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Cat. No.: 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 No.: 169679-53-2
화학식: C₂₇H₂₈BrN₅O₅S
분자량:614.51

보관:

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

Data Sheet (267 KB)

TA-0201 Chemical Structure

CAS No.: 169679-53-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

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]

All Endothelin Receptor Isoforms :

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 No. 169679-53-2
분자량 614.51
화학식 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
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Select Batch:

Purity: 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)

References

[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

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Keywords

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
Chemical Information
순도&문서
References

상품명:
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TA-0201

All Endothelin Receptor Isoforms

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

TA-0201 Related Classifications

HY-124234 Related Classifications