Biochem/physiol Actions

Cell permeable: no

Reversible: no

Product does not compete with ATP.

Primary TargetEndothelin receptor antagonist

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)

General description

A highly potent but non-selective endothelin receptor antagonist [IC₅₀ = 4 nM for the ET_A receptor (rabbit renal artery vascular smooth muscle cells); IC₅₀ = 15 nM for ET_B receptor (rat cerebellum)].

A highly potent but non-selective endothelin receptor antagonist [IC₅₀ = 4 nM for the ET_A receptor (rabbit renal artery vascular smooth muscle cells); IC₅₀ = 15 nM for the ET_B receptor (rat cerebellum)].

Legal Information

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

Other Notes

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.).

Packaging

500 µg in Plastic ampoule

Reconstitution

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.

Sequence

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

Warning

Toxicity: Standard Handling (A)