BQ-3020

CAS: 143113-45-5 F: C96H140N20O25S W: 2006.32

BQ-3020 is a selective endothelin receptor (ETB receptor) agonist that displacesET-1 binding to ETB receptors, with an I

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Bioactivity	BQ-3020 is a selective endothelin receptor (ETB receptor) agonist that displaces [125I] ET-1 binding to ETB receptors, with an IC50 value of 0.2 nM. BQ-3020 elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research12.
Invitro	BQ-3020（0.01–300 nM，7分钟）对 PhE 预收缩的尿路上皮剥离组织产生浓度依赖性松弛[1]。BQ-3020 (0.01–200 nM，20 min) 通过抑制 ETB 受体引起兔肺动脉剂量依赖性血管收缩，其 EC50 值为 0.57 nM[2]。
In Vivo	BQ-3020 (3 mg/kg 皮下注射, 单次给药) 可使癌痛小鼠模型在注射后 3 小时内的癌痛减轻约 50%[3]。 Animal Model:
Name	BQ-3020
CAS	143113-45-5
Sequence	Ac-Leu-Met-Asp-Lys-Glu-Ala-Val-Tyr-Phe-Ala-His-Leu-Asp-Ile-Ile-Trp
Shortening	Ac-Acetyl-LMDKEAVYFAHLDIIW
Formula	C96H140N20O25S
Molar Mass	2006.32
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Arteaga JL,et.al. Endothelin ET(B) receptors are involved in the relaxation to the pig urinary bladder neck. Neurourol Urodyn. 2012 Jun;31(5):688-94. [2]. Ihara M, et.al. A novel radioligand [125I]BQ-3020 selective for endothelin (ETB) receptors. Life Sci. 1992;51(6):PL47-52. [3]. Quang PN, et.al. Peripheral endothelin B receptor agonist-induced antinociception involves endogenous opioids in mice. Pain. 2010 May;149(2):254-262.

(-)-Isosclerone