1. GPCR/G Protein
  2. Bradykinin Receptor
  3. Icatibant

Icatibant  (Synonyms: 艾替班特; HOE 140)

目录号: HY-17446 纯度: 99.63%
COA 产品使用指南

Icatibant (HOE-140) 是有效的,特异的缓激肽B2受体拮抗剂,IC50Ki 值分别为 1.07 nM 和 0.798 nM。

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Custom Peptide Synthesis

Icatibant Chemical Structure

Icatibant Chemical Structure

CAS No. : 130308-48-4

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规格 价格 是否有货 数量
10 mM * 1 mL in Water ¥9327
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1 mg ¥2250
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5 mg ¥4500
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Customer Review

Other Forms of Icatibant:

查看 Bradykinin Receptor 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Icatibant (HOE-140) is a potent and specific peptide antagonist of bradykinin B2 receptor with IC50 and Ki of 1.07 nM and 0.798 nM respectively[1][2][3].

IC50 & Target

Bradykinin B2 Receptor (B2R)

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A-431 IC50
3.3 nM
Compound: Icatibant
Concentration required to inhibit specific binding of [3H]BK (1.2 nM) to A-431 cells (human epidermoid carcinoma) which express Bradykinin receptor B2 by 50%.
Concentration required to inhibit specific binding of [3H]BK (1.2 nM) to A-431 cells (human epidermoid carcinoma) which express Bradykinin receptor B2 by 50%.
[PMID: 9767643]
A-431 IC50
3.3 nM
Compound: Icatibant
Concentration required to inhibit specific binding of [3H]BK at 1.2 nM to A-431 cells (human epidermoid carcinoma) which express Bradykinin receptor B2 by 50%.
Concentration required to inhibit specific binding of [3H]BK at 1.2 nM to A-431 cells (human epidermoid carcinoma) which express Bradykinin receptor B2 by 50%.
[PMID: 9767642]
CHO IC50
0.49 nM
Compound: 1 (Icatibant)
In vitro inhibitory activity towards human bradykinin receptor B2 expressed in CHO cells using [3H]BK (1.0 nM) as a radioligand
In vitro inhibitory activity towards human bradykinin receptor B2 expressed in CHO cells using [3H]BK (1.0 nM) as a radioligand
[PMID: 15027853]
CHO IC50
0.49 nM
Compound: Icatibant
Inhibition specific binding of [3H]BK (1.0 nM) to human Bradykinin receptor B2 which was expressed in CHO (Chinese hamster ovary) cells by 50%.
Inhibition specific binding of [3H]BK (1.0 nM) to human Bradykinin receptor B2 which was expressed in CHO (Chinese hamster ovary) cells by 50%.
[PMID: 9767643]
体外研究
(In Vitro)

Icatibant (10-30 μM) potentiates angiotensin III, but not angiotensin II (contraction mediated by angiotensin AT1 receptors), and Lys-des-Arg9-bradykinin, but not des-Arg9-bradykinin (effects mediated by the bradykinin B1 receptors)[3].

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

体内研究
(In Vivo)

Icatibant (0.3, or 1.5 mg/kg, subcutaneous administration twice daily in mice) shows a significant preventive effect on ulcerative Colitis[2].

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

Animal Model: Female mice of the CBA/J (H-2k) strain[2].
Dosage: 0.06, 0.3, or 1.5 mg/kg.
Administration: Subcutaneous administration twice daily.
Result: The length of the large intestine was 93.6±6.8 mm with the 1.5 mg/kg dosage and 94.0±4.1 mm with the 0.3 mg/kg dosage , showing a significant preventive effect on shortening.
Clinical Trial
分子量

1304.52

Formula

C59H89N19O13S

CAS 号
性状

固体

颜色

White to off-white

中文名称

艾替班特

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

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

溶解性数据
细胞实验: 

H2O 中的溶解度 : 100 mg/mL (76.66 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.7666 mL 3.8328 mL 7.6657 mL
5 mM 0.1533 mL 0.7666 mL 1.5331 mL
查看完整储备液配制表

* 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 (sealed storage, away from moisture)。-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。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 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。

  • 方案 一

    请依序添加每种溶剂: PBS

    Solubility: 50 mg/mL (38.33 mM); 澄清溶液; 超声助溶

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: 99.63%

参考文献

完整储备液配制表

* 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 (sealed storage, away from moisture)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 0.7666 mL 3.8328 mL 7.6657 mL 19.1641 mL
5 mM 0.1533 mL 0.7666 mL 1.5331 mL 3.8328 mL
10 mM 0.0767 mL 0.3833 mL 0.7666 mL 1.9164 mL
15 mM 0.0511 mL 0.2555 mL 0.5110 mL 1.2776 mL
20 mM 0.0383 mL 0.1916 mL 0.3833 mL 0.9582 mL
25 mM 0.0307 mL 0.1533 mL 0.3066 mL 0.7666 mL
30 mM 0.0256 mL 0.1278 mL 0.2555 mL 0.6388 mL
40 mM 0.0192 mL 0.0958 mL 0.1916 mL 0.4791 mL
50 mM 0.0153 mL 0.0767 mL 0.1533 mL 0.3833 mL
60 mM 0.0128 mL 0.0639 mL 0.1278 mL 0.3194 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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.

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产品名称:
Icatibant
目录号:
HY-17446
需求量: