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  3. S-Isopropylisothiourea hydrobromide

S-Isopropylisothiourea hydrobromide  (Synonyms: S-isopropyl ITU; IPTU)

目录号: HY-101304 纯度: 98.0%
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S-Isopropylisothiourea hydrobromide (S-isopropyl ITU; IPTU) 是一种可透过血脑屏障 (BBB) 的 NOS 抑制剂,其对小鼠脊髓、小脑和牛主动脉和猪内皮细胞的 NOS 的 IC50 值分别为 0.66、0.75、0.29 和 0.5 μM。S-Isopropylisothiourea hydrobromide 具有显著的升压作用,且不损害重要器官的灌注,还能抑制福尔马林诱导的晚期相疼痛。S-Isopropylisothiourea hydrobromide 可用于研究出血性休克和基于 NOS 的疼痛反应。

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S-Isopropylisothiourea hydrobromide

S-Isopropylisothiourea hydrobromide Chemical Structure

CAS No. : 4269-97-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

S-Isopropylisothiourea hydrobromide (S-isopropyl ITU; IPTU) is a blood-brain barrier (BBB) penetrant NOS inhibitor with IC50 values of 0.66, 0.75 and 0.29 μM against mouse spinal cord, cerebellar, bovine aortic and porcine endothelial cell NOS. S-Isopropylisothiourea exhibits a significant blood pressure-raising effect without damaging the perfusion of vital organs and can also inhibit the late-phase pain response induced by formalin. S-Isopropylisothiourea hydrobromide is used in the researchs for hemorrhagic shock and pain response based on NOS[1][2].

IC50 & Target[1][2]

eNOS

0.5 μM (IC50)

nNOS

0.66 μM (IC50)

nNOS

0.75 μM (IC50)

eNOS

0.29 μM (IC50)

体内研究
(In Vivo)

S-Isopropylisothiourea hydrobromide (50 mg/kg,腹腔注射,单次给药) 可透过血脑屏障,在中枢神经系统达到有效浓度,并通过抑制小鼠血管内皮型一氧化氮合酶 (eNOS) 发挥强效且持续的升压作用[1]
S-Isopropylisothiourea hydrobromide (10-50 mg/kg,腹腔注射,单次给药) 在50 mg/kg 剂量下表现出选择性镇痛作用,特别是在疼痛后期 (15-30分钟) 抑制疼痛[1]
S-Isopropylisothiourea hydrobromide (0.1 mg/kg,静脉注射,3次给药) 显著升高平均动脉压,并在严重出血性休克大鼠模型中达到 100% 的存活率[2]
S-Isopropylisothiourea hydrobromide (0.3 mg/kg + 1 mg/kg·h,静脉输注,维持输注 120 分钟) 可显著升高平均动脉压至正常水平,且不降低心输出量,并维持重要器官的灌注[2]

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

Animal Model: Formalin-induced hindpaw licking behaviour established in mice (male, LACA, 25-35 g)[1]
Dosage: 10, 20 and 30 mg/kg
Administration: Intraperitoneal injection (i.p.), single dose
Result: Reduced the movement and grooming behaviors of mice.
Did not affect the paw edema induced by formalin.
Animal Model: Pylorus-ligated model established in male Wistar rats[2]
Dosage: 0.1 mg/kg
Administration: Intravenous injection (i.v.), 10 min, 20 min, and 40 min, administered in three doses
Result: Increased MAP to 65-70 mmHg, and the survival rate was 100%.
Animal Model: Porcine hemorrhagic shock model established in York shire pigs (6-10 weeks, 10-15.5 kg)[2]
Dosage: 0.3 mg/kg plus 1 mg/kg·h
Administration: Intravenous injection (i.v.), maintain infusion for 120 min
Result: Increased MAP to 90 mmHg.
Maintained a stable heart rate and do not affect the cardiac output.
Increased the vascular resistance of the system.
分子量

199.11

Formula

C4H11BrN2S

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料

纯度: 98.0%

参考文献

S-Isopropylisothiourea hydrobromide 相关分类

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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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S-Isopropylisothiourea hydrobromide
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