ChemicalBook--->CAS DataBase List--->153049-49-1

153049-49-1

153049-49-1 Structure

153049-49-1 Structure
IdentificationBack Directory
[Name]

PD 145065
[CAS]

153049-49-1
[Synonyms]

PD 145065
Ac-bhg-Leu-Asp-Ile-Ile-Trp
AC-DBHG-LEU-ASP-ILE-ILE-TRP
AC-D-BHG-LEU-ASP-ILE-ILE-TRP-OH
[AC-DBHG16] ENDOTHELIN-1 (16-21)
endothelin receptor antagonist*pd 145065
N-Acetyl-α-[10,11-Dihydro-5H-dibenzo[a,d]cycloheptadien-5-yl]-D-Gly-Leu-Asp-Ile-Ile-Trp
L-Tryptophan, N-[N-[N-[N-[N-[N-acetyl-D-2-(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-yl)glycyl]-L-leucyl]-L-α-aspartyl]-L-isoleucyl]-L-isoleucyl]- (9CI)
[Molecular Formula]

C52H67N7O10
[MDL Number]

MFCD00467202
[MOL File]

153049-49-1.mol
[Molecular Weight]

950.13
Chemical PropertiesBack Directory
[storage temp. ]

−20°C
[solubility ]

phosphate buffer, pH 7.5: 1mg/mL
[form ]

White solid
[color ]

white
[Sequence]

Ac-{D-Bhg}-Leu-Asp-Ile-Ile-Trp-OH (Bhg = 5H-dibenzo[a,d]cycloheptene-5-glycine)
[InChIKey]

HRAQSWKGRRUBDJ-OMUAVVNCSA-N
Safety DataBack Directory
[WGK Germany ]

3
[Storage Class]

11 - Combustible Solids
Hazard InformationBack Directory
[Uses]

PD 145065 is a highly potent but non-selective endothelin receptor antagonist with an IC50 value of 4 nM for the ETA receptor for rabbit renal artery vascular smooth muscle cells[1].
[Biological Activity]

Cell permeable: no''Primary Target
Endothelin receptor antagonist''Product does not compete with ATP.''Reversible: no''Target IC50: 4 nM against endothelin receptor (ETA receptor) in rabbit renal artery vascular smooth muscle cells; 15 nM for the ETB receptor (r at cerebellum)
[References]

[1] Warner TD, et al. Reversal of established responses to endothelin-1 in vivo and in vitro by the endothelin receptor antagonists, BQ-123 and PD 145065. Br J Pharmacol. 1994 May;112(1):207-13. DOI:10.1111/j.1476-5381.1994.tb13053.x
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