P3209
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
UNSPSC Code:
12352200
MDL number:
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
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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