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Abarelix(acetate)
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Abarelix(acetate)图片
CAS NO:785804-17-3
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
A synthetic GnRHR antagonist
Cas No.785804-17-3
别名阿巴瑞克乙酸盐; PPI 149 Acetate; R 3827 Acetate
Canonical SMILESCC(N[C@H](CC1=CC(C=CC=C2)=C2C=C1)C(N[C@H](CC3=CC=C(Cl)C=C3)C(N[C@H](CC4=CC=CN=C4)C(N[C@@H](CO)C(N(C)[C@@H](CC5=CC=C(O)C=C5)C(N[C@H](CC(N)=O)C(N[C@@H](CC(C)C)C(N[C@@H](CCCCNC(C)C)C(N6CCC[C@H]6C(N[C@H](C)C(N)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O.OC(C)=O
分子式C72H95ClN14O14.XC2H4O2
分子量1416.1
溶解度DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml,PBS (pH 7.2): 5 mg/ml
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Abarelix is a synthetic third generation gonadotropin-releasing hormone receptor (GnRHR) antagonist (IC50 = 3.5 nM in HEK293 cells expressing the human receptor).1,2 It increases histamine release from rat peritoneal mast cells in vitro and from a human skin model ex vivo.3,4 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.3 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.

|1. Tan, O., and Bukulmez, O. Biochemistry, molecular biology and cell biology of gonadotropin-releasing hormone antagonists. Curr. Opin. Obstet. Gynecol. 23(4), 238-244 (2011).|2. Jiang, G., Stalewski, J., Galyean, R., et al. GnRH antagonists: A new generation of long acting analogues incorporating p-ureido-phenylalanines at positions 5 and 6. J. Med. Chem. 44(3), 453-467 (2001).|3. Broqua, P., Riviere, P.J.-M., Conn, P.M., et al. Pharmacological profile of a new, potent, and long-acting gonadotropin-releasing hormone antagonist: Degarelix. J. Pharmacol. Exp. Ther. 301(1), 95-102 (2002).|4. Koechling, W., Hjortkjaer, R., and TankÓ, L.B. Degarelix, a novel GnRH antagonist, causes minimal histamine release compared with cetrorelix, abarelix and ganirelix in an ex vivo model of human skin samples. Br. J. Clin. Pharmacol. 70(4), 580-587 (2010).