BQ-3020
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.
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- CAS. Nr.: 143113-45-5
- Formel: C96H140N20O24S
- Molecular Weight:1990.32
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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ETB 0.2 nM (IC50) |
BQ-3020 (0.01–300 nM, 7 min), produced concentration-dependent relaxationso on PhE-precontracted urothelium-denuded strips[1].
BQ-3020 (0.01–200 nM, 20 min) causes potent dose-dependent vasoconstriction with EC50 values of 0.57nM in rabbit pulmonary arteries by inhibiting ETB receptors[2].
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MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Cancer pain mouse model [3]
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Dosage:3 mg/kg
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Administration:Injected subcutaneously at the site of the greatest tumor development
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Result:Attenuated cancer pain by approximately 50% up to 3 h post-injection compared to PBS-vehicle and contralateral injection
Chemical Information
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CAS. Nr. 143113-45-5
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Molecular Weight 1990.32
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Formel C96H140N20O24S
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Sequence
Ac-Leu-Met-Asp-Lys-Glu-Ala-Val-Tyr-Phe-Ala-His-Leu-Asp-Ile-Ile-Trp
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Sequence Shortening
Ac-LMDKEAVYFAHLDIIW
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[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. [Content Brief]
[2]. Ihara M, et.al. A novel radioligand [125I]BQ-3020 selective for endothelin (ETB) receptors. Life Sci. 1992;51(6):PL47-52. [Content Brief]
[3]. Quang PN, et.al. Peripheral endothelin B receptor agonist-induced antinociception involves endogenous opioids in mice. Pain. 2010 May;149(2):254-262. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
BQ-3020 Related Classifications
HY-P1016 Related Classifications
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