2. GPCR/G Protein Apoptosis
  3. Endothelin Receptor Apoptosis
  4. A-192621

A-192621 is a potent, nonpeptide, orally active and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. The selectivity of A-192621 is 636-fold higher than ETA (IC50 of 4280 nM and Ki of 5600 nM). A-192621 promotes apoptosis in PASMCs. A-192621 alos causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level.

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A-192621 Chemical Structure

A-192621 Chemical Structure

CAS No. : 195529-54-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

A-192621 Related Antibodies

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Description

A-192621 is a potent, nonpeptide, orally active and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. The selectivity of A-192621 is 636-fold higher than ETA (IC50 of 4280 nM and Ki of 5600 nM). A-192621 promotes apoptosis in PASMCs. A-192621 alos causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level[1][2][3].

IC50 & Target[1]

ETB

4.5 nM (IC50)

ETB

8.8 nM (Ki)

ETA

4280 nM (IC50)

ETA

5600 nM (Ki)

Cellular Effect
Cell Line Type Value Description References
CHO IC50
0.65 nM
Compound: 38
Antagonistic activity was measured by ET receptor mediated hydrolysis of inositol phosphates
Antagonistic activity was measured by ET receptor mediated hydrolysis of inositol phosphates
[PMID: 10479298]
In Vitro

A-192621 (1-100 μM; 48 hours; PASMCs) treatment markedly reduces the cell viability of PASMCs in a dose-dependent manner[2].
A-192621 (1-100 μM; 48 hours; PASMCs) treatment significantly increases the caspase-3/7 activity and cleaved caspase-3 expression in PASMCs. A-192621 induces apoptosis in a dose-dependent manner and increases the cells' susceptibility to apoptosis by Doxorubicin treatment[2].

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

A-192621 Related Antibodies

Cell Viability Assay[2]

Cell Line: Pulmonary arterial smooth muscle cells (PASMCs) with Doxorubicin
Concentration: 1 μM, 10 μM, 50 μM, 100 μM
Incubation Time: 72 hours
Result: The viability of PASMCs was significantly decreased in a dose-dependent manner.

Western Blot Analysis[2]

Cell Line: Pulmonary arterial smooth muscle cells (PASMCs) with Doxorubicin
Concentration: 1 μM, 10 μM, 100 μM
Incubation Time: 72 hours
Result: The caspase-3/7 activity in PASMCs was significantly increased in a dose-dependent manner.
In Vivo

A-192621 (30-100 mg/kg; oral administration; daily; for 3 days; male Sprague-Dawley rats) treatment inhibits both dilatory and pressor responses induced by S6c mediated by ETB with an ED50 value of 30 mg/kg, and failed to inhibit the ET-1-induced pressor response mediated by ETA. A-192621 alone causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level in the conscious normotensive rat[3].

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

Animal Model: Male Sprague-Dawley rats (250-350 g)[3]
Dosage: 30 mg/kg 100 mg/kg
Administration: Oral administration; daily; for 3 days
Result: Inhibited both dilatory and pressor responses induced by S6c mediated by ETB with an ED50value of 30 mg/kg.
Molecular Weight

558.66

Formula

C33H38N2O6
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@H]1[C@H](C2=CC=C(OCCC)C=C2)N(CC(NC3=C(CC)C=CC=C3CC)=O)C[C@@H]1C4=CC=C(OCO5)C5=C4)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (179.00 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7900 mL 8.9500 mL 17.9000 mL
5 mM 0.3580 mL 1.7900 mL 3.5800 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 2.5 mg/mL (4.47 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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(per animal)

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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+
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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.
Purity & Documentation

Purity: 99.85%

SDS (252 KB)

COA (258 KB) LCMS (105 KB)

Handling Instructions (2659 KB)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7900 mL 8.9500 mL 17.9000 mL 44.7499 mL
5 mM 0.3580 mL 1.7900 mL 3.5800 mL 8.9500 mL
10 mM 0.1790 mL 0.8950 mL 1.7900 mL 4.4750 mL
15 mM 0.1193 mL 0.5967 mL 1.1933 mL 2.9833 mL
20 mM 0.0895 mL 0.4475 mL 0.8950 mL 2.2375 mL
25 mM 0.0716 mL 0.3580 mL 0.7160 mL 1.7900 mL
30 mM 0.0597 mL 0.2983 mL 0.5967 mL 1.4917 mL
40 mM 0.0447 mL 0.2237 mL 0.4475 mL 1.1187 mL
50 mM 0.0358 mL 0.1790 mL 0.3580 mL 0.8950 mL
60 mM 0.0298 mL 0.1492 mL 0.2983 mL 0.7458 mL
80 mM 0.0224 mL 0.1119 mL 0.2237 mL 0.5594 mL
100 mM 0.0179 mL 0.0895 mL 0.1790 mL 0.4475 mL
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A-192621 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-192621195529-54-5A192621A 192621Endothelin ReceptorApoptosisCaspase-3apoptosisDoxorubicinvascularremodelingbloodpressureET-1Inhibitorinhibitorinhibit

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