Histrelin acetate_product_DataBase

Bioactivity

Histrelin acetate, a GnRH analogue, is a GnRH Receptor agonist. Histrelin acetate increases serum luteinising hormone (LH), follicle stimulating hormone (FSH) and testosterone levels. Histrelin acetate can be used in the research of prostate cancer, endometriosis[1][2][5].

Invitro

Histrelin (10-100 nM) acetate 刺激离体大鼠下丘脑-神经垂体外植体释放加压素 (VP)[4]。Histrelin (100 nM) acetate 刺激大鼠下丘脑-神经垂体系统释放催产素 (OT)[5]。

In Vivo

Histrelin (0.1 mg/kg，皮下注射) acetate 可恢复 Csfmop/Csfmop 小鼠[2]中的循环 LH 浓度。Histrelin （10,30 或 100 μg/天，皮下注射) acetate 会减少兔子的子宫内膜腺体数量并使间质萎缩[3]。

Name

Histrelin acetate

CAS

220810-26-4

Sequence

{Pyr}-His-Trp-Ser-Tyr-{d-His(Bzl)}-Leu-Arg-Pro-{NHEt}

Shortening

{Pyr}-HWSY-{d-His(Bzl)}-LRP-{NHEt}

Formula

C66H86N18O12.xC2H4O2

Molar Mass

1323.50 (free base)

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture and light

Powder	-80°C	2 years
	-20°C	1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Reference

[1]. Emma D Deeks, et al. Histrelin: in advanced prostate cancer. Drugs. 2010 Mar 26;70(5):623-30. [2]. Marlena Juszczak, et al. Hypothalamic gonadotropin-releasing hormone receptor activation stimulates oxytocin release from the rat hypothalamo-neurohypophysial system while melatonin inhibits this process. Brain Res Bull. 2010 Jan 15;81(1):185-90. [3]. P E Cohen, et al. Colony-stimulating factor-1 plays a major role in the development of reproductive function in male mice. Mol Endocrinol. 1997 Oct;11(11):1636-50. [4]. D W Hahn, et al. Development of an animal model for quantitatively evaluating effects of drugs on endometriosis. Fertil Steril. 1985 Sep;44(3):410-5. [5]. E Boczek-Leszczyk, et al. Vasopressin release from the rat hypothalamo-neurohypophysial system: effects of gonadotrophin-releasing hormone (GnRH), its analogues and melatonin. J Physiol Pharmacol. 2010 Aug;61(4):459-66.

PeptideDB

Histrelin acetate

CAS: 220810-26-4 F: C66H86N18O12.xC2H4O2 W: 1323.50 (free base)