Art. -Nr.: HY-108896

Icatibant acetate

(Synonyms: HOE 140 acetate)

13 Cited Publications

Kundenbewertung

Based on 13 publication(s) in Google Scholar

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

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Reinheit: 99.87%
CAS. Nr.: 138614-30-9
Formel: C₆₁H₉₃N₁₉O₁₅S
Molecular Weight:1364.57

Speicherung:

Sealed storage, away from moisture and light.

Powder -80°C, 2 years , -20°C, 1 year

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

Icatibant acetate Chemical Structure

CAS. Nr.: 138614-30-9

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vivo
- Clinical Trial
Chemical Information
Publications (13)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

IC₅₀ & Target

Bradykinin B2 Receptor (B2R)

Alle Bradykinin Receptor Isoform-spezifische Produkte anzeigen :

In Vivo

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.

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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 138614-30-9
Appearance Solid
Molecular Weight 1364.57
Formel C₆₁H₉₃N₁₉O₁₅S
Color White to off-white
Synonyms

HOE 140 acetate
Sequence

Asp-Arg-Arg-Pro-Hyp-Gly-Thia-Thr-Thr-Arg-Asp-Phe-Ile-Glu-Ile-Ile-Trp-Arg-Lys-NH2
Sequence Shortening

DRRP-Hyp-G-Thia-TTREDFIIWRK-NH2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Sealed storage, away from moisture and light

Powder	-80°C	2 years
	-20°C	1 year

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

Publications (13)

All ELISABio/Physico-chemical AssayRT-PCRHistological Imaging/StainingIn Vivo Efficacy Study

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Journal Impact Factor

Nat Commun

Reduced hepatic bradykinin degradation accounts for cold-induced BAT thermogenesis and WAT browning in male mice. [Abstract]

2023 May 2;14(1):2523. PMID: 37130842

Icatibant acetate 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 acetate 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 acetate 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 acetate 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.
Adv Sci (Weinh)

SRSF5-Mediated Alternative Splicing of M Gene is Essential for Influenza A Virus Replication: A Host-Directed Target Against Influenza Virus. [Abstract]

2022 Dec;9(34):e2203088. PMID: 36257906
Br J Pharmacol

Factor XII and prekallikrein promote microvascular inflammation and psoriasis in mice. [Abstract]

2024 Oct;181(19):3760-3778. PMID: 38872396

Icatibant acetate 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.
Biomed Pharmacother

Maximakinin reversed H2O2 induced oxidative damage in rat cardiac H9c2 cells through AMPK/Akt and AMPK/ERK1/2 signaling pathways. [Abstract]

2024 May:174:116489. PMID: 38513595
Am J Physiol Cell Physiol

Redox-sensitive GPCR signaling drives Gq-dependent Ca²⁺ mobilization and cytokine production in human bronchial epithelial cells. [Abstract]

2026 Jun 18. PMID: 42314770
iScience

Bradykinin induces acute kidney injury after hypothermic circulatory arrest through the repression of the Nrf2-xCT pathway. [Abstract]

2024 May 22;27(6):110075. PMID: 38868208
iScience

QHRD106 ameliorates ischemic stroke injury as a long-acting tissue kallikrein preparation. [Abstract]

2023 Jul 3;26(7):107268. PMID: 37496671
J Renin Angiotensin Aldosterone Syst

The Effect of the Angiotensin-Converting Enzyme Inhibitor on Bone Health in Castrated Hypertensive Rats Is Mediated via the Kinin-Kallikrein System. [Abstract]

2022 Jun 14:2022:9067167. PMID: 35814865
Sci Rep

Penicillin causes non-allergic anaphylaxis by activating the contact system. [Abstract]

2020 Aug 25;10(1):14160. PMID: 32843685
Biochem Biophys Res Commun

Bradykinin attenuates NiSO4-induced autophagy in MIN6 cells and protects islet function in mice by regulating the PI3K/AKT/mTOR signaling pathway. [Abstract]

2024 Dec 31:746:151265. PMID: 39756208
Biochem Biophys Res Commun

Inflammatory mediator bradykinin increases population of sensory neurons expressing functional T-type Ca(2+) channels. [Abstract]

2016 Apr 29;473(2):396-402. PMID: 26944020
Patent

US20250320500A1.
SSRN

2023 Dec 27.

Lösungsmittel & Löslichkeit

In Vitro:

H₂O : 100 mg/mL (73.28 mM; Need ultrasonic)

DMSO : 100 mg/mL (73.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.7328 mL

3.6642 mL

7.3283 mL

5 mM

0.1466 mL

0.7328 mL

1.4657 mL

10 mM

0.0733 mL

0.3664 mL

0.7328 mL

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 and light). 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Working Solution

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: ≥ 100 mg/mL (73.28 mM); Clear solution

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	0.7328 mL	3.6642 mL	7.3283 mL	18.3208 mL
	5 mM	0.1466 mL	0.7328 mL	1.4657 mL	3.6642 mL
	10 mM	0.0733 mL	0.3664 mL	0.7328 mL	1.8321 mL
	15 mM	0.0489 mL	0.2443 mL	0.4886 mL	1.2214 mL
	20 mM	0.0366 mL	0.1832 mL	0.3664 mL	0.9160 mL
	25 mM	0.0293 mL	0.1466 mL	0.2931 mL	0.7328 mL
	30 mM	0.0244 mL	0.1221 mL	0.2443 mL	0.6107 mL
	40 mM	0.0183 mL	0.0916 mL	0.1832 mL	0.4580 mL
	50 mM	0.0147 mL	0.0733 mL	0.1466 mL	0.3664 mL
	60 mM	0.0122 mL	0.0611 mL	0.1221 mL	0.3053 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.

Keywords

Icatibant acetate

13 Cited Publications

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Icatibant acetate

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Publications Citing Use of MedChemExpress (MCE) Icatibant acetate

Alle Bradykinin Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (13)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Icatibant acetate

Anti-Infection Compound Library

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

FDA-Approved Drug Library

Drug Repurposing Compound Library

Anti-Cardiovascular Disease Compound Library

NMPA-Approved Drug Library

Neurotransmitter Receptor Compound Library

FDA Approved & Pharmacopeial Drug Library

Drug-Induced Liver Injury (DILI) Compound Library

Targeted Diversity Library

Rare Diseases Drug Library

Peptide Library

Human Metabolite Library

Non-steroidal Anti-Inflammatory Compound Library

Heterocyclic Compound Library

Off-patent Drug Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Peptide Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Icatibant acetate

Alle Bradykinin Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (13)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Icatibant acetate Related Classifications

HY-108896 Related Classifications