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Art. -Nr.: HY-124234

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TA-0201

TA-0201 is a novel orally active, competitive, non-peptide endothelin receptor antagonist. TA-0201 antagonizes the specific binding of [¹²⁵I]ET-1 to cloned human receptors of ET_A and ET_B with K_i values of 15 pM and 41 nM, respectively. TA-0201 inhibits the pressor response to the exogenous big ET-1.

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CAS. Nr.: 169679-53-2
Formel: C₂₇H₂₈BrN₅O₅S
Molecular Weight:614.51

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (267 KB)

TA-0201 Chemical Structure

CAS. Nr.: 169679-53-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

binding of [¹²⁵I]ET-1 to cloned human receptors of ET_A and ET_B with K_i values of 15 pM and 41 nM, respectively^[1]

Alle Endothelin Receptor Isoform-spezifische Produkte anzeigen :

ET_A
ET_B

Cellular Effect

Cell Line	Type	Value	Description	References
A7R5	IC₅₀	0.015 nM Compound: 26; TA0201	Displacement of 125I-ET1 from ETA receptor in rat A7R5 cells Displacement of 125I-ET1 from ETA receptor in rat A7R5 cells	[PMID: 27321813]
CHO	IC₅₀	0.4 nM Compound: 2, T-0201	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	[PMID: 22862294]
CHO	IC₅₀	12 nM Compound: 2, T-0201	Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis	[PMID: 22862294]

Chemical Information

CAS. Nr. 169679-53-2
Molecular Weight 614.51
Formel C₂₇H₂₈BrN₅O₅S
SMILES

O=S(NC1=NC=NC(OCCOC2=NC=C(C=N2)Br)=C1C3=CC=C(C)C=C3)(C4=CC=C(C(C)(CO)C)C=C4)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (267 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Ohashi N, et al. Determination of TA-0201, a novel orally active non-peptide endothelin antagonist, in rat plasma and tissues by a liquid chromatography--electrospray ionization--tandem mass spectrometry system. J Pharm Biomed Anal. 1999 Mar;19(3-4):491-9. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
Chemical Information
Reinheit & Dokumentation
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TA-0201

Alle Endothelin Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

TA-0201 Related Classifications

HY-124234 Related Classifications