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

Icatibant  (Synonyms: 艾替班特; HOE 140)

目錄號(hào): HY-17446 純度: 99.63%
COA 產(chǎn)品使用指南 技術(shù)支持

Icatibant (HOE-140) 是有效的,特異的緩激肽B2受體拮抗劑,IC50Ki 值分別為 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

1.  客戶無需承擔(dān)相應(yīng)的運(yùn)輸費(fèi)用。

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     可免費(fèi)申領(lǐng)三個(gè)不同產(chǎn)品的試用裝。

3.  試用裝只面向終端客戶。

規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in Water ¥9327
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1 mg ¥2250
In-stock
5 mg ¥4500
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Customer Review

Other Forms of Icatibant:

查看 Bradykinin Receptor 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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)

 

細(xì)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]
體外研究
(In Vitro)

Icatibant (10-30 μM) 增強(qiáng)血管緊張素 III,但不增強(qiáng)血管緊張素 II (由血管緊張素 AT1 受體介導(dǎo)的收縮) 和 Lys-des-Arg9-緩激肽,但不增強(qiáng) des-Arg9-緩激肽 (由緩激肽 B1 受體介導(dǎo)的作用) 的作用[3]。

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

體內(nèi)研究
(In Vivo)

Icatibant (0.3 或 1.5 mg/kg,小鼠每天兩次皮下給藥) 顯示出對潰瘍性結(jié)腸炎的顯著預(yù)防作用[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 號(hào)
性狀

固體

顏色

White to off-white

中文名稱

艾替班特

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)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)

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

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

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí),請?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請?jiān)?個(gè)月內(nèi)使用。

* 備注:如您選擇水作為儲(chǔ)備液,請稀釋至工作液后,再用 0.22 μm 的濾膜過濾除菌后使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn):

以下溶解方案,請直接配制工作液。建議現(xiàn)用現(xiàn)配,在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比; 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶。

  • 方案 一

    請依序添加每種溶劑: PBS

    Solubility: 50 mg/mL (38.33 mM); 澄清溶液; 超聲助溶

動(dòng)物溶解方案計(jì)算器
請輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過程有損耗,建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
該產(chǎn)品水溶性佳,請具體參考實(shí)測 水 / PBS / Saline 中的溶解度數(shù)據(jù)。
您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測溶解度,如有需要,請與 MCE 中國技術(shù)支持聯(lián)系。
純度 & 產(chǎn)品資料

純度: 99.63%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí),請?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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

* 備注:如您選擇水作為儲(chǔ)備液,請稀釋至工作液后,再用 0.22 μm 的濾膜過濾除菌后使用。

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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產(chǎn)品名稱:
Icatibant
目錄號(hào):
HY-17446
需求量: