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Merck
CN

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)].

别名:

PD 145065

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关于此项目

经验公式（希尔记法）:
C52H63N7O10 · 2Na
化学文摘社编号:
153049-49-1
分子量:
992.08
UNSPSC Code:
12352200

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InChI key

HRAQSWKGRRUBDJ-OMUAVVNCSA-N

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

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

Quality Level

100

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)

存储类别

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

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