DMP 811
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.
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- CAS. Nr.: 139964-19-5
- Formel: C23H24N6O2
- Molecular Weight:416.49
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
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AT1 Receptor 6 nM (IC50) |
AT2 Receptor >10 μM (IC50) |
DMP 811 (0.1 nM-10 μM) selectively binds to AT1 receptors in rat adrenal cortical microsomes with IC50 values of 6 nM (without BSA) and 0.1 μM (with BSA) and shows low affinity for AT2 receptors in rat adrenal medullary membranes (IC50 >10 μM)[1].
DMP 811 (1-100 nM; 15 min) noncompetitively inhibits Ang II (HY-13948)-induced contraction in isolated rabbit aorta[1].
DMP 811 (10 nM; 15 min) completely and selectively inhibits Ang II-induced contraction in guinea pig ileum without affecting responses to acetylcholine, serotonin, or bradykinin[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | AUC | Cmax | Tmax | F | CL | Vss | T1/2 |
|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 3 mg/kg | i.v. | 40.3 μg·h/mL | 42.2 μg/mL | 0.083 h | / | 0.078 L/h/kg | 0.19 L/kg | 3.0 h |
| Rat[1] | 10 mg/kg | i.v. | 176 μg·h/mL | 154 μg/mL | 0.083 h | / | 0.062 L/h/kg | 0.17 L/kg | 3.7 h |
| Rat[1] | 10 (solution) mg/kg | p.o. | 12.6 μg·h/mL | 1.52 μg/mL | 1.8 h | 7.2 % | / | / | / |
| Rat[1] | 10 (suspension) mg/kg | p.o. | 11.2 μg·h/mL | 1.37 μg/mL | 1.5 h | 6.4 % | / | / | / |
| Rat[1] | 3 (suspension) mg/kg | p.o. | 3.7 μg·h/mL | 0.58 μg/mL | 2.0 h | 9.2 % | / | / | / |
| Dog[1] | 3 mg/kg | i.v. | 15.4 μg·h/mL | / | / | / | 0.20 L/h/kg | 0.38 L/h | 6.6 h |
| Dog[1] | 10 (solution) mg/kg | p.o. | 14.81 μg·h/mL | 4.45 μg/mL | 0.75 h | 29.5 % | / | / | / |
| Dog[1] | 10 (capsule) mg/kg | p.o. | 6.55 μg·h/mL | 0.99 μg/mL | 2.7 h | 13.2 % | / | / | / |
| Dog[1] | 3 (capsule) mg/kg | p.o. | 2.08 μg·h/mL | 0.49 μg/mL | 1.5 h | 13.5 % | / | / | / |
DMP 811 (0.003-0.3 mg/kg; i.g.; single dose) reduces blood pressure in renal hypertensive rats with an oral ED30 of 0.005 mg/kg[1].
DMP 811 (0.3 and 1 mg/kg; i.g.; single dose) reduces blood pressure in Furosemide (HY-B0135)-treated dogs[1].
DMP 811 (0.03-1 mg/kg; i.v.; single dose) inhibits Ang II (HY-13948)-induced pressor responses in pithed rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male CD Sprague-Dawley rats (300-400 g) with renal hypertensive
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Dosage:0.003-0.1 mg/kg
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Administration:i.v.; single dose
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Result:Caused a dose-dependent decrease in blood pressure with an ED30 of 0.005 mg/kg.
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Animal Model:Male CD Sprague-Dawley rats (300-400 g) with renal hypertensive[1]
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Dosage:0.03-0.3 mg/kg
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Administration:p.o.; single dose
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Result:Caused a dose-dependent decrease in blood pressure with an oral ED30 of 0.03 mg/kg.
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Animal Model:Mongrel dogs (8-13 kg) treated with Furosemide, and with elevated plasma renin activity)[1]
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Dosage:0.3, 1 mg/kg
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Administration:i.g.; single dose
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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.
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Animal Model:Male CD Sprague-Dawley rats (300-400 g) pithed normotensive model[1]
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Dosage:0.03, 0.1, 0.3, 1 mg/kg
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Administration:i.v.; single dose
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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.
Chemical Information
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CAS. Nr. 139964-19-5
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Molecular Weight 416.49
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Formel C23H24N6O2
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SMILES
O=C(O)C1=C(N=C(N1CC=2C=CC(=CC2)C=3C=CC=CC3C4=NN=NN4)CCC)CC
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Wong PC, et al. Pharmacology and pharmacokinetics of a novel nonpeptide angiotensin II receptor antagonist--DMP 811. Clin Exp Hypertens. 1995;17(8):1233-1256. [Content Brief]
[3]. Agra AM, et al. High-performance liquid chromatographic determination of a potent AII receptor antagonist (DMP 811) in plasma. J Chromatogr. 1993 Oct 29;620(2):205-9. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
DMP 811 Related Classifications
HY-180401 Related Classifications
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- DMP 811
- 139964-19-5
- DMP811
- DMP-811
- Angiotensin Receptor
- angiotensin II subtype receptor AT1
- furosemide-treated dogs
- conscious normotensive CD Sprague-Dawley rats
- guinea pig ileum
- conscious renal hypertensive rats
- rat adrenal medullary membranes
- Mongrel dogs
- isolated rabbit aorta
- CD Sprague-Dawley rats
- AT2
- hypertension
- AT1
- pithed CD Sprague-Dawley rats
- rat adrenal cortical microsomes
- Inhibitor
- inhibitor
- inhibit