1. Metabolic Enzyme/Protease
  2. Ser/Thr Protease
  3. NCO-650 free base

NCO-650 free base 是一种抗过敏剂,通过抑制肥大细胞内的关键胰蛋白酶样蛋白酶 (类胰蛋白酶) 来发挥作用。NCO-650 free base 可抑制肥大细胞释放组胺、肥大细胞内 cAMP 升高、支气管收缩,以及灌注压和全身血压下降。NCO-650 free base 可用于过敏性疾病和支气管哮喘的研究。

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NCO-650 free base

NCO-650 free base Chemical Structure

CAS No. : 81907-78-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NCO-650 free base is an antiallergic agent that acts by inhibiting tryptase, a key trypsin-like protease in mast cells. NCO-650 free base inhibits mast cell histamine release, increases intracellular cAMP levels in mast cells, suppresses bronchoconstriction, and prevents decreases in perfusion pressure and systemic blood pressure. NCO-650 free base is applicable to the research of allergic diseases and bronchial asthma[1][2][3].

体外研究
(In Vitro)

NCO-650 可通过剂量依赖性作用强效抑制抗原 (IC50 = 1.9 μM)、抗 IgE (IC50 = 3.6 μM)、Concanavalin A (HY-P2149) (IC50 = 4.6 μM)、Ionophore A23187 (HY-N6687) (IC50 = 2.9 μM) 以及 Compound 48/80 (HY-115768) (IC50 = 6.1 μM) 诱导的大鼠腹膜肥大细胞组胺释放[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

NCO-650 (100 mg/kg;​十二指肠内给药;单次给药) 可在麻醉雄性杂种犬中对 Compound 48/80 诱导的支气管收缩产生 64% 的抑制作用,同时还能阻断相关血管效应,但不会改变组胺诱导的支气管收缩[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mongrel (male, 8.5-18.5 kg, anesthetized, nonimmunologically induced bronchial asthma model)[3]
Dosage: 100 mg/kg
Administration: i.d.; single dose
Result: Produced a 64% inhibition of the maximal increase in ventilation overflow induced by compound 48/80.
Significantly inhibited the decreases in perfusion pressure and systemic blood pressure caused by compound 48/80.
Had no effect on ventilation overflow, perfusion pressure, or systemic blood pressure when administered alone.
Did not inhibit the increase in ventilation overflow induced by inhalation of 0.005-0.01% histamine for 10 min.
分子量

331.45

Formula

C19H29N3O2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 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.

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产品名称:
NCO-650 free base
目录号:
HY-182414
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