2. GPCR/G Protein
  3. Endothelin Receptor
  4. Avosentan

Avosentan (Ro 67-0565; SPP-301) is an orally active endothelin (ETA) receptor antagonist. Avosentan can block the ETA receptor, thereby reducing vascular contraction and exerting a renal protective effect. Avosentan inhibits vascular contraction caused by ET-1 and alleviates the reduction in retinal and optic nerve head blood flow induced by it, lowering intraocular pressure in the glaucoma monkey model. Avosentan non-specifically blocks ETB receptors at high doses, inhibiting ETB-mediated diuresis and natriuresis, and may cause fluid retention. Avosentan can be used to reduce proteinuria with diabetic nephropathy, but induces significant fluid overload and congestive heart failure.

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Avosentan

Avosentan Estructura química

No. CAS : 290815-26-8

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10 mM * 1 mL in DMSO
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Avosentan Related Antibodies

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Descripciòn

Avosentan (Ro 67-0565; SPP-301) is an orally active endothelin (ETA) receptor antagonist. Avosentan can block the ETA receptor, thereby reducing vascular contraction and exerting a renal protective effect. Avosentan inhibits vascular contraction caused by ET-1 and alleviates the reduction in retinal and optic nerve head blood flow induced by it, lowering intraocular pressure in the glaucoma monkey model. Avosentan non-specifically blocks ETB receptors at high doses, inhibiting ETB-mediated diuresis and natriuresis, and may cause fluid retention. Avosentan can be used to reduce proteinuria with diabetic nephropathy, but induces significant fluid overload and congestive heart failure[1][2][3][4].

IC50 & Target[1][2][3][4]

ETA

 

Cellular Effect
Cell Line Type Value Description References
CHO IC50
1.4 nM
Compound: 25; Avosentan
Displacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cells
Displacement of 125I-ET1 from ETA receptor (unknown origin) expressed in CHO cells
[PMID: 27321813]
In Vitro

Avosentan (0.01-1 μM, 30 min) has no direct effect on quiescent vessels but has a strong inhibitory effect on the endothelin-1 induced contractions in isolated porcine ciliary arteries and shows stronger effect in endothelium-denuded vessels[2].

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

Avosentan Related Antibodies
In Vivo

Avosentan (Incremental doses of 0.003-3 mg/kg, i.v., at 30-min intervals) inhibits ETB receptor-mediated effects and consequently leads to acute fluid retention in anesthetized rats[1].
Avosentan (0.1-100 mg/kg, i.g., single dose or once daily for 5 weeks) is protective in hypertensive nephropathy at doses not causing fluid retention in rats[3].
Avosentan (0.003%-0.3%, topically applied to the glaucomatous eye, twice daily for 5 days) reduces intraocular pressure (IOP) in glaucomatous monkey eyes in a dose-dependent manner[4].

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

Animal Model: Renal excretory function assay established male Sprague-Dawley (SD) rats (12-14 weeks)[1]
Dosage: Incremental doses of 0.003, 0.03, 3 mg/kg, BQ-788 (HY-15894A) was administered 30 min after the highest dose
Administration: Intravenous administration (i.v.), at 30-min intervals
Result: Decreased urine output and fractional excretion of water in a concentration-dependent manner.
Returned sodium excretion to control values and slightly decreased mean arterial pressure (MAP)
Did not further decrease urine output or water excretion and was without effect.
Significantly decreased hematocrite.
Animal Model: Hypertensive nephropathy model established male double transgenic rats (dTGR) with human angiotensinogen and renin genes[3]
Dosage: 0.1, 1, 10, 100 mg/kg (single dose) and 10 mg/kg (long-term)
Administration: Oral gavage (i.g.), single dose or once daily for 5 weeks
Result: Caused 18.3% decrease in diuresis, 8.3% drop in hematocrit at 100 mg/kg and No significant fluid retention at 10 mg/kg.
Reduced proteinuria and significantly lowered the scores of renal glomerular fibrosis and other damages after 5-week treatments.
Significantly increased survival rate combined with Valsartan (HY-18204).
Animal Model: IOP model established in adult female cynomolgus monkeys each weighing 3-5 kg, in which glaucoma had been induced unilaterally by repeated diode laser photocoagulation of the mid-trabecular meshwork[4]
Dosage: Topically applied to the glaucomatous eye, twice daily for 5 days
Administration: Oral gavage (i.g.), single dose or once daily for 5 weeks
Result: Significantly reduced IOP only at 2 hrs after the first dose, and at 2 and 3 hrs after the 9th dose.
Produced a longer duration of action at 0.03% and 0.3% concentrations.
No anterior chamber cellular response was observed in any eye during the 5 days of treatment by slit-lamp examination.
Ensayo clínico
Peso molecular

479.51

Fòrmula

C23H21N5O5S
No. CAS
Appearance

Solid

Color

White to off-white

SMILES

COC1=C(OC(C(NS(C2=NC=C(C=C2)C)(=O)=O)=NC(C3=CC=NC=C3)=N4)=C4OC)C=CC=C1
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvente y solubilidad
In Vitro: 

DMSO : 6.67 mg/mL (13.91 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 2.0855 mL 10.4273 mL 20.8546 mL
5 mM 0.4171 mL 2.0855 mL 4.1709 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. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Calculadora de molaridad

  • Calculadora de dilución

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 0.67 mg/mL (1.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 0.67 mg/mL (1.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
Referencias

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. 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 2.0855 mL 10.4273 mL 20.8546 mL 52.1366 mL
5 mM 0.4171 mL 2.0855 mL 4.1709 mL 10.4273 mL
10 mM 0.2085 mL 1.0427 mL 2.0855 mL 5.2137 mL
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Avosentan Related Classifications

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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:

Avosentan290815-26-8Ro 67-0565 SPP-301SPP301SPP 301SPP-301Endothelin ReceptorHypertensive nephropathyEndothelin receptor antagonistAngiotensin receptor antagonistFluid retention Glaucoma monkeyIntraocular pressureIsolated ciliary arteriesMyographyInhibitorinhibitorinhibit

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