BQ-123

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BQ-123 (PMZ 2123) 是一种有效的、选择性的、非竞争性的环状五肽 ETA 受体拮抗剂，IC50 为 7.3 nM。

BQ-123 (PMZ 2123) is a potent, selective, non-competitive cyclic pentapeptide ETA receptor antagonist with IC50 of 7.3 nM; antagonizes endothelin-1-induced contractions in rabbit aorta, increases in inositol phosphates in cultured rat vascular smooth muscle A10 cells, shifts concentration-response curves in isolated rabbit aorta elicited by angiotensin II, but does not bind to angiotensin II receptors nor affect angiotensin II-induced increases in inositol phosphates.Diabetes Phase 1 Clinical(In Vivo):Sustained infusions of BQ-123 (0.16-164 nmol/kg per min, intravenously, for 6 h) produces dose-dependent reductions in mean arterial pressure in spontaneously hypertensive rats (SHR), the maximal reduction being obtained with a dose of 16 nmol/kg per min.BQ-123 (3 mg/kg; i.v.; given 15 minutes before pentylenetetrazole (PTZ)) impedes the formation and spread of seizure to a great degree in PTZ (50 mg/kg; i.p.) +BQ-123 groups.

——

Animal Model:Male Wistar albino ratsDosage:3 mg/kg Administration:Intravenous injection; given 15 minutes before PTZResult:Number of rats with major seizure decreased.

PMZ 2123 | BQ123

GPCR/G Protein

Endothelin Receptor

EndothelinAreceptor

Metabolic Disease

Diabetes

136553-81-6

610.7012

C31H42N6O7

>98% (HPLC)

DMSO: ≥ 34 mg/mL

O=C(O)C[C@H]1NC([C@@H](CC2=CNC3=C2C=CC=C3)NC([C@H](CC(C)C)NC([C@@H](C(C)C)NC([C@@](CCC4)([H])N4C1=O)=O)=O)=O)=O

Cyclo(D-α-aspartyl-L-prolyl-D-valyl-L-leucyl-D-tryptophyl)

(-20℃)

With Ice Pack

≥ 2 years