2. Metabolic Enzyme/Protease
  3. Renin
  4. CP 71362

CP 71362 是一种肾素抑制剂，是高效的底物类似物过渡态模拟物，具有降压特性。CP 71362 对大鼠、犬及人血浆肾素均表现出显著的抑制活性 (IC50 分别为 3 nM、0.0033 nM 和 20 nM)。CP 71362 呈剂量依赖性地降低麻醉及清醒缺钠动物的平均动脉压，具有消除迅速、作用持续时间短的药代动力学特征。CP 71362 可用于高血压和充血性心力衰竭的相关研究。

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CP 71362

CP 71362 Chemical Structure

CAS No. : 112227-15-3

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CP 71362 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CP 71362 is a renin inhibitor, a highly potent substrate-analog transition state mimic with antihypertensive properties. CP 71362 exhibits significant inhibitory activity against plasma renin from rats, dogs, and humans (IC50 values are 3 nM, 0.0033 nM, and 20 nM, respectively). CP 71362 reduces the mean arterial pressure of anesthetized and conscious sodium-depleted animals in a dose-dependent manner, and has pharmacokinetic characteristics of rapid elimination and short duration of action. CP 71362 can be used in research related to hypertension and congestive heart failure[1][2].

体外研究
(In Vitro)

CP-71,362 对肾素具有高特异性，对牛脾脏 cathepsin D 的效力低 6 个数量级 (IC50=1.3×10-6 M)，且在浓度高达 1×10-3 M 时对兔肺 ACE 无抑制活性[2]。

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

CP 71362 相关抗体:
体内研究
(In Vivo)

CP 71362 (1.1-4.5 ± 0.7 μg/kg/min；静脉注射；持续输注) 可在麻醉且钠耗竭的犬中引起剂量依赖性的平均动脉压降低，其 ED50 输注速率为 1.1 μg/kg/min，在 3.7 ± 0.4 μg/kg/min 时可产生最大 35 mmHg 的血压下降[1]。
CP 71362 (9.7-30 μg/kg/min；静脉注射；持续输注) 可降低清醒缺钠 Sprague-Dawley 大鼠的平均动脉压，其 ED50 输注速率为 9.7 μg/kg/min，30 μg/kg/min 剂量下可使血压下降 30-40 mmHg[1]。
CP 71362 (0.1-3 mg/kg；静脉推注) 可在清醒的钠耗竭豚鼠 (Cavia porcellus)中产生剂量依赖性的平均动脉压降低，其中 1.0 mg/kg 和 3.0 mg/kg 的推注剂量可维持显著作用至少 2 小时[2]。
CP 71362 (静脉输注，1.06-100 µg/kg/min；10-30 分钟) 可在麻醉的钠耗竭犬中产生剂量依赖性、可逆的平均动脉压降低效应，其 ED50 为 1.06 µg/kg/min，且在 ED50 剂量下可完全抑制血浆肾素活性[2]。
CP 71362 (静脉输注，30 分钟) 可在清醒、钠耗竭的 SHR 中快速诱导剂量依赖性且完全可逆的平均动脉压降低，其 ED50 为 5 µg/kg/min[2]。

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

Animal Model: (anesthetized, sodium-depleted)[1]
Dosage: 1.1 μg/kg/min (ED50 infusion rate); 3.7 ± 0.4 μg/kg/min; 4.5 ± 0.7 μg/kg/min
Administration: i.v.; continuous infusion
Result: Reduced mean arterial pressure by 35 mmHg (from 119 mmHg to 84 mmHg, n=5).
Achieved an ED50 infusion rate of 1.1 μg/kg/min for half-maximal decrease in renin-dependent blood pressure.
Produced near-maximal effects on mean arterial pressure at 4.5 ± 0.7 μg/kg/min (~4× the ED50 dose).
Returned mean arterial pressure to pre-infusion levels within 30-60 minutes after cessation of infusion.
Animal Model: Sprague-Dawley (conscious, sodium-depleted)[1]
Dosage: 9.7 μg/kg/min (ED50 infusion rate); 30 μg/kg/min
Administration: i.v.; continuous infusion
Result: Reduced mean arterial pressure by 30-40 mmHg at 30 μg/kg/min.
Achieved an ED50 infusion rate of 9.7 μg/kg/min for half-maximal fall in renin-dependent blood pressure.
Animal Model: Charles River (300-350g; sodium-depleted, renin-dependent hypertension model)[2]
Dosage: 0.1 mg/kg; 1.0 mg/kg; 3.0 mg/kg
Administration: i.v. bolus
Result: Caused a maximum mean arterial pressure decrease of 32 ± 5 mmHg, with significant lowering sustained for 60 minutes at 0.1 mg/kg.
Caused a maximum mean arterial pressure decrease of 36 ± 3 mmHg, with significant lowering sustained for at least 120 minutes at 1.0 mg/kg.
Caused a maximum mean arterial pressure decrease of 38 ± 1 mmHg, with significant lowering sustained for at least 120 minutes at 3.0 mg/kg.
Animal Model: Mongrel (10-15 kg; sodium-depleted, renin-dependent hypertension model)[2]
Dosage: 1.06 µg/kg/min; 4.52 µg/kg/min; 5.0 µg/kg/min; 10.0 µg/kg/min; 20.0 µg/kg/min; 50.0 µg/kg/min; 100.0 µg/kg/min
Administration: i.v. infusion; 30 minutes (most doses); 10 minutes (4.52 µg/kg/min)
Result: Caused dose-dependent lowering of mean arterial pressure, with a maximum decrease of ~50 mmHg at 10.0 µg/kg/min.
Achieved an ED50 of 1.06 µg/kg/min for mean arterial pressure lowering.
Reduced mean arterial pressure from ~115 mmHg to 80 mmHg at 4.52 µg/kg/min, with pressure returning to pre-infusion levels approximately 1 hour after infusion termination.
Reduced plasma renin activity from 23.8 ± 2.5 to 0.04 ± 0.01 ng AngI/mL/hr (p < 0.01) at 1.11 µg/kg/min (ED50 dose).
Animal Model: Spontaneously Hypertensive Rats (SHR) (Charles River, 275-300 g; sodium-depleted, renin-dependent hypertension model)[2]
Dosage: 4.3 µg/kg/min; 10.8 µg/kg/min; 43.3 µg/kg/min
Administration: i.v. infusion; 30 minutes
Result: Caused dose-dependent mean arterial pressure lowering, with a maximum decrease of 43 mmHg at 43.3 µg/kg/min.
Achieved an ED50 of 5 µg/kg/min for mean arterial pressure lowering.
Reached a stable nadir within 10-20 minutes of starting infusion, with pressure returning to baseline within 5 minutes of stopping infusion.
分子量

945.20

Formula

C51H76N8O9
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

CP 71362 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • 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.

Keywords:

CP 71362112227-15-3CP71362CP-71362Reninrat plasma reninrabbit lung ACEsubstrate analog transition state mimicbovine spleen cathepsin Drenin angiotensin systemcongestive heart failurehuman plasma reninrenin inhibitorhypertensiondog plasma reninInhibitorinhibitorinhibit

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