostate cancer, but not RWPE-1 non-cancerous, cells at 2.5, 5, and 10 µM; reduces tumor growth in a PC3 mouse xenograft model at 10, 20, or 50 mg/animal; decreases severity of osteoarthritis-associated histopathological alterations in a mouse model of osteoarthritis at 20 mg/kg

Formal name: (5α)-cevane-3β,6α,20-triol

Synonyms: 

Molecular weight: 431.7

CAS: 23496-41-5

Purity: ≥98%

Formulation: A crystalline solid

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