2. GPCR/G Protein
  3. GnRH Receptor
  4. AG-045572

AG-045572 是一种 GnRH 受体拮抗剂，对人类和大鼠的 GnRH receptor 的 Ki 值分别为 6.0 nM 和 3.8 nM。AG-045572 通过 CYP3A 代谢并抑制睾酮。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

AG-045572 Chemical Structure

AG-045572 Chemical Structure

CAS No. : 263847-55-8

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 价格 是否有货 数量
1 mg ￥725
In-stock
5 mg ￥1810
In-stock
10 mg ￥2530
In-stock
25 mg ￥4500
In-stock
50 mg 现货 询价
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

AG-045572 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AG-045572 is a GnRH receptor antagonist with Kis of 6.0 nM and 3.8 nM for human and rat GnRH receptor, respectively. AG-045572 is metabolized by CYP3A and ressuppresses testosterone[1].

体外研究
(In Vitro)

AG-045572 (10 μM，40 min，for human liver microsomes; 10 μM，10 min，for male rat liver microsomes; 1 μM，10 min，for female rat liver microsomes) 在大鼠和人体内均通过 CYP3A 代谢，在雄性和雌性人、雌性大鼠肝脏微粒体以及表达的 CYP3A4 和 CYP3A5 中的 Km 值相似 (分别为0.39、0.27、0.28、0.25和0.26 μM)，而在雄性大鼠肝脏微粒体中的 Km 值为 1.5 μM，表明 AG-045572 在雄性和雌性大鼠体内通过不同的 CYP3A 同工酶代谢[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

AG-045572 相关抗体:
体内研究
(In Vivo)

AG-045572 (10 mg/kg (静脉注射) 或 20 mg/kg (口服)，单剂量) 用于完整雄性大鼠，显示出中等的 T1/2、CL 和 Vss，但口服生物利用度较低，用于雌性大鼠的生物利用度较高 (24%)，用于阉割雄性大鼠的药代动力学与雌性大鼠相似[1]。
AG-045572 (40 mg/kg，肌肉注射，每天 2 次，共 3 天) 预处理完整雄性大鼠后，其药代动力学发生变化，各项参数与雌性和阉割雄性大鼠相似[1]。
KDM5B-IN-4 (compound 11ad) 在异种移植模型中的药代动力学分析[1]

Parameter T1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (h*ng/mL) MRT0-t (h) Vz (L/kg) Cl (L h/kg) F
p.o. (25mg/kg) 5.30 6.0 411.67 3024.33 6.90 / / 20.28%
i.v. (5mg/kg) 2.95 0.083 551.67 44437.67 10.29 19.51 0.49 /

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male rats were surgically castrated via scrotal approach under halothane anesthesia and allowed 14 days post-operative recovery prior to study[1]
Dosage: 10 mg/kg, 20 mg/kg; 40 mg/kg
Administration: administered acutely at 10 mg/kg (i.v.) or 20 mg/kg (p.o.), one time; For multiple-dose pretreatment, male rats at 40 mg/kg, i.m. twice a day for 3 days.
Result: Showed medium T1/2, CL and Vss but oral bioavailability was low, in female rats the bioavailability was much higher (24%)
Became similar to those in female and castrated male rats.
分子量

491.62

Formula

C30H37NO5
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

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

纯度 & 产品资料
参考文献

AG-045572 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AG-045572263847-55-8AG045572AG 045572GnRH ReceptorGonadotropin releasing hormone receptorGNRHRGnRH receptor antagonistorallyagonistin-haledliver microsomescastrated ratInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
AG-045572
目录号：
HY-107534
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z