Ganirelix (acetate) - CAS:129311-55-3

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Ganirelix (acetate) (Synonyms:加尼瑞克;阿扎胆醇;加尼瑞克乙)

目录号 : KCM10951 CAS No. : 129311-55-3 纯度 : ≥98%

Data Sheet 产品使用指南

Ganirelix is a gonadotropin-releasing hormone receptor (GNRHR) antagonist (IC = 3.6 nM; pA = 9.3). It induces a concentration-dependent increase in histamine release from rat peritoneal mast cells in vitro (EC = 11 μg/ml). In vivo, ganirelix (2 mg/kg, s.c.) decreases plasma testosterone in intact male rats for the first 7 days post-administration. Ganirelix (125 μg per day for 30 days) decreases the surface area of endometriotic lesions and serum progesterone levels in female baboons. Formulations containing ganirelix have been used to prevent premature ovulation in women undergoing in vitro fertilization.

规格	价格	是否有货	数量
500μg		In-stock
1mg		In-stock
5mg		In-stock
10mg		In-stock

加入购物车大包装询价

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Ganirelix (acetate) In-stock
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生物活性

Ganirelix acetate (Ganirest) is a competitive and selective gonadotropin-releasing hormone (GnRH) antagonist. Ganirelix acetate blocks endogenous GnRH-induced release of luteinizing hormone (LH) and follicle-stimulating hormone. Ganirelix acetate antagonizes Prostaglandin E2 (HY-101952)-induced detrusor overactivity and enhances Carbachol (HY-B1208)-induced detrusor contraction. Ganirelix acetate is applicable to research related to female infertility and detrusor overactivity[1][2].

IC₅₀&Target

GnRH

体外研究

Ganirelix (1 nM-1 μM) acetate had no effect on Carbachol induced or nerve induced detrusor muscle contractions in female rat bladder specimens in vitro[2].

体内研究

Ganirelix (0.1 mg/kg; subcutaneous injection; Daily administration of medication; Acetate can reduce plasma LH levels in female rats for 14 consecutive days, significantly alleviate prostaglandin E2 induced overactivity of the detrusor muscle, and enhance high concentration Carbachol induced detrusor muscle contraction [2].
Ganirelix (1.4 mg/L; intravesical administration; Single dose administration of acetate can regulate normal urinary function in female rats by prolonging the interval between urination, increasing urine output and bladder capacity, while reducing baseline urodynamic pressure, threshold urodynamic pressure, and maximum urodynamic pressure parameters; Its reduction in flow pressure did not reach statistical significance [2].

Animal Model:	Sprague-Dawley (female, 225-300 g, intravesical infusion of 50 μM prostaglandin E2-induced detrusor overactivity)
Dosage:	0.1 mg/kg
Administration:	s.c.; daily; 14 days
Result:	Reduced plasma luteinising hormone (LH) levels to 0.48 ng/mL. Reduced micturition interval (MI) by 22%. Reduced micturition volume (MV) by 23%. Reduced bladder capacity (BC) by 21% . Increased threshold pressure (TP) by 16%. Increased flow pressure (FP) by 16%. Enhanced maximal carbachol-induced contraction force to 231% of 60 mM K+-induced contractions at 10 μM Carbachol. Showed no significant differences in body weight, bladder weight, or baseline urodynamic parameters compared to controls.

Animal Model:	Sprague-Dawley (female, 225-300 g)
Dosage:	1.4 mg/L; 0.14 mg/L
Administration:	intravesical; single dose
Result:	Increased micturition interval (MI) to 7.06 min at 1.4 mg/L. Increased micturition volume (MV) to 1.17 mL at 1.4 mg/L. Increased bladder capacity (BC) to 1.17 mL 1.4 mg/L. Reduced basal pressure (BP) to 21.5 cm H2O at 1.4 mg/L. Reduced threshold pressure (TP) to 34.9 cm H2O at 1.4 mg/L. Reduced maximum pressure (MP) to 126.0 cm H2O at 1.4 mg/L. Reduced flow pressure (FP) with no statistical significance at 1.4 mg/L. Showed no effect on any measured urodynamic parameters at 0.14 mg/L.

分子式

C₈₀H₁₁₃ClN₁₈O₁₃^.₂C₂H₄O₂

分子量

1690.42

CAS号

129311-55-3

中文名称

加尼瑞克乙酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性数据

In Vitro:

H2O : 50 mg/mL (29.58 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.5916 mL	2.9578 mL	5.9157 mL
5 mM	0.1183 mL	0.5916 mL	1.1831 mL
10 mM	0.0592 mL	0.2958 mL	0.5916 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂：PBS

Solubility: 50 mg/mL (29.58 mM); Clear solution; Need ultrasonic

纯度： ≥98%

Data Sheet

产品使用指南

[1]. Gustofson RL, et al. Ganirelix acetate causes a rapid reduction in estradiol levels without adversely affecting oocyte maturation in women pretreated with leuprolide acetate who are at risk of ovarian hyperstimulation syndrome. Hum Reprod. 2006;21(11):2830-2837.

[2]. Russo A. et al. Effects of the gonadotropin-releasing hormone antagonist ganirelix on normal micturtion and prostaglandin E(2)-induced detrusor overactivity in conscious female rats. Eur Urol. 2011;59(5):868-874.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

重置计算

动物实验计算换算器

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

Other Forms of Rapamycin:

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The molarity calculator equation

The dilution calculator equation

动物实验计算换算器