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
质量水平
方案
≥98% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
颜色
white
溶解性
phosphate buffer, pH 7.5: 1 mg/mL
运输
ambient
储存温度
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
一般描述
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)].
生化/生理作用
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)
制备说明
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.
其他说明
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.).
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明
Toxicity: Standard Handling (A)
储存分类代码
11 - Combustible Solids
WGK
WGK 1
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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