An α2-AR (EC50s = 1 receptor antagonist; binds to α2A-

Efaroxan (hydrochloride) – 10 mg

Brand:
Cayman
CAS:
89197-00-2
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

Efaroxan is an α2-adrenergic receptor (α2-AR; EC50s = 1 receptor antagonist.{52072} It binds to α2A-, α2B-, and α2C-ARs (Kis = 13, 38, and 1,820 nM, respectively) and selectively to I1 over I2 receptors (Kis = 52 and >10,000 nM, respectively). Efaroxan is an I3 agonist that binds to putative I3 receptors on human pancreatic islets of Langerhans and stimulates insulin secretion when used at a concentration of 100 μM.{52073} It also binds to rat RIN-5AH insulinoma cell membranes (IC50 = 32 nM) and stimulates insulin secretion when used at a concentration of 100 μM.{52074} Efaroxan (5 mg/kg) lowers basal blood glucose levels in mice.{52075} It also increases 3,4-dihydroxyphenylalanine (L-DOPA; Item No. 13248) synthesis in rat cortex and hippocampus by 77 and 57%, respectively, when administered at a dose of 10 mg/kg.{52076}  

 

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SKU: 29008 - 10 mg Category:

Description

An α2-AR (EC50s = 1 receptor antagonist; binds to α2A-, α2B-, and α2C-ARs (Kis = 13, 38, and 1,820 nM, respectively) and selectively to I1 over I2 receptors (Kis = 52 and >10,000 nM, respectively); binds to putative I3 receptors on human pancreatic islets of Langerhans and stimulates insulin secretion at 100 μM; binds to rat RIN-5AH insulinoma cell membranes (IC50g = 32 nM) and stimulates insulin secretion at 100 μM; lowers basal blood glucose levels in mice at 5 mg/kg; increases L-DOPA synthesis in rat cortex and hippocampus by 77 and 57%, respectively at 10 mg/kg

Formal name: 2-(2-ethyl-2,3-dihydro-2-benzofuranyl)-4,5-dihydro-1H-imidazole, monohydrochloride

Synonyms:  (±)-Efaroxan|RX 821037

Molecular weight: 252.7

CAS: 89197-00-2

Purity: ≥98%

Formulation: A solid

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