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513020

Sigma-Aldrich

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:
153049-49-1
Molecular Weight:
992.08
UNSPSC Code:
12352200

Quality Level

100

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
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.).

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Storage Class Code

11 - Combustible Solids

WGK

WGK 1

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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