Vantas Chemical Properties

storage temp. 

Store at -20°C

solubility 

DMF: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 0.25 mg/ml; PBS (pH 7.2): 10 mg/ml

form 

A crystalline solid

Vantas Usage And Synthesis

Description

Histrelin is a synthetic gonadotropin-releasing hormone (GNRH) agonist that binds to the GNRH receptor (GNRHR; K_i = 0.2 nM in CHO cells expressing the human receptor). It stimulates release of oxytocin and vasopressin ex vivo from the isolated rat hypothalamo-neurohypophysial system at a concentration of 100 nM. In vivo, the initial dose of histrelin (100 μg) stimulates acute increases in luteinizing hormone (LH), follicle-stimulating hormone (FSH), and testosterone serum levels (50-, 2.5-, and 15-fold, respectively), while chronic treatment leads to 95% decreases in LH and FSH responses in rhesus monkeys. Formulations containing histrelin have been used in the treatment of advanced prostate cancer and central precocious puberty.

Definition

ChEBI: An acetate salt obtained by combining histrelin with acetic acid. The amount of acetic acid present can vary and a variable amount of water may be present. Histrelin acetate is used as a subcutaneous hydrogel implant for the treatment of prostate cancer an for the suppression of gonadal sex hormone production in children with central precocious puberty.

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