| Identification | Back Directory | [Name]
BQ-3020 | [CAS]
143113-45-5 | [Synonyms]
BQ-3020
AC-LMDKEAVYFAHLDIIW
M.W. 2006.35 C96H140N20O25S
Acetyl-(Ala 11,15)-ET 1 (6-21)
endothelin receptor antagonist
AC-(ALA11,15)-ENDOTHELIN-1 (6-21)
N-AC, ALA11,15-ENDOTHELIN 1, 6-21
ACETYL-(ALA11,15)-ENDOTHELIN-1 (6-21)
ACETYL-(D-TRP16)-ENDOTHELIN-1 (16-21)
N-ACETYL[ALA11,15]-ENDOTHELIN-1 (6-21)
N-ACETYL-[ALA11,15]ENDOTHELIN-I (6-21)
ENDOTHELIN-1(6-21), N-ACETYL-[ALA11,15]-
Acetyl-(Ala11·15)-Endothelin-1 (6-21)
BQ-3020
n-acetyl-[ala11,15]-endothelin 1 fragment 6-21
BQ-3020 ENDOTHELIN-1(6-21),N-ACETYL-(ALA 11, 15) SYNTHETIC >97%
AC-LEU-MET-ASP-LYS-GLU-ALA-VAL-TYR-PHE-ALA-HIS-LEU-ASP-ILE-ILE-TRP
AC-LEU-MET-ASP-LYS-GLU-ALA-VAL-TYR-PHE-ALA-HIS-LEU-ASP-ILE-ILE-TRP-OH
6-21-Endothelin 1 (swine reduced), N-acetyl-11-L-alanine-15-L-alanine-
ACETYL-LEU-MET-ASP-LYS-GLU-ALA-VAL-TYR-PHE-ALA-HIS-LEU-ASP-ILE-ILE-TRP-OH
Acetyl-(Ala11·15)-Endothelin-1 (6-21) Ac-Leu-Met-Asp-Lys-Glu-Ala-Val-Tyr-Phe-Ala-His-Leu-Asp-Ile-Ile-Trp-OH | [Molecular Formula]
C96H140N20O25S | [MDL Number]
MFCD00236977 | [MOL File]
143113-45-5.mol | [Molecular Weight]
2006.34 |
| Chemical Properties | Back Directory | [Boiling point ]
2125.8±65.0 °C(Predicted) | [density ]
1.287±0.06 g/cm3(Predicted) | [storage temp. ]
−20°C | [solubility ]
Soluble to 0.50 mg/ml in sodium bicarbonate (0.03M) | [form ]
powder | [pka]
3.39±0.10(Predicted) | [color ]
white | [Sensitive ]
Light Sensitive | [Sequence]
Ac-Leu-Met-Asp-Lys-Glu-Ala-Val-Tyr-Phe-Ala-His-Leu-Asp-Ile-Ile-Trp-OH | [InChIKey]
NUAGCEFLVCODRQ-KETPNHLCSA-N |
| Hazard Information | Back Directory | [Uses]
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. | [Biological Activity]
BQ-3020a linear endothelin analogis a selective ETB endothelin receptor agonist. | [in vivo]
BQ-3020 (3 mg/kg for i.h., single dose) attenuates cancer pain by approximately 50% up to 3 h post-injection compared to PBS-vehicle and contralateral injection in cancer pain mouse model[3].
| Animal Model: | Cancer pain mouse model [3] | | Dosage: | 3 mg/kg | | Administration: | Injected subcutaneously at the site of the greatest tumor development | | Result: | Attenuated cancer pain by approximately 50% up to 3 h post-injection compared to PBS-vehicle and contralateral injection
|
| [IC 50]
ETB: 0.2 nM (IC50) | [storage]
-20°C | [References]
[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. DOI:10.1002/nau.22203
[2] Ihara M, et.al. A novel radioligand [125I]BQ-3020 selective for endothelin (ETB) receptors. Life Sci. 1992;51(6):PL47-52. DOI:10.1016/0024-3205(92)90418-o
[3] Quang PN, et.al. Peripheral endothelin B receptor agonist-induced antinociception involves endogenous opioids in mice. Pain. 2010 May;149(2):254-262. DOI:10.1016/j.pain.2010.02.009 |
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