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
• Empirical Formula (Hill Notation): C₅₂H₆₃N₇O₁₀ · 2Na
• CAS Number: 153049-49-1
• Molecular Weight: 992.08
• UNSPSC Code: 12352200

Properties

• 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

Description

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 the ET_B 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)

Warning

Toxicity: Standard Handling (A)

Sequence

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

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.

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.).

Legal Information

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 1
• flash_point_f: Not applicable
• flash_point_c: Not applicable