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

For research use only. We do not sell to patients.

DMP 811

DMP 811 Chemical Structure

CAS No. : 139964-19-5

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

DMP 811 Related Antibodies

Top Publications Citing Use of Products

View All Angiotensin Receptor Isoform Specific Products:

View All Isoforms
AT1 Receptor AT2 Receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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)

In Vitro

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.

DMP 811 Related Antibodies
Parmacokinetics
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 % / / /
In Vivo

DMP 811 (0.003-0.1 mg/kg; i.v.; single dose) reduces blood pressure in renal hypertensive rats with an ED30 of 0.005 mg/kg[1].
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.

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.
Molecular Weight

416.49

Formula

C23H24N6O2
CAS No.
SMILES

O=C(O)C1=C(N=C(N1CC=2C=CC(=CC2)C=3C=CC=CC3C4=NN=NN4)CCC)CC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

DMP 811 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

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

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
DMP 811
Cat. No.:
HY-180401
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.