1. GPCR/G Protein
  2. Endothelin Receptor
  3. Edonentan

Edonentan (BMS 207940) is an antagonist for endothelin receptor (ETA receptor), with a Ki of 10 pM. Edonentan is metabolic stable, exhibits good pharmakokinetic characters in rats. Edonentan regulates the endothelin system, blocks the big Endothelin-induced pressor response in rats model.

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Edonentan

Edonentan Chemical Structure

CAS No. : 210891-04-6

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Based on 1 publication(s) in Google Scholar

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Description

Edonentan (BMS 207940) is an antagonist for endothelin receptor (ETA receptor), with a Ki of 10 pM. Edonentan is metabolic stable, exhibits good pharmakokinetic characters in rats. Edonentan regulates the endothelin system, blocks the big Endothelin-induced pressor response in rats model[1].

IC50 & Target

ETA

10 pM (Ki)

ETB

810 nM (Ki)

Molecular Weight

536.64

Formula

C28H32N4O5S

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

CC(C)(C)CC(N(CC1=CC(C2=NC=CO2)=CC=C1C3=CC=CC=C3S(=O)(NC4=NOC(C)=C4C)=O)C)=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 : 55 mg/mL (102.49 mM; Need ultrasonic and warming; 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 1.8634 mL 9.3172 mL 18.6345 mL
5 mM 0.3727 mL 1.8634 mL 3.7269 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.

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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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Volume (start)

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C2

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V2

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

Dosage

mg/kg

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g

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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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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 1.8634 mL 9.3172 mL 18.6345 mL 46.5862 mL
5 mM 0.3727 mL 1.8634 mL 3.7269 mL 9.3172 mL
10 mM 0.1863 mL 0.9317 mL 1.8634 mL 4.6586 mL
15 mM 0.1242 mL 0.6211 mL 1.2423 mL 3.1057 mL
20 mM 0.0932 mL 0.4659 mL 0.9317 mL 2.3293 mL
25 mM 0.0745 mL 0.3727 mL 0.7454 mL 1.8634 mL
30 mM 0.0621 mL 0.3106 mL 0.6211 mL 1.5529 mL
40 mM 0.0466 mL 0.2329 mL 0.4659 mL 1.1647 mL
50 mM 0.0373 mL 0.1863 mL 0.3727 mL 0.9317 mL
60 mM 0.0311 mL 0.1553 mL 0.3106 mL 0.7764 mL
80 mM 0.0233 mL 0.1165 mL 0.2329 mL 0.5823 mL
100 mM 0.0186 mL 0.0932 mL 0.1863 mL 0.4659 mL
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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.

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Product Name:
Edonentan
Cat. No.:
HY-15402
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