Icatibant
Based on 13 publication(s) in Google Scholar
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.
- Purity: 99.97%
- CAS No.: 130308-48-4
- Formula: C59H89N19O13S
- Molecular Weight:1304.52
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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)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Icatibant
More- Nat Commun. 2023 May 2;14(1):2523. [Abstract]
- Adv Sci (Weinh). 2022 Dec;9(34):e2203088. [Abstract]
- Br J Pharmacol. 2024 Oct;181(19):3760-3778. [Abstract]
- Biomed Pharmacother. 2024 May:174:116489. [Abstract]
- Am J Physiol Cell Physiol. 2026 Jun 18. [Abstract]
- iScience. 2024 May 22;27(6):110075. [Abstract]
- iScience. 2023 Jul 3;26(7):107268. [Abstract]
- J Renin Angiotensin Aldosterone Syst. 2022 Jun 14:2022:9067167. [Abstract]
- Sci Rep. 2020 Aug 25;10(1):14160. [Abstract]
- Biochem Biophys Res Commun. 2024 Dec 31:746:151265. [Abstract]
- Biochem Biophys Res Commun. 2016 Apr 29;473(2):396-402. [Abstract]
- Patent. US20250320500A1.
- SSRN. 2023 Dec 27.
Customer Validation & Images
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ELISA
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Bio/Physico-chemical Assay
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RT-PCR
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Histological Imaging/Staining
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In Vivo Efficacy Study
All Bradykinin Receptor Isoforms
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Biological Activity
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Bradykinin B2 Receptor (B2R) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | IC50 |
3.3 nM
Compound: Icatibant
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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%.
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[PMID: 9767642] |
| A-431 | IC50 |
3.3 nM
Compound: Icatibant
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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%.
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[PMID: 9767643] |
| CHO | IC50 |
0.49 nM
Compound: 1 (Icatibant)
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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
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[PMID: 15027853] |
| CHO | IC50 |
0.49 nM
Compound: Icatibant
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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%.
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[PMID: 9767643] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female mice of the CBA/J (H-2k) strain[2].
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Dosage:0.06, 0.3, or 1.5 mg/kg.
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Administration:Subcutaneous administration twice daily.
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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.
Chemical Information
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CAS No. 130308-48-4
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Appearance Solid
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Molecular Weight 1304.52
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Formula C59H89N19O13S
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Color White to off-white
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Synonyms
HOE 140
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Sequence Shortening
RRPXGXSXXR
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Shipping
Room temperature in continental US; may vary elsewhere.
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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)
Publications (13)
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Journal Impact Factor
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Most Recent
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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 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.
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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
2024 Oct;181(19):3760-3778. PMID: 38872396
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.
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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
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 -
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Solvent & Solubility
H2O : 100 mg/mL (76.66 mM; Need ultrasonic)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (38.33 mM); Clear solution; Need ultrasonic
Purity & Documentation
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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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
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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