1. GPCR/G Protein
  2. Endothelin Receptor
  3. 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 ETA and ETB with Ki values of 15 pM and 41 nM, respectively. TA-0201 inhibits the pressor response to the exogenous big ET-1.

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TA-0201

TA-0201 Chemical Structure

CAS No. : 169679-53-2

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Description

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 ETA and ETB with Ki values of 15 pM and 41 nM, respectively. TA-0201 inhibits the pressor response to the exogenous big ET-1[1].

IC50 & Target

binding of [125I]ET-1 to cloned human receptors of ETA and ETB with Ki values of 15 pM and 41 nM, respectively[1]

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]
Molecular Weight

614.51

Formula

C27H28BrN5O5S

CAS No.
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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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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TA-0201
Cat. No.:
HY-124234
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