标签归档：icatibant

Icatibant acetate(Synonyms: HOE 140 acetate)

发表于由

Icatibant acetate;(Synonyms: HOE 140 acetate) 纯度: 99.64%

Icatibant acetate (HOE-140 acetate) 是有效的，特异的缓激肽 B2 受体拮抗剂，IC50 和 Ki 值分别为 1.07 nM和 0.798 nM。

Icatibant acetate (Synonyms: HOE 140 acetate)

Icatibant acetate Chemical Structure

CAS No. : 138614-30-9

规格 价格 是否有货 数量
10;mM;*;1 mL in DMSO ￥10510 In-stock
1 mg ￥1150 In-stock
5 mg ￥3500 In-stock
10 mg ; 询价 ;
50 mg ; 询价 ;

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生物活性

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[1][2][3].

体外研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(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].

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

分子量

1364.57

Formula

C61H93N19O15S
CAS 号

138614-30-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

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)
溶解性数据
In Vitro:;

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

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
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.

    [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.

    [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.