A synthetic GnRHR antagonist (IC50 = 3.5 nM); decreases plasma LH levels six hours post-treatment in castrated rats

Abarelix (acetate) – 1 mg

Brand:
Cayman
CAS:
785804-17-3
Storage:
-20
UN-No:
Non-Hazardous - /

Abarelix is a synthetic third generation gonadotropin-releasing hormone receptor (GnRHR) antagonist (IC50 = 3.5 nM in HEK293 cells expressing the human receptor).{48583,39553} In vivo, abarelix (200 μg/kg) decreases plasma luteinizing hormone (LH) levels six hours post-treatment in castrated rats, with levels returning to baseline within 24 hours.{48584} Abarelix (2 mg/kg) also transiently decreases plasma testosterone levels in intact rats, with levels returning to baseline within seven days post-treatment. Formulations containing abarelix have previously been used in the treatment of advanced prostate cancer.  

 

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SKU: 28746 - 1 mg Category:

Description

A synthetic GnRHR antagonist (IC50 = 3.5 nM); decreases plasma LH levels six hours post-treatment in castrated rats, with levels returning to baseline within 24 hour at 200 μg/kg; transiently decreases plasma testosterone levels in intact rats, with levels returning to baseline within seven days post-treatment at 2 mg/kg

Formal name: N-acetyl-3-(2-naphthalenyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridinyl)-D-alanyl-L-seryl-N-methyl-L-tyrosyl-D-asparaginyl-L-leucyl-N6-(1-methylethyl)-L-lysyl-L-prolyl-D-alaninamide, acetate salt

Synonyms: 

Molecular weight: 1,416.10

CAS: 785804-17-3

Purity: ≥95%

Formulation: A crystalline solid

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