2. Metabolic Enzyme/Protease
  3. Angiotensin-converting Enzyme (ACE)
  4. CV 5975

CV 5975 是一种口服血管紧张素转换酶 (ACE) 竞争性抑制剂，其对兔肺 ACE 的 IC50 为 3.1 nM，Ki 值为 2.6 nM。CV 5975 可抑制血浆、主动脉、肾脏和脑组织中的 ACE，重复给药会增强抑制作用。CV 5975 可抑制 Angiotensin I (HY-P1032) 诱导的升压反应和回肠收缩，并增强缓激肽诱导的回肠收缩和降压反应。CV 5975 可通过非 ACE 依赖机制降低血压，在多种高血压和正常血压动物模型中具有持续作用，重复给药或与 Hydrochlorothiazide (HY-B0252) 联合给药可增强其作用。CV 5975 可用于高血压的相关研究。

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CV 5975

CV 5975 Chemical Structure

CAS No. : 100277-62-1

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CV 5975 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

CV 5975 is an orally active angiotensin converting enzyme (ACE) competitive inhibitor with a rabbit lung ACE IC50 of 3.1 nM and Ki values of 2.6 nM. CV 5975 inhibits ACE in plasma, aorta, kidney, and brain, intensifying inhibition with repeated administration. CV 5975 inhibits Angiotensin I (HY-P1032)-induced pressor responses and ileum contraction, and augments bradykinin-induced ileum contraction and depressor responses. CV 5975 reduces blood pressure via ACE-independent mechanisms, with sustained action across multiple hypertensive and normotensive animal models, intensified by repeated dosing or Hydrochlorothiazide (HY-B0252) co-administration. CV 5975 can be used for the research of hypertension[1][2][3][4].

IC50 & Target[1]

ACE

 

体外研究
(In Vitro)

CV 5975 (40 克；3.5-29 小时) 利用脂肪酶 PN 进行的化学酶动力学拆分可生成对映体过量值为 64%的 (R)-4，后者经甲磺酰化、SN2 反应和脱保护反应转化为 CV-5975，以 (R)-4 计总收率为 25%[1]。
CV 5975 (40 克；48 小时) 经 Baker's yeast 介导的 α-氧代酯 3 不对称还原反应可生成 (R)-4，其对映体过量值为 61%，产率为 46%，适用于 CV-5975 的合成[1]。
CV 5975 (10 nM；60 分钟) 可强效抑制白化雄性兔肺来源的粗制血管紧张素转换酶，其 IC50 为 3.1 × 10-9 M，效力远高于其三种立体异构体[2]。
CV 5975 (20 分钟) 可强效且竞争性地抑制部分纯化的兔肺血管紧张素转换酶 (ACE)，其 IC50 为 3.1 nM，Ki 为 2.6 nM，高亲和力稳态 Ki* 为 4.4 pM[4]。

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

CV 5975 相关抗体:
体内研究
(In Vivo)

CV 5975 (0.3-3 mg/kg；静脉注射或口服；单次给药) 可强效且持久地抑制雄性 Sprague-Dawley 大鼠中 Angiotensin I 诱导的升压反应：在静脉给予 0.3 mg/kg 后，抑制率维持在 90%以上至少 2 小时；在口服给予 3 mg/kg 后，抑制时长可达 7 小时，是受试哌啶基衍生物中作用持续时间最长的一种[2]。
CV 5975 (10 mg/kg；口服；单次给药) 对正常血压的 Wistar Kyoto 大鼠产生轻微但显著的降压作用，该作用可持续 10 小时[3]。
CV 5975 (1-10 mg/kg；口服；每天给药；连续 2 周) 在自发性高血压大鼠中呈现剂量依赖性的持续性降压作用；重复给药时，其效力和作用时长均增强，同时可产生显著的全组织 ACE 抑制作用，且该作用与血压降低相关[3]。
CV 5975 (1-10 mg/kg；口服；单次给药) 可在双肾一夹肾性高血压大鼠中产生强效、持久且呈剂量依赖性的降压作用，在 10 mg/kg 口服剂量下，血压最大降幅达 65 mmHg，且该效果可持续 24 小时以上[3]。
CV 5975 (1-10 mg/kg；口服；单次给药) 在单肾单夹型肾性高血压大鼠中发挥剂量依赖性降压作用，10 mg/kg 口服剂量下可使血压显著降低并持续 10 小时以上[3]。
CV 5975 (1-10 mg/kg；口服；单次给药；连续 2 周每日给药) 在低肾素型 DOCA/盐高血压大鼠中产生轻度、剂量依赖性的降压作用，且每日重复给药未增强疗效[3]。
CV 5975 (0.3-1 mg/kg；口服；单次给药) 可在两肾一夹型肾性高血压犬中产生持久的降压作用，在 1 mg/kg 剂量下可使收缩压和舒张压降低约 40 mmHg[3]。
CV 5975 (0.3-1 mg/kg；口服) 可在 0.3 和 1 mg/kg 口服剂量下强效抑制正常血压犬中 Angiotensin I 诱导的升压反应，抑制率超过 90%[4]。

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

Animal Model: Sprague-Dawley (male, 300-400 g)[2]
Dosage: 0.3 mg/kg (i.v.); 3 mg/kg (p.o.)
Administration: i.v. or p.o.; single dose
Result: Inhibited angiotensin I-induced pressor responses by 96% at 10 minutes, 99% at 30 minutes, 93% at 60 minutes, and 91% at 120 minutes after intravenous 0.3 mg/kg administration.
Exhibited the longest duration of ACE inhibition among tested piperidyl derivatives, with recovery to 50% of control taking over 4 hours after intravenous 0.3 mg/kg administration.
Inhibited angiotensin I-induced pressor responses by 70% at 20 minutes, 84% at 1 hour, 91% at 3 hours, 88% at 5 hours, and 84% at 7 hours after oral 3 mg/kg administration.
Animal Model: Wistar Kyoto rats (male, 20 to 22 weeks old)[3]
Dosage: 10 mg/kg
Administration: p.o.; single dose
Result: Slightly but significantly reduced mean arterial blood pressure, with maximum reductions of 9 mmHg at 5 hr, 8 mmHg at 7 hr, and 10 mmHg at 10 hr.
Returned blood pressure to pre-drug levels by 24 hr post-administration.
Animal Model: Spontaneously hypertensive rats (male, 20 to 22 weeks old)[3]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: p.o.; single dose; daily for 2 weeks
Result: Reduced blood pressure dose-dependently by 10 to 35 mmHg, with maximum effects at 5 to 10 hr that lasted more than 24 hr.
Intensified antihypertensive potency and duration upon repeated dosing, with maximum effects observed on day 7; 1 week after treatment cessation, blood pressure remained significantly lower than controls (202 mmHg at 1 mg/kg, 203 mmHg at 3 mg/kg, 202 mmHg at 10 mg/kg) and returned to control levels by 2 weeks post-cessation.
Inhibited ACE activity in all tested tissues (plasma, aorta, kidney, lung, brain) after repeated daily dosing for 1 week.
Animal Model: Wistar rats (male, 6 weeks old initially, used 4 to 6 weeks after 2-kidney, 1-clip renal hypertension surgery, systolic blood pressure 160 to 240 mmHg)[3]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: p.o.; single dose
Result: Caused a dose-related, marked, sustained decrease in blood pressure; the maximum effect of ~65 mmHg was seen at 7 to 10 hr post-dose, and blood pressure remained below pre-drug levels for more than 24 hr.
Animal Model: Wistar rats (male, 6 weeks old initially, used 4 to 6 weeks after 1-kidney, 1-clip renal hypertension surgery, systolic blood pressure 160 to 240 mmHg)[3]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: p.o.; single dose
Result: Reduced blood pressure dose-dependently; at 10 mg/kg, the effect was observed from 3 hr post-dose and blood pressure remained lower than control levels for more than 10 hr.
Animal Model: Wistar rats (male, 6 weeks old initially, used 4 to 6 weeks after hyporeninemic DOCA/salt hypertension surgery, systolic blood pressure 160 to 240 mmHg)[3]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration: p.o.; single dose; daily for 2 weeks
Result: Induced a mild, consistent antihypertensive effect after single administration.
Reduced arterial blood pressure in a dose-related manner with repeated daily dosing, with no intensification of effect; the antihypertensive effect disappeared within 24 hr after each dose cessation.
Animal Model: Beagle dogs (male, 13 to 16 kg, used 2 to 5 weeks after 2-kidney, 1-clip renal hypertension surgery)[3]
Dosage: 0.3 mg/kg; 1 mg/kg
Administration: p.o.; single dose
Result: Induced a modest, long-lasting reduction in systemic blood pressure within 1 hr of administration, with effects persisting for more than 10 hr.
Lowered both systolic and diastolic blood pressure by about 40 mmHg at 1 mg/kg, and heart rate tended to increase (not statistically significant).
Animal Model: Sprague-Dawley rats (male, 300-400 g)[4]
Dosage: 0.03 mg/kg (i.v.); 0.3 mg/kg (i.v.); 3 mg/kg (p.o.); 10 mg/kg (p.o.)
Administration: i.v. or p.o.
Result: Induced maximum inhibition of angiotensin I (A-I) pressor response at 5 min, with longer lasting effects than enalaprilat at 0.03 mg/kg i.v.
Had a half-time of recovery (T1/2) of about 5 hr, and an ID50 of 0.07 mg/kg i.v. over a 7 hr observation period at 0.3 mg/kg i.v.
Augmented bradykinin (BK)-induced depressor response to -31.6 mmHg at 1 hr, -32.0 mmHg at 3 hr, -28.6 mmHg at 5 hr, and -24.8 mmHg at 7 hr at 3 mg/kg p.o.
Had an inhibitory effect on A-I pressor response lasting over 24 hr, with an ID50 of 1.8 mg/kg p.o. over a 24 hr observation period at 10 mg/kg p.o.
Animal Model: Beagle dogs (either sex, 13-15 kg)[4]
Dosage: 0.3 mg/kg; 1 mg/kg
Administration: p.o.
Result: Inhibited angiotensin I (A-I)-induced pressor response by over 90%, with prolonged inhibitory action compared to enalapril at 0.3 mg/kg p.o.
Inhibited A-I-induced pressor response by over 90%, with duration of action extending beyond 24 hr, while enalapril's effect at 1 mg/kg p.o. was no longer evident at 24 hr at 1 mg/kg p.o.
分子量

449.56

Formula

C22H31N3O5S
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

CV 5975 相关分类

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  • 稀释计算器

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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.

Keywords:

CV 5975100277-62-1CV5975CV-5975Angiotensin-converting Enzyme (ACE)kidneyangiotensin Iplasmahypertensionaortabradykininrabbit lung ACEbrainspontaneously hypertensive ratsangiotensin converting enzymeInhibitorinhibitorinhibit

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