BQ-123 _Endothelin Receptor Antagonist - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBQ-123Cat. No.: HY-12378CAS No.: 136553-81-6分式: CHNO分量: 610.7作靶點(diǎn): Endothelin Receptor作通路: GPCR/G Protein儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 34 mg/mL (55.67 mM)* means soluble, b

2、ut saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.6375 mL 8.1873 mL 16.3747 mL5 mM 0.3275 mL 1.6375 mL 3.2749 mL10 mM 0.1637 mL 0.8187 mL 1.6375 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請根據(jù)您的實(shí)驗(yàn)動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的

3、儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (4.09 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (4.09 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGIC

4、AL ACTIVITY物活性 BQ-123種選擇性內(nèi)素 A 受體 (ETAR) 拮抗劑，IC50 值為 7.3 nM，Ki值為 25 nM 1 2。IC50 & Target IC50: 7.3 nM (Endothelin A receptors) 1Ki: 25 nM (Endothelin A receptors) 2體內(nèi)研究 BQ-123 (3 mg/kg; i.v.; given 15 minutes before pentylenetetrazole (PTZ) impedes the formation and spreadof seizure to a great degree

5、 in PTZ (50 mg/kg; i.p.) +BQ-123 groups 3.Animal Model: Male Wistar albino rats 3Dosage: 3 mg/kgAdministration: Intravenous injection; given 15 minutes before PTZResult: Number of rats with major seizure decreased.REFERENCES1. Spratt JC, et al. Systemic ETA receptor antagonism with BQ-123 blocks ET-

6、1 induced forearm vasoconstriction and decreasesperipheral vascular resistance in healthy men. Br J Pharmacol. 2001 Oct;134(3):648-54.2. Sakamoto A, et al. Distinct subdomains of human endothelin receptors determine their selectivity to endothelinA-selective antagonistand endothelinB-selective agoni

7、sts. J Biol Chem. 1993 Apr 25;268(12):8547-53.3. Erdogan H et al. The protective effects of endothelin-A receptor antagonist BQ-123 in pentylenetetrazole-induced seizure in rats. HumExp Toxicol, 2014 Oct, 33(10):1008-16.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use o