Fertirelin

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Chemical Structure| 38234-21-8 同义名 : -
CAS号 : 38234-21-8
货号 : A273550
分子式 : C55H76N16O12
纯度 : 99%
分子量 : 1153.29
MDL号 : MFCD00133495
存储条件:

Pure form Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(91.04 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 100 mg/mL(86.71 mM),配合低频超声助溶

动物实验配方:
生物活性
描述 Gonadotropin-releasing-hormone (GnRH) analogues are synthetic compounds derived from decapeptide neurohormones (LHRH; LH/FSH-RH). They have a key role in hormone dependent cancer, particularly breast and prostate cancer(i.e. ovariectomy and orchiectomy), providing an androgen and estrogen ablation. GnRH exert an inhibitory action on the growth of hormone-dependent human and canine mammary tumor[3]. The GnRH receptor rather interacts with the mitogenic signal transduction of growth-factor receptors and related oncogene products associated with tyrosine kinase activity via activation of a phosphotyrosine phosphatase resulting in downregulation of cancer cell proliferation[4]. GnRH analogues counteract the proliferating effects of both epidermal growth factor (EGF) and insulin like growth factor (IGF-I); additionally, it affects the mitogen-activated protein kinase (MAPK) cascade and modulates the activity of the urokinase-type plasminogen activator (uPA)/plasminogen activator inhibitory (PAI) system, which is involved in the process of metastasis[5]. Fertirelin, an analog of GnRH 2.5 to 10 times more potent than native GnRH, has become the treatment of choice for reversing follicular cysts[6]. Administration of high doses of Fertirelin is found to reduce superovulatory responses[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

0.87mL

0.17mL

0.09mL

4.34mL

0.87mL

0.43mL

8.67mL

1.73mL

0.87mL

参考文献

[1]Yamada K, Nakao T, et al. Influence of GnRH analogue (fertirelin acetate) doses on synchronization of ovulation and fixed-time artificial insemination in lactating dairy cows. Anim Reprod Sci. 2002 Nov 15;74(1-2):27-34.

[2]Nakao T, Harada A, et al. Effect of fenprostalene 14 days after fertirelin treatment on intervals from treatment to conception in cows with follicular cysts diagnosed by milk progesterone test. J Vet Med Sci. 1993 Apr;55(2):207-10.

[3]Salvatore Florio,et al. GnRH and steroids in cancer. Front Biosci. 2002 Jun 1;7:d1590-608.

[4]Carsten Gründker,et al. Role of gonadotropin-releasing hormone (GnRH) in ovarian cancer. Reprod Biol Endocrinol. 2003 Oct 7;1:65.

[5]A Rizzo,et al. The pharmacological pathways of GnRH mediating the inhibition of mammary tumours: implications in humans and domestic animals. Curr Med Chem.2012;19(7):982-91.

[6]Nakao T et al. Effect of fenprostalene 14 days after fertirelin treatment on intervals from treatment to conception in cows with follicular cysts diagnosed by milk progesterone test. J Vet Med Sci. 1993 Apr;55(2):207-10.

[7] Nariai K, et al. Optimum dose of LH-RH analogue Fertirelin Acetate for the induction of superovulation in mice. Exp Anim. 2005 Jan;54(1):97-9.