513020
PD 145065
A highly potent but non-selective endothelin receptor antagonist [IC50= 4 nM for the ETA receptor (rabbit renal artery vascular smooth muscle cells); IC50 = 15 nM for the ETB receptor (rat cerebellum)].
Synonym(s):
PD 145065
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About This Item
Empirical Formula (Hill Notation):
C52H63N7O10 · 2Na
CAS Number:
Molecular Weight:
992.08
UNSPSC Code:
12352200
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze
Quality Segment
assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
color
white
solubility
phosphate buffer, pH 7.5: 1 mg/mL
shipped in
ambient
storage temp.
2-8°C
InChI
1S/C52H67N7O10/c1-8-29(5)44(49(65)57-41(52(68)69)25-34-27-53-38-21-15-14-18-35(34)38)59-50(66)45(30(6)9-2)58-48(64)40(26-42(61)62)55-47(63)39(24-28(3)4)56-51(67)46(54-31(7)60)43-36-19-12-10-16-32(36)22-23-33-17-11-13-20-37(33)43/h10-21,27-30,39-41,43-46,53H,8-9,22-26H2,1-7H3,(H,54,60)(H,55,63)(H,56,67)(H,57,65)(H,58,64)(H,59,66)(H,61,62)(H,68,69)/t29-,30-,39-,40-,41-,44-,45-,46+/m0/s1
InChI key
HRAQSWKGRRUBDJ-OMUAVVNCSA-N
General description
A highly potent but non-selective endothelin receptor antagonist [IC50 = 4 nM for the ETA receptor (rabbit renal artery vascular smooth muscle cells); IC50 = 15 nM for the ETB receptor (rat cerebellum)].
Biochem/physiol Actions
Cell permeable: no
Primary Target
Endothelin receptor antagonist
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 (rat cerebellum)
Preparation Note
Following reconstitution, aliquot and freeze (-20°C) for long-term storage. Stock solutions are stable for up to 4 months at -20°C. Avoid freeze/thaw cycles of solutions.
Other Notes
Ac-D-Bhg-Leu-Asp-Ile-Ile-Trp-OH (Bhg = 5H-dibenzo[a,d]cycloheptene-5-glycine)
Han, H.K., et al. 1998. Life Sci. 63, 1599.
Allcock, G.H., et al. 1995. Br. J. Pharmacol.116, 2482.
Wellings, R.P., et al. 1994. Eur. J. Pharmacol.256, 201.
Cody, W.L., et al. 1993. Med. Chem. Res. 3, 154.
Doherty, A.M., et al. 1993. J. Cardiovasc.Pharmacol. 22, S98 (Suppl.).
Allcock, G.H., et al. 1995. Br. J. Pharmacol.116, 2482.
Wellings, R.P., et al. 1994. Eur. J. Pharmacol.256, 201.
Cody, W.L., et al. 1993. Med. Chem. Res. 3, 154.
Doherty, A.M., et al. 1993. J. Cardiovasc.Pharmacol. 22, S98 (Suppl.).
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
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