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Cat. No.: HY-114674

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A-127722

A-127722 is A 2, 4-dialarylpyrrolidine-3-carboxylic acid ET_A selective endothelin receptor (ET receptor) antagonist with IC₅₀ value of 0.36 nM.

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

CAS No.: 195704-72-4
Formula: C₂₉H₃₈N₂O₆
Molecular Weight:510.62

Storage:

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

Data Sheet (273 KB)

A-127722 Chemical Structure

CAS No.: 195704-72-4

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Use of MCE Products

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

Biological Activity
- Description
- Cellular Effect
Chemical Information
Protocols (1)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

A-127722 is A 2, 4-dialarylpyrrolidine-3-carboxylic acid ET_A selective endothelin receptor (ET receptor) antagonist with IC₅₀ value of 0.36 nM^[1].

All Endothelin Receptor Isoforms :

ET_A
ET_B

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.055 nM Compound: 5; ABT-627; Xinlay	Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane	[PMID: 27266371]
MMQ	IC₅₀	0.04 nM Compound: 17v	Inhibition of phosphoinositol hydrolysis of MMQ cells. Inhibition of phosphoinositol hydrolysis of MMQ cells.	[PMID: 8676339]
MMQ	IC₅₀	0.31 nM Compound: 17v	Inhibitory activity against the Endothelin A receptor of rat MMQ cells Inhibitory activity against the Endothelin A receptor of rat MMQ cells	[PMID: 8676339]
MMQ	IC₅₀	0.36 nM Compound: 1	Binding affinity against Endothelin A receptor in MMQ cells in rat Binding affinity against Endothelin A receptor in MMQ cells in rat	[PMID: 11689084]
Pituitary gland cell	IC₅₀	0.4 nM Compound: 13	Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand. Binding affinity towards endothelin A receptor in prolactin secreting rat pituitary cells using [125I]ET1 as radioligand.	[PMID: 9022798]

Chemical Information

CAS No. 195704-72-4
Molecular Weight 510.62
Formula C₂₉H₃₈N₂O₆
SMILES

O=C([C@H]1[C@H](C2=CC=C(OC)C=C2)N(CC(N(CCCC)CCCC)=O)C[C@@H]1C3=CC=C(OCO4)C4=C3)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Protocols

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 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]. Winn M, et al. 2,4-Diarylpyrrolidine-3-carboxylic acids--potent ETA selective endothelin receptor antagonists. 1. Discovery of A-127722. J Med Chem. 1996 Mar 1;39(5):1039-48. [Content Brief]

Calculators

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Dilution Calculator

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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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