| Identification | Back Directory | [Name]
BQ-123 SODIUM SALT | [CAS]
136553-81-6 | [Synonyms]
BQ-123
BQ-518
PMZ 2123
BQ-123 SODIUM SALT
BQ-123;BQ 123;BQ123
ETA-RECEPTOR ANTAGONIST
M.W. 610.70 C31H42N6O7
D-TRP-D-ASP-PRO-D-VAL-LEU
C(DTRP-DASP-PRO-DVAL-LEU)
cyclo(Trp-Asp-Pro-Val-Leu)
CYCLO(D-ASP-PRO-D-VAL-LEU-D-TRP)
CYCLO(-D-TRP-D-ASP-PRO-D-VAL-LEU)
CYCLO(D-ASP-PRO-D-VAL-LEU-DTRP NA)
Cyclo(D-Asp-L-Pro-D-Val-L-Leu-D-Trp-)
Cyclo(D-Trp-D-Asp-L-Pro-D-Val-L-Leu-)
Cyclo[D-Asp-L-Pro-D-Val-L-Leu-D-Trp-]
BQ-123 SYNTHETIC >99% SELECTIVE ETA ENDO THE
BQ-123 >=99%, sodium salt, lyophilized powder
CYCLO (-D-TRP-D-ASP-PRO-D-VAL-LEU) SODIUM SALT
Cyclo(D-α-aspartyl-L-prolyl-D-valyl-L-leucyl-D-tryptophyl
Cyclo(D-α-aspartyl-L-prolyl-D-valyl-L-leucyl-D-tryptophyl)
CYCLO (D-ALPHA-ASPARTYL-L-PROLYL-D-VALYL-L-LEUCYL-D-TRYPTOPHYL)
2-[(3R,6R,9S,12R,15S)-6-(1H-indol-3-ylmethyl)-9-(2-methylpropyl)-2,5,8,11,14-pentaoxo-12-propan-2-yl-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-3-yl]acetic acid
2-((3R,6S,9R,12R,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 | [Molecular Formula]
C31H42N6O7 | [MDL Number]
MFCD00905129 | [MOL File]
136553-81-6.mol | [Molecular Weight]
610.7 |
| Chemical Properties | Back Directory | [Boiling point ]
1053.6±65.0 °C(Predicted) | [density ]
1.33±0.1 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
Soluble to 0.40 mg/ml in sterile | [form ]
lyophilized powder
| [pka]
4.04±0.10(Predicted) | [color ]
White to off-white | [Water Solubility ]
Soluble in water (0.4 mg/ml) |
| Hazard Information | Back Directory | [Uses]
BQ-123 has been used as a selective endothelin-A receptor antagonist to study its effects on tumor necrosis factor α (TNFα)-induced human airway smooth muscle cells (HASMCs) proliferation. It is also used as endothelin-A receptor antagonist to study its effects on TNFα-induced granulocyte–macrophage colony-stimulating factor (GM-CSF) expression. | [Definition]
ChEBI: BQ 123 is a cyclic peptide. | [Biological Activity]
bq-123 is a potent and selective antagonist of eta endothelin receptor with ki values of 1.4 and 1500 nm for eta and etb receptors, respectively.endothelin receptor is a g protein-coupled receptor. eta receptor increases intracellular-free ca2+. also, activation of eta receptor increases vasoconstriction and blood pressure.bq-123 is a selective eta receptor antagonist. in the eta-expressing cells, bq123 (10-6 m) inhibited endothelin-1 (et-1) (10-6 m)-induced [ca2+]i increase by 95% [1]. in rat vascular smooth muscle cells (vsmc), bq-123 inhibited et-1 receptor binding, cellular contraction, [ca2+ ]i mobilization, [3h]thymidine incorporation, map kinase activation and mtt reduction induced by et-1. however, bq-123 didn’t inhibit angiotensin ii (ang ii)- and arginine vasopressin (avp)-induced increases in map kinase activity and [ca2+]i mobilization [2].in spontaneously hypertensive rats (shr), renin hypertensive rats and normotensive rats, bq-123 (16 nm/kg/min) reduced mean arterial pressure in a dose-dependent way in shr. also, bq-123 lowered blood pressure in both renin hypertensive rats and normotensive rats [3]. in a kidney transplantation rat model with reperfusion injury, bq-123 prevented reperfusion injury and inhibited the synthesis and release of et-1,2 [4]. | [Biochem/physiol Actions]
Selective ETA endothelin receptor antagonist. | [storage]
-20°C | [References]
[1]. sakamoto a, yanagisawa m, sawamura t, et al. distinct subdomains of human endothelin receptors determine their selectivity to endothelina-selective antagonist and endothelinb-selective agonists. j biol chem, 1993, 268(12): 8547-8553.
[2]. guo x, okada k, fujita n, et al. inhibitory effect of bq-123 on endothelin-1-stimulated mitogen-activated protein kinase and cell growth of rat vascular smooth muscle cells. hypertens res, 1996, 19(1): 23-30.
[3]. douglas sa, 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 hypertens, 1994, 12(5): 561-567.
[4]. büyükgebiz o, aktan ao, haklar g, et al. bq-123, a specific endothelin (eta) receptor antagonist, prevents ischemia-reperfusion injury in kidney transplantation. transpl int, 1996, 9(3): 201-207. |
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