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

Tezosentan  (Synonyms: RO 610612)

Cat. No.: HY-17351 Purity: 98.79%
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Tezosentan (RO 610612) is an endothelin (ET) receptor antagonist, with pA2s of 9.5, 7.7 for ETA and ETB receptors, respectively.

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

Tezosentan Chemical Structure

Tezosentan Chemical Structure

CAS No. : 180384-57-0

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Based on 1 publication(s) in Google Scholar

Tezosentan Related Antibodies

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  • Biological Activity

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  • Purity & Documentation

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Description

Tezosentan (RO 610612) is an endothelin (ET) receptor antagonist, with pA2s of 9.5, 7.7 for ETA and ETB receptors, respectively.

IC50 & Target

ETA

9.5 (pA2)

ETB

7.7 (pA2)

In Vitro

Affinity of Tezosentan for the ET receptors is assessed in different cells and tissues. Tezosentan inhibits the specific 125I-labeled ET-1 binding to ETA receptors with an inhibitory potency (Ki) of 0.3 nM on CHO cells and of 18 nM on membranes of baculovirus-infected insect cells. Similarly, Tezosentan inhibits the specific binding of 125I-labeled ET-1, ET-3, or sarafotoxin S6c to ETB receptors with an inhibitory affinity of 10 to 21 nM. Tezosentan up to a concentration of 1 μM did not exhibit any binding inhibitory activity in 27 radioligand binding assays different from ET binding. On H1 central, 5-hydroxytryptamine2A, and vasopressin V1 receptors, Tezosentan (1 μM) induces a weak inhibition of less than 20%[1].

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

Tezosentan Related Antibodies
In Vivo

In pithed Wistar rats, Tezosentan dose-dependently inhibits the pressor effect of big ET-1 (P<0.001 at all doses). At the lowest dose tested of 1 mg/kg, Tezosentan inhibits the pressor effect of the various doses of big ET-1 by 50 to 80%. Tezosentan has no effect by itself on blood pressure in these pithed rats. Tezosentan is very effective in a rat model of acute renal failure. ET antagonists have been shown to prevent the vasoconstriction and the renal failure that follow acute renal ischemia in rats[1].

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

605.63

Formula

C27H27N9O6S
CAS No.
Appearance

Solid

Color

Off-white to gray

SMILES

O=S(C1=NC=C(C(C)C)C=C1)(NC2=NC(C3=CC(C4=NNN=N4)=NC=C3)=NC(OCCO)=C2OC5=CC=CC=C5OC)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (82.56 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 1.6512 mL 8.2559 mL 16.5117 mL
5 mM 0.3302 mL 1.6512 mL 3.3023 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 (sealed storage, away from moisture and light). 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)

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References
Animal Administration
[1]

Rats[1]
A pseudocrush syndrome is simulated by injection of i.m. glycerol. A control group does not receive glycerol and is used as a reference. Tezosentan or bosentan for comparison or saline as control is injected as two bolus i.v. doses of 10 mg/kg 1 h and 20 min before glycerol. Rats are allowed to recover for 2 h and then are placed in individual metabolic cages for 48 h. Blood samples withdraw from a catheter placed in the abdominal aorta and urine free of food and feces are collected at 24 and 48 h. Plasma and urinary creatinine levels are measured with a centrifugal analyzer. Renal function is assessed by calculating creatinine clearance at 24 and 48 h after glycerol administration[1].

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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). 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 1.6512 mL 8.2559 mL 16.5117 mL 41.2793 mL
5 mM 0.3302 mL 1.6512 mL 3.3023 mL 8.2559 mL
10 mM 0.1651 mL 0.8256 mL 1.6512 mL 4.1279 mL
15 mM 0.1101 mL 0.5504 mL 1.1008 mL 2.7520 mL
20 mM 0.0826 mL 0.4128 mL 0.8256 mL 2.0640 mL
25 mM 0.0660 mL 0.3302 mL 0.6605 mL 1.6512 mL
30 mM 0.0550 mL 0.2752 mL 0.5504 mL 1.3760 mL
40 mM 0.0413 mL 0.2064 mL 0.4128 mL 1.0320 mL
50 mM 0.0330 mL 0.1651 mL 0.3302 mL 0.8256 mL
60 mM 0.0275 mL 0.1376 mL 0.2752 mL 0.6880 mL
80 mM 0.0206 mL 0.1032 mL 0.2064 mL 0.5160 mL
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Tezosentan 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:

Tezosentan180384-57-0RO 610612RO610612RO-610612Endothelin ReceptorInhibitorinhibitorinhibit

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