2. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel
  3. Adrenergic Receptor Sodium Channel Potassium Channel
  4. ICI 147798

ICI 147798 是一种口服有效的 β-肾上腺素受体 (β-adrenoceptor) 拮抗剂，其 pKB 为 9.1 (豚鼠右心房) 和 8.8 (豚鼠气管)。ICI 147798 是一种利尿剂和眼内压降低剂。ICI 147798 可阻断 β-肾上腺素受体，抑制异丙肾上腺素诱导的心动过速和血管降压反应，对 β-1 肾上腺素受体表现出缓慢解离、不可克服的拮抗作用，对 β-2 肾上腺素受体表现出可克服的竞争性拮抗作用。ICI 147798 可诱导利钠和利钾作用，抑制钠转运，降低眼内压[1]2]。

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

ICI 147798

ICI 147798 Chemical Structure

CAS No. : 83812-65-1

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 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

ICI 147798 相关抗体

Top Publications Citing Use of Products

查看 Adrenergic Receptor 亚型特异性产品:

查看所有亚型
α adrenergic receptor β adrenergic receptor

查看 Sodium Channel 亚型特异性产品:

查看所有亚型
Nav1.1 Nav1.2 Nav1.3 Nav1.4 Nav1.5 Nav1.6 Nav1.7 Nav1.8 Nav1.9

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ICI 147798 is an orally effective β-adrenoceptor antagonist with a pKB of 9.1 (in guinea pig right atrium) and 8.8 (in guinea pig trachea). ICI 147798 acts as a diuretic and intraocular pressure-lowering agent. ICI 147798 blocks β-adrenoceptors, inhibits isoproterenol-induced tachycardia and vasodepressor responses, exhibits slowly dissociating, insurmountable antagonism against β1-adrenoceptors, and shows surmountable competitive antagonism against β2-adrenoceptors. ICI 147798 induces natriuresis and kaliuresis, inhibits sodium transport, and reduces intraocular pressure[1][2][3].

IC50 & Target[1]

β-adrenoceptor

8.8 (pkB)

体外研究
(In Vitro)

ICI 147798 可抑制离体蟾蜍膀胱标本中的 Na+ 转运，其黏膜侧和浆膜侧的 IC50 值分别为 56 μM 和 120 μM[1]。
ICI 147798 是离体豚鼠右心房中的 β-肾上腺素受体拮抗剂，其 pKB 值为 9.1[1]。
ICI 147798 是离体豚鼠气管中的 β-肾上腺素受体拮抗剂，其 pKB 值为 8.8[1]。

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

ICI 147798 相关抗体:
体内研究
(In Vivo)

ICI 147798 (0.125-0.75%；滴眼；单次给药) 对未麻醉的新西兰兔在水负荷诱导的高眼压模型中可产生具有统计学意义、浓度依赖性的眼压降低效果，其降眼压的 ED50 为 0.27%，0.5% 剂量下的作用持续时间为 5 小时[2]。
ICI 147798 (0.1-1.0 mg/kg；静脉注射) 可作为强效静脉用 β-肾上腺素受体拮抗剂作用于未麻醉的新西兰兔，其阻断异丙肾上腺素诱导的心动过速的 ED50 为 0.23 mg/kg[2]。
ICI 147798 (0.5%；局部给药；单剂量，每日 2 次，连续 4 天) 对未麻醉的新西兰兔体内异丙肾上腺素诱导的心动过速无显著阻断作用，即使在每日给药 2 次、连续给药 4 天后也是如此[2]。

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

Animal Model: New Zealand rabbits (adult, 2-5 kg, both sexes, water-load-induced ocular hypertension model)[2]
Dosage: 300 μl, 0.5%; 200 μl, 0.5%; 200 μl, 0.125%; 200 μl, 0.25%; 100 μl, 0.5%; 200 μl, 0.75%; 100 μl, 0.75%
Administration: eye drop; single dose
Result: Reduced mean water-load-induced IOP increase to 4.0 mmHg at 1 hour, 5.3 mmHg at 3 hours, and 6.2 mmHg at 5 hours after 300 μl, 0.5% topical dosing to one eye.
Reduced mean water-load-induced IOP increase to 4.5 mmHg (left eye) and 4.0 mmHg (right eye) at 1 hour after 200 μl, 0.5% topical dosing to both eyes (P<0.05 vs control).
Exhibited concentration-dependent IOP-lowering effect with an ED50 of 0.27%.
Reduced mean water-load-induced IOP increase to 5.5 mmHg (left eye) and 5.5 mmHg (right eye) after 100 μl, 0.5% dosing in 5% PEG 400 + 5% Pluronic F127 vehicle.
Showed no enhanced IOP-lowering efficacy with 0.75% concentration or 200 μl volume, with mean ΔmmHg values ranging from 5.0 to 5.5 mmHg.
分子量

515.99

Formula

C24H30ClN7O4
CAS 号
运输条件

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

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

ICI 147798 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:

ICI 14779883812-65-1ICI147798ICI-147798Adrenergic ReceptorSodium ChannelPotassium ChannelBeta ReceptorNa channelsNa+ channelsKcsAglaucomaadenylate cyclaseβ-adrenoceptorβ-1 adrenoceptorsNew Zealand rabbitstoad bladderguinea pig right atriaguinea pig tracheaβ-2 adrenoceptorshistamine H2-receptorInhibitorinhibitorinhibit

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：
ICI 147798
目录号：
HY-182635
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