2. GPCR/G Protein
  3. Angiotensin Receptor
  4. A 779

A 779 is a specific antagonist of G-protein coupled receptor (Mas receptor), which is an Ang1-7 receptor distinct from the classical AngII.

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A 779 Chemical Structure

A 779 Chemical Structure

CAS No. : 159432-28-7

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Based on 12 publication(s) in Google Scholar

A 779 Related Antibodies

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Description

A 779 is a specific antagonist of G-protein coupled receptor (Mas receptor), which is an Ang1-7 receptor distinct from the classical AngII.

IC50 & Target

AT2 Receptor

 

AT1 Receptor

 

In Vitro

A-779 inhibits the effect of Ang-(1-7), which suppresses the proliferating cell nuclear antigen (PCNA) protein expression up-regulated by Ang II, but A-779 alone has no effect to induce proliferation and migration of VSMCs. Pretreatment with Ang-(1-7) significantly retards Ang II-induced inflammatory responses of VSMCs associated with up-regulated MCP-1, VCAM-1 and IL-1β expressions, and this effect of Ang-(1-7) is blocked by A-779. But A-779 alone has no effect to induce inflammatory response of VSMCs. Pretreatment VSMCs with Ang-(1-7) for 5 min significantly inhibits Akt and ERK1/2 phosphorylation induced by Ang II, and this effect is also blocked by A-779, but alone has no effect to induce phosphorylation of Akt and ERK1/2 in VSMCs[3].

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

A 779 Related Antibodies
In Vivo

Infusion of Ang(1-7) and A-779 (400 ng/kg/min, s.c.) alone or combined for 6 weeks does not prevent uterus atrophy or inhibit the body weight gain of OVX rats. A-779 markedly elevates serum bone specific alkaline phosphatase (BALP), telopeptides of collagen type I (CTX), tartarate resistant acid phosphatase (TRAcP 5b), osteocalcin (OC) and urinary deoxypyridinoline (DPD). Infusion of Ang(1-7) and/or A-779 does not significantly change serum minerals concentrations in sham or OVX groups. A-779 in the OVX animals does not change AngII, Ang(1-7), AT1R, AT2R, ACE, ACE-2, Mas receptor, RANKL and OPG proteins expressions in relation to OVX group, while AngII (P < 0.05), AT1R (P < 0.05), ACE (P < 0.01) and RANKL (P < 0.01) expressions are significantly higher and Ang(1-7), AT2R, ACE-2, MasR and OPG are significantly (P < 0.01) lower than sham group. Blocking of the G-protein coupled receptor (Mas) by A-779 markedly abolishes Ang(1-7) favorable effects on bone health suggesting the vital role of Mas receptor in mediating Ang(1-7) osteo-protective effects[1]. Inhibition of Ang1-7 cascade by A-779 (400 ng/kg/min) significantly eradicates captopril protective effects on bone metabolism, mineralization and micro-structure. A-779 also restores OVX effects on RANKL expression and ACE-1/AngII/AT1R cascade and down-regulates OPG expression and ACE-2/Ang1-7/Mas pathway[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

872.97

Formula

C39H60N12O11
CAS No.
Appearance

Solid

Color

White to off-white

Sequence

Asp-Arg-Val-Tyr-Ile-His-{d-Ala}
Sequence Shortening

DRVYIH-{d-Ala}
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (114.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1455 mL 5.7276 mL 11.4551 mL
5 mM 0.2291 mL 1.1455 mL 2.2910 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.59%

COA (252 KB) LCMS (263 KB)

Handling Instructions (2659 KB)
References
Animal Administration
[1]

A bilateral OVX operation is use to induce postmenopausal osteoporosis in female Wistar albino rats. The animals are generally anesthetized using single IP injection of ketamine + xylazine combination (80 mg/kg and 5 mg/kg; respectively). After ligation, the ovaries are excised from a longitudinal incision made on the dorsolateral body region. Sham rats have the same procedure without the ligation and excision. The risk of postoperative infection is eliminated by applying fusidic acid topical antibiotic cream twice weekly for 4 weeks. Following the sham and OVX operations, animals are divided into eight groups (n = 8/group) including, Sham, Sham + Ang(1-7), Sham + A-779, Sham + Ang(1-7)+A-779, OVX, OVX + Ang(1-7), OVX + A-779 and OVX + Ang(1-7)+A-779. Eight weeks following sham and OVX operations, osmotic pumps are implanted subcutaneously to deliver Ang(1-7) (200 ng/kg/min), A-779 (400 ng/kg/min) or a mixture of Ang(1-7) and A-779 (200 ng/kg/min and 400 ng/kg/min; respectively) for 6 consecutive weeks. Body weights of all animals are monitored and recorded at the beginning and every week throughout the study. Animals' general health is maintained during periods of treatments. At the end of treatments periods, animals are placed fasting in metabolic cages for 16 hr and urine samples are collected and frozen at −70°C. Then, the blood samples are collected by cardiac puncture under ketamine + xylazine anesthesia and serum samples are obtain by centrifugation at 4000 RPM to. Animals are then sacrificed by decapitation and the uterine tissues and femoral bones are removed and cleaned. Uterine tissues are cleaned from fats and the wet weights are determined directly and expressed as g/100 g body weight. In each rat, both femurs are removed and cleaned from soft tissues. The left femoral bone samples are frozen at −70°C until analyzed, while the right femoral bones are kept in 10% formalin for mico-CT and minerals analysis.

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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.1455 mL 5.7276 mL 11.4551 mL 28.6379 mL
5 mM 0.2291 mL 1.1455 mL 2.2910 mL 5.7276 mL
10 mM 0.1146 mL 0.5728 mL 1.1455 mL 2.8638 mL
15 mM 0.0764 mL 0.3818 mL 0.7637 mL 1.9092 mL
20 mM 0.0573 mL 0.2864 mL 0.5728 mL 1.4319 mL
25 mM 0.0458 mL 0.2291 mL 0.4582 mL 1.1455 mL
30 mM 0.0382 mL 0.1909 mL 0.3818 mL 0.9546 mL
40 mM 0.0286 mL 0.1432 mL 0.2864 mL 0.7159 mL
50 mM 0.0229 mL 0.1146 mL 0.2291 mL 0.5728 mL
60 mM 0.0191 mL 0.0955 mL 0.1909 mL 0.4773 mL
80 mM 0.0143 mL 0.0716 mL 0.1432 mL 0.3580 mL
100 mM 0.0115 mL 0.0573 mL 0.1146 mL 0.2864 mL
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A 779 Related Classifications

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:

A 779159432-28-7A779A-779Angiotensin ReceptorInhibitorinhibitorinhibit

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