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Key Documents

P3209

Sigma-Aldrich

PD 156,252

≥97% (HPLC)

Synonym(s):

N-Acetyl-α-[10,11-Dihydro-5H-dibenzo[a,d]cycloheptadien-5-yl]-D-Gly-Leu-Asp-Ile-N-Methyl-Ile-Trp

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About This Item

Empirical Formula (Hill Notation):
C53H67N7O10
CAS Number:
Molecular Weight:
962.14
MDL number:
UNSPSC Code:
12352200

assay

≥97% (HPLC)

composition

Peptide content, ~70%

storage temp.

−20°C

Biochem/physiol Actions

Non-selective endothelin receptor antagonist.

Other Notes

Contains the conserved endothelin sequence, His-Leu-Asp-Ile-Ile-Trp, with His replaced by a bulky aromatic moiety.

Storage Class

13 - Non Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)


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H K Han et al.
Life sciences, 63(18), 1599-1609 (1998-11-07)
Endothelins are potent vasoconstrictor peptides which have a wide range of tissue distribution and three receptor subtypes (ET(A), ET(B) and ET(C)). Among the linear hexapeptide ET(A)/ET(B) receptor antagonists, PD 145065 (Ac-D-Bhg-L-Leu-L-Asp-L-Ile-L-Ile-L-Trp, Bhg = (10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-yl)-Gly) and PD 156252 (Ac-D-Bhg-L-Leu-L-Asp-L-Ile-(N-methyl)-L-Ile-L-Trp) were selected
W L Cody et al.
Journal of medicinal chemistry, 40(14), 2228-2240 (1997-07-04)
The endothelins (ETs) are a family of bicyclic 21-amino acid peptides that are potent and prolonged vasoconstrictors. It has been shown that highly potent combined ETA/ETB receptor antagonists can be developed from the C-terminal hexapeptide of ET (His16-Leu17-Asp18-Ile19-Ile20-Trp21), such as

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