Icatibant (acetate)
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 Ki of 1.07 nM and 0.798 nM respectively.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.87%
- CAS 番号: 138614-30-9
- 分子式: C61H93N19O15S
- 分子量:1364.57
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保管条件:
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)
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 Icatibant acetate
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.
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Bradykinin Receptor アイソフォーム固有の製品をすべて表示
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生物活性
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Bradykinin B2 Receptor (B2R) |
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 138614-30-9
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性状 Solid
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分子量 1364.57
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分子式 C61H93N19O15S
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Color White to off-white
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別名
HOE 140 (acetate); イカチバント酢酸塩
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配列
Asp-Arg-Arg-Pro-Hyp-Gly-Thia-Thr-Thr-Arg-Asp-Phe-Ile-Glu-Ile-Ile-Trp-Arg-Lys-NH2
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シーケンスの短縮
DRRP-Hyp-G-Thia-TTREDFIIWRK-NH2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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)
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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 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.
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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 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.
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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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溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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: ≥ 100 mg/mL (73.28 mM); Clear solution
純度とドキュメンテーション
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取扱説明書 (2659 KB)
参考文献
[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 and light). 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 / 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.
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