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

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.

For research use only. We do not sell to patients.

Custom Peptide Synthesis

Icatibant Chemical Structure

Icatibant Chemical Structure

CAS No. : 130308-48-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
 USD 1119 In-stock
Solution
10 mM * 1 mL in Water USD 1119 In-stock
Solid
1 mg USD 270 In-stock
5 mg USD 540 In-stock
10 mg USD 780 In-stock
50 mg   Get quote  
100 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Icatibant:

Icatibant Related Antibodies

Top Publications Citing Use of Products

View All Bradykinin Receptor Isoform Specific Products:

View All Isoforms
Bradykinin B1 Receptor (B1R) Bradykinin B2 Receptor (B2R)

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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)

 

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]
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].

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

Icatibant Related Antibodies
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].

MedChemExpress (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
Molecular Weight

1304.52

Formula

C59H89N19O13S
CAS No.
Appearance

Solid

Color

White to off-white

Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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)

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (76.66 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 50 mg/mL (38.33 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.63%

SDS (252 KB)

COA (253 KB) RP-HPLC (109 KB) MS (258 KB) Elemental Analysis Report (111 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Icatibant Related Classifications

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:

Icatibant130308-48-4HOE 140HOE140HOE-140Bradykinin ReceptorangiotensinulcerativecolitisInhibitorinhibitorinhibit

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