A synthetic GNRH agonist; binds to GNRHR (Ki = 0.2 nM in CHO cells expressing the human receptor); stimulates oxytocin and vasopressin release ex vivo from the isolated rat hypothalamo-neurohypophysial system (100 nM); initial dose of 100 μg stimulates acute increases in LH

Histrelin (acetate) – 5 mg

Brand:
Cayman
CAS:
220810-26-4
Storage:
-20
UN-No:
Non-Hazardous - /

Histrelin is a synthetic gonadotropin-releasing hormone (GNRH) agonist that binds to the GNRH receptor (GNRHR; Ki = 0.2 nM in CHO cells expressing the human receptor).{36464} It stimulates release of oxytocin (Item No. 11799) and vasopressin ex vivo from the isolated rat hypothalamo-neurohypophysial system at a concentration of 100 nM.{36469,36470} 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.{36471} Formulations containing histrelin have been used in the treatment of advanced prostate cancer and central precocious puberty.  

 

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SKU: 23663 - 5 mg Category:

Description

A synthetic GNRH agonist; binds to GNRHR (Ki = 0.2 nM in CHO cells expressing the human receptor); stimulates oxytocin and vasopressin release ex vivo from the isolated rat hypothalamo-neurohypophysial system (100 nM); initial dose of 100 μg stimulates acute increases in LH, 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

Formal name: 6-[1-(phenylmethyl)-D-histidine]-9-(N-ethyl-L-prolinamide)-1-9-luteinizing hormone-releasing factor (swine), acetate

Synonyms:  [(ImBzl)-d-His6,Pro9-NET]-LHRH|[Des-Gly10,D-His(Bzl)6,Pro-NHEt9]-LHRH|[Des-Gly10,D-His(Bzl)6]-LHRHethyl amide

Molecular weight: 1,323.50

CAS: 220810-26-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Cancer||Research Area|Endocrinology & Metabolism|Hormones & Receptors||Research Area|Endocrinology & Metabolism|Reproductive Biology

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