2. GPCR/G Protein
  3. Angiotensin Receptor
  4. DMP 811

DMP 811 是一种强效、口服有效且选择性作用于血管紧张素 II 亚型受体 AT1 的拮抗剂。DMP 811 对 AT1 (IC50 = 6 nM) 表现出高度选择性，对 AT2 的选择性较低 (IC50 > 10 μM)。DMP 811 在大鼠和狗中均表现出强效的抗高血压活性。DMP 811 可用于高血压相关研究。

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DMP 811

DMP 811 Chemical Structure

CAS No. : 139964-19-5

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DMP 811 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DMP 811 is a potent, orally active and selective angiotensin II subtype receptor AT1 antagonist. DMP 811 exhibits selectivity for AT1 (IC50 = 6 nM) over AT2 (IC50 >10 μM). DMP 811 exhibits potent antihypertensive activity in rats and dogs. DMP 811 can be used for the research of hypertension[1][2][3].

IC50 & Target[1]

AT1 Receptor

6 nM (IC50)

AT2 Receptor

>10 μM (IC50)

体外研究
(In Vitro)

DMP 811 (0.1 nM-10 μM) 可选择性结合大鼠肾上腺皮质微粒体中的 AT1 受体，其 IC50 值在无 BSA 时为 6 nM，有 BSA 时为 0.1 μM；而对大鼠肾上腺髓质膜中的 AT2 受体亲和力较低 (IC50 >10 μM) [1]。
DMP 811 (1-100 nM；15 分钟) 以非竞争性方式抑制离体兔主动脉中 Ang II (HY-13948) 诱导的收缩[1]。
DMP 811 (10 nM；15 分钟) 可完全且选择性抑制血管紧张素 II 诱导的豚鼠回肠收缩，而不影响对乙酰胆碱、血清素或缓激肽引起的反应[1]。

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

DMP 811 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Rat[3] 3 mg/kg i.v. AUC 40.3 μg·h/mL
Rat[3] 3 mg/kg i.v. CL 0.078 L/h/kg
Rat[3] 3 mg/kg i.v. Vss 0.19 L/kg
Rat[3] 3 mg/kg i.v. T1/2 3.0 h
Rat[3] 3 mg/kg i.v. Cmax 42.2 μg/mL
Rat[3] 3 mg/kg i.v. Tmax 0.083 h
Rat[3] 10 mg/kg i.v. AUC 176 μg·h/mL
Rat[3] 10 mg/kg i.v. CL 0.062 L/h/kg
Rat[3] 10 mg/kg i.v. Vss 0.17 L/kg
Rat[3] 10 mg/kg i.v. T1/2 3.7 h
Rat[3] 10 mg/kg i.v. Cmax 154 μg/mL
Rat[3] 10 mg/kg i.v. Tmax 0.083 h
Rat[3] 10 (solution) mg/kg p.o. AUC 12.6 μg·h/mL
Rat[3] 10 (solution) mg/kg p.o. Cmax 1.52 μg/mL
Rat[3] 10 (solution) mg/kg p.o. Tmax 1.8 h
Rat[3] 10 (solution) mg/kg p.o. F 7.2 %
Rat[3] 10 (suspension) mg/kg p.o. AUC 11.2 μg·h/mL
Rat[3] 10 (suspension) mg/kg p.o. Cmax 1.37 μg/mL
Rat[3] 10 (suspension) mg/kg p.o. Tmax 1.5 h
Rat[3] 10 (suspension) mg/kg p.o. F 6.4 %
Rat[3] 3 (suspension) mg/kg p.o. AUC 3.7 μg·h/mL
Rat[3] 3 (suspension) mg/kg p.o. Cmax 0.58 μg/mL
Rat[3] 3 (suspension) mg/kg p.o. Tmax 2.0 h
Rat[3] 3 (suspension) mg/kg p.o. F 9.2 %
Dog[3] 3 mg/kg i.v. AUC 15.4 μg·h/mL
Dog[3] 3 mg/kg i.v. CL 0.20 L/h/kg
Dog[3] 3 mg/kg i.v. Vss 0.38 L/h
Dog[3] 3 mg/kg i.v. T1/2 6.6 h
Dog[3] 10 (solution) mg/kg p.o. AUC 14.81 μg·h/mL
Dog[3] 10 (solution) mg/kg p.o. Cmax 4.45 μg/mL
Dog[3] 10 (solution) mg/kg p.o. Tmax 0.75 h
Dog[3] 10 (solution) mg/kg p.o. F 29.5 %
Dog[3] 10 (capsule) mg/kg p.o. AUC 6.55 μg·h/mL
Dog[3] 10 (capsule) mg/kg p.o. Cmax 0.99 μg/mL
Dog[3] 10 (capsule) mg/kg p.o. Tmax 2.7 h
Dog[3] 10 (capsule) mg/kg p.o. F 13.2 %
Dog[3] 3 (capsule) mg/kg p.o. AUC 2.08 μg·h/mL
Dog[3] 3 (capsule) mg/kg p.o. Cmax 0.49 μg/mL
Dog[3] 3 (capsule) mg/kg p.o. Tmax 1.5 h
Dog[3] 3 (capsule) mg/kg p.o. F 13.5 %
体内研究
(In Vivo)

DMP 811 (0.003-0.1 mg/kg；静脉注射；单次给药) 可降低肾性高血压大鼠的血压，其静注 ED30 为 0.005 mg/kg[1]。
DMP 811 (0.003-0.3 mg/kg；灌胃；单次给药) 可降低肾性高血压大鼠的血压，其口服 ED30 为 0.005 mg/kg[1]。
DMP 811 (0.3 和 1 mg/kg；灌胃；单次给药) 可降低 Furosemide (HY-B0135) 处理犬的血压[1]。
DMP 811 (0.03-1 mg/kg；静脉注射；单次给药) 可抑制去皮层大鼠中由 Ang II (HY-13948) 诱导的升压反应[1]。

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

Animal Model: Male CD Sprague-Dawley rats (300-400 g) with renal hypertensive
[1]
Dosage: 0.003-0.1 mg/kg
Administration: i.v.; single dose
Result: Caused a dose-dependent decrease in blood pressure with an ED30 of 0.005 mg/kg.
Animal Model: Male CD Sprague-Dawley rats (300-400 g) with renal hypertensive[1]
Dosage: 0.03-0.3 mg/kg
Administration: p.o.; single dose
Result: Caused a dose-dependent decrease in blood pressure with an oral ED30 of 0.03 mg/kg.
Animal Model: Mongrel dogs (8-13 kg) treated with Furosemide, and with elevated plasma renin activity)[1]
Dosage: 0.3, 1 mg/kg
Administration: i.g.; single dose
Result: Caused a dose-dependent decrease in blood pressure.
Decreased blood pressure by about 30% with a duration greater than 6 h at 1 mg/kg.
Animal Model: Male CD Sprague-Dawley rats (300-400 g) pithed normotensive model[1]
Dosage: 0.03, 0.1, 0.3, 1 mg/kg
Administration: i.v.; single dose
Result: Shifted the log dose-pressor response curve for Ang II to the right nonparallelly and reduced the maximal Ang II response.
Significantly lowered diastolic blood pressure at 0.03-1 mg/kg.
Did not alter the norepinephrine dose-pressor curve at 1 mg/kg.
分子量

416.49

Formula

C23H24N6O2
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

DMP 811 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

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Keywords:

DMP 811139964-19-5DMP811DMP-811Angiotensin Receptorangiotensin II subtype receptor AT1furosemide-treated dogsconscious normotensive CD Sprague-Dawley ratsguinea pig ileumconscious renal hypertensive ratsrat adrenal medullary membranesMongrel dogsisolated rabbit aortaCD Sprague-Dawley ratsAT2hypertensionAT1pithed CD Sprague-Dawley ratsrat adrenal cortical microsomesInhibitorinhibitorinhibit

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