BQ-123
(Synonyms: 环(D-ALPHA-天冬氨酰-L-脯氨酰-D-缬氨酰-L-亮氨酰-D-色氨酰)) 目录号 : GC15887
BQ-123是一种高效、选择性内皮素A（ETA）受体拮抗剂，IC50 值为7.3nM，Ki值为25nM。
Cas No.:136553-81-6
Sample solution is provided at 25 µL, 10mM.
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BQ-123 is a highly potent and selective endothelin A (ETA) receptor antagonist with an IC50 value of 7.3nM and a Ki value of 25nM[1]. BQ-123 is a cyclic pentapeptide first isolated from the fermentation broth of Streptomyces misakiensis in 1991[2]. BQ123 can effectively reverse ischemic acute renal failure and increase the reabsorption of sodium ions by proximal tubular cells[3].
In vitro, BQ-123 (12mM) treatment of rat brain primary cultures for 48h increased the number of β-III tubulin-positive neurons under normoxic conditions and reduced neuronal loss under hypoxic conditions[4].
In vivo, BQ-123 (3mg/kg) was intravenously injected into rats with pentylenetetrazol (PTZ)-induced tonic-clonic epilepsy, significantly delayed the onset of epilepsy in rats, significantly reversed the oxidative effects of PTZ on brain tissue, and increased neuronal chromatin in the dentate gyrus of the hippocampus[5]. BQ-123 (0.16-164nM/kg/min) was treated with continuous intravenous infusion for 6h in spontaneously hypertensive rats (SHR) and reduced mean arterial pressure in a dose-dependent manner[6].
References:
[1] Ihara M, Ishikawa K, Fukuroda T, et al. In vitro biological profile of a highly potent novel endothelin (ET) antagonist BQ-123 selective for the ETA receptor[J]. Journal of cardiovascular pharmacology, 1992, 20: S11-S14.
[2] Peishoff C E, Janes R W, Wallace B A. Comparison of the structures of the endothelin A receptor antagonists BQ123 and N-methyl leucine BQ123 with the crystal structure of the C-terminal tail of endothelin-1[J]. FEBS letters, 1995, 374(3): 379-383.
[3] Sheridan A M, Bonventre J V. Pathophysiology of ischemic acute renal failure[J]. Blood Purification in Intensive Care, 2001, 132: 7-21.
[4] Danielyan L, Mueller L, Proksch B, et al. Similar protective effects of BQ-123 and erythropoietin on survival of neural cells and generation of neurons upon hypoxic injury[J]. European journal of cell biology, 2005, 84(11): 907-913.
[5] Erdogan H, Ekici F, Katar M, et al. The protective effects of endothelin-A receptor antagonist BQ-123 in pentylenetetrazole-induced seizure in rats[J]. Human & experimental toxicology, 2014, 33(10): 1008-1016.
[6] Douglas S A, Gellai M, Ezekiel M, et al. BQ-123, a selective endothelin subtype A-receptor antagonist, lowers blood pressure in different rat models of hypertension[J]. Journal of hypertension, 1994, 12(5): 561-568.
BQ-123是一种高效、选择性内皮素A（ETA）受体拮抗剂，IC50 值为7.3nM，Ki值为25nM[1]。BQ-123是1991年首次从Misakiensis链霉菌的发酵液中分离的环状五肽[2]。BQ123可有效逆转缺血性急性肾衰竭，能增加近端小管细胞对钠离子的重吸收[3]。
在体外，BQ-123（12mM）处理大鼠脑原代培养物48h，在常氧条件下增加了β-III微管蛋白阳性神经元的数量，在缺氧条件下减少了神经元损失[4]。
在体内，BQ-123（3mg/kg）通过静脉注射治疗戊四唑（PTZ）诱导的强直-阵挛性癫痫大鼠，显著延迟了大鼠癫痫发作时间，显著逆转了PTZ对脑组织的氧化作用，增加了海马齿状回区的神经元染色质[5]。BQ-123（0.16-164nM/kg/min）通过静脉注射持续输注6h治疗自发性高血压大鼠（SHR），剂量依赖性地降低了平均动脉压[6]。
| Cell experiment [1]: | |
Cell lines | Rat brain primary cultures |
Preparation Method | Astroglia-rich primary cultures were prepared from the brains of newborn Wistar rats.Cells (1×106) were seeded in culture dishes containing glass coverslips. The cells were cultured in 90% DMEM containing 10% FCS, 20mg/ml streptomycin sulfate and 20U/ml penicillin G in an incubator containing a humidified air/10% CO2 atmosphere at 37℃ until 5 days. At this time the medium was replaced by DMEM containing EPO (erythropoietin β, NeoRecormon 5U/ml cell culture medium) or/and 12mM BQ-123(dissolved in PBS). The cell cultures were incubated for 48h under normoxic condition (NC) and hypoxic conditions (HC). The tubulin b III-positive cells from three experiments (six fields on each coverslip) were manually counted. |
Reaction Conditions | 12mM; 48h |
Applications | Rat brain primary cultures exposed to BQ-123 and/or EPO revealed an increase in the number of β-III tubulin-positive neurons under NC. The hypoxia-caused loss of neurons was abolished by administration of BQ-123 or EPO. |
| Animal experiment [2]: | |
Animal models | Male Wistar albino rats |
Preparation Method | Rats were randomly assigned to 3 groups: Group 1 (control): untreated, sham-operated rats, group 2 (PTZ): animals treated with a single 50 mg/kg intraperitoneal administration of pentylenetetrazole (PTZ), and group 3 (PTZ+BQ-123): animals treated with single 50mg/kg i.p. administration of PTZ and 3mg/kg intravenous injection of BQ-123, given 15min before PTZ. Under ether anesthesia, the animals were killed 30min after the administration of PTZ. Their brains were removed, put on a cold surface, divided into two halves with surgical knife by dissected along the corpus callosum, and then rinsed in cold saline solution. The right brain hemispheres were used for histological examination. The left brain tissue was stored at −80°C until biochemical analyses. |
Dosage form | 3mg/kg/day; i.v. |
Applications | The time of epileptic seizures in rats in the BQ-123 group was significantly delayed, and only one rat had a major epileptic seizure. BQ-123 treatment significantly reversed the oxidative effect of PTZ on brain tissue. Chromatin increased in neurons in the hippocampal gyrus dentatus region of rats in the BQ-123 group. |
References: [1]Danielyan L, Mueller L, Proksch B, et al. Similar protective effects of BQ-123 and erythropoietin on survival of neural cells and generation of neurons upon hypoxic injury[J]. European journal of cell biology, 2005, 84(11): 907-913. [2]Erdogan H, Ekici F, Katar M, et al. The protective effects of endothelin-A receptor antagonist BQ-123 in pentylenetetrazole-induced seizure in rats[J]. Human & experimental toxicology, 2014, 33(10): 1008-1016. | |
| Cas No. | 136553-81-6 | SDF | |
| 别名 | 环(D-ALPHA-天冬氨酰-L-脯氨酰-D-缬氨酰-L-亮氨酰-D-色氨酰) | ||
| 化学名 | 2-((3R,6S,9S,12S,17aS)-9-((1H-indol-3-yl)methyl)-6-isobutyl-3-isopropyl-1,4,7,10,13-pentaoxohexadecahydro-1H-pyrrolo[1,2-a][1,4,7,10,13]pentaazacyclopentadecin-12-yl)acetic acid | ||
| Canonical SMILES | O=C([C@H]1N(C([C@H](CC(O)=O)NC([C@H](CC2=CNC3=CC=CC=C23)NC4=O)=O)=O)CCC1)N[C@@H](C(N[C@H]4CC(C)C)=O)C(C)C | ||
| 分子式 | C31H42N6O7 | 分子量 | 611 |
| 溶解度 | DMF: 1 mg/ml,DMSO: 20 mg/ml,DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml,PBS (pH 7.2): slightly | 储存条件 | Desiccate at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6367 mL | 8.1833 mL | 16.3666 mL |
| 5 mM | 0.3273 mL | 1.6367 mL | 3.2733 mL |
| 10 mM | 0.1637 mL | 0.8183 mL | 1.6367 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
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2.
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