Icatibant (Synonyms: HOE 140)

Name: Icatibant
Brand: MedChemExpress
SKU: HY-17446
Rating: 5.0 (12 reviews)

Cat. No.: HY-17446 Purity: 99.97%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

Icatibant (HOE-140) is a potent and specific peptide antagonist of bradykinin B2 receptor with IC₅₀ and K_i of 1.07 nM and 0.798 nM respectively.

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

Custom Peptide Synthesis

CAS No. : 130308-48-4

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in Water	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	Get quote
200 mg	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

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

Customer Review

Based on 12 publication(s) in Google Scholar

Other Forms of Icatibant:

Icatibant acetate In-stock
Icatibant (Standard) Get quote

12 Publications Citing Use of MCE Icatibant

ELISA

Bio/Physico-chemical Assay

RT-PCR

Histological Imaging/Staining

In Vivo Efficacy Study

: Icatibant purchased from MedChemExpress. Usage Cited in: Br J Pharmacol. 2024 Oct;181(19):3760-3778. [Abstract]; Icatibant (1.5 mg/kg; i.p.; every 12 h) treatment reduced plasma levels of TNF-α and IL-1β in the psoriatic mice.

: Icatibant purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 May 2;14(1):2523. [Abstract]; Icatibant (1 mg/kg; i.p.; 3 h) significantly downregulated UCP1 in the BAT of C57BL/6J mice exposed to acute cold.

: Icatibant purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 May 2;14(1):2523. [Abstract]; Icatibant (1 mg/kg; i.p.; 3 h) markedly reduced mRNA levels of browning marker genes in the sWAT of C57BL/6J mice exposed to acute cold.

: Icatibant purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 May 2;14(1):2523. [Abstract]; Icatibant (1 mg/kg; i.p.; 3 h) enlarged lipid droplets in the sWAT of C57BL/6J mice exposed to acute cold.

: Icatibant purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 May 2;14(1):2523. [Abstract]; Icatibant (1 mg/kg; i.p.; 3 h) reduced body temperature of C57BL/6J mice during acute cold exposure.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

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 K_i 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 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]
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]
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.

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-2^k) 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.

Molecular Weight

1304.52

Formula

C₅₉H₈₉N₁₉O₁₃S

CAS No.

130308-48-4

Appearance

Solid

Color

White to off-white

Sequence Shortening

RRPXGXSXXR

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
10 mM	0.0767 mL	0.3833 mL	0.7666 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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)

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: 99.97%

Select Batch:

Data Sheet (277 KB) SDS (393 KB)

COA (253 KB) RP-HPLC (250 KB) MS (235 KB) Elemental Analysis Report (111 KB)

Handling Instructions (2659 KB)

References

[1]. Hock FJ, et al. Hoe 140 a new potent and long acting bradykinin-antagonist: in vitro studies. Br J Pharmacol. 1991 Mar;102(3):769-73. [Content Brief]

[2]. Y Arai, et al. Effect of Icatibant, a Bradykinin B2 Receptor Antagonist, on the Development of Experimental Ulcerative Colitis in Mice. Dig Dis Sci. 1999 Apr;44(4):845-51. [Content Brief]

[3]. Marie-Thérèse Bawolak, et al The Bradykinin B2 Receptor Antagonist Icatibant (Hoe 140) Blocks Aminopeptidase N at Micromolar Concentrations: Off-Target Alterations of Signaling Mediated by the Bradykinin B1 and Angiotensin Receptors. Eur J Pharmacol. 2006 Dec 3;551(1-3):108-11. [Content Brief]

Complete Stock Solution Preparation Table

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.

Icatibant Related Classifications

Endocrinology

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

Your Recently Viewed Products:

Product Name

Requested Quantity *

Applicant Name *

Salutation

Email Address *

Phone Number *

Department

Organization Name *

City

State

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Icatibant (Synonyms: HOE 140)

Customer Review

Other Forms of Icatibant:

Icatibant Related Antibodies

12 Publications Citing Use of MCE Icatibant

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Bradykinin Receptor Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Icatibant Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Icatibant Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report