BQ-123

Catalog No.S7883 Batch:S788301

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Technical Data

Formula

C31H42N6O7
Molecular Weight 610.7 CAS No. 136553-81-6
Solubility (25°C)* In vitro DMSO 100 mg/mL (163.74 mM)
Ethanol 92 mg/mL (150.64 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description BQ-123 is a selective endothelin A receptor (ETA) antagonist with IC50 of 7.3 nM. Phase 2.
Targets
Endothelin A receptor [1]
(Cell-free assay)
7.3 nM
In vitro In porcine aortic vascular smooth muscle cells, BQ-123 selectively inhibits ETA-mediated contraction. [1] In rat vascular smooth muscle cells, BQ-123 inhibits endothelin-1-induced phosphoinositide breakdown and DNA synthesis. [2]
In vivo In rats, BQ-123 (1 mg/kg, i.v.) ameliorates myocardial ischemic-reperfusion injury. [3] In rats with pentylenetetrazole (PTZ)-induced tonic-clonic seizures, BQ-123 (3 mg/kg, i.v.) potently impedes the formation and spread of seizure. [4] In pregnant C57BL/6 mice, BQ-123 (6.7 mg/kg, i.p.) prevents LPS-induced preterm birth in mice via the induction of uterine and placental IL-10. [5]

Protocol (from reference)

Animal Study:[3]
  • Animal Models

    Male Wistar rats

  • Dosages

    1 mg/kg

  • Administration

    i.v.

Customer Product Validation

Data from [Data independently produced by , , Br J Pharmacol, 2016, 173(6):1018-32. ]

Selleck's BQ-123 has been cited by 7 publications

Lead acetate deteriorates the improvement effect of L-arginine and tetrahydrobiopterin on endothelin-1 receptors activity in rat aorta [ Baghdad Science Journal, 2023, 20(5 Suppl.)] PubMed: none
Induction of GLI1 by miR-27b-3p/FBXW7/KLF5 pathway contributes to pulmonary arterial hypertension [ J Mol Cell Cardiol, 2022, 171:16-29] PubMed: 35810662
Telmisartan attenuatesuric acid-induced epithelial-mesenchymal transition in renal tubular cells [ BioMed Research International, 2019-, 10.1155/2019/3851718] PubMed: None
Notch signaling activation induces cell death in MAPKi-resistant melanoma cells [Mikheil DM Pigment Cell Melanoma Res, 2019, 10.1111/pcmr.12764] PubMed: 30614626
Telmisartan Attenuates Uric Acid-Induced Epithelial-Mesenchymal Transition in Renal Tubular Cells. [ Biomed Res Int, 2019, 2019:3851718] PubMed: 30993112
L-arginine and tetrahydrobiopterin modulate endothelin-1A receptor activity in isolated rat aorta [ ZANCO, 2019, 31-2] PubMed: None
Evolution of the developmental plasticity and a coupling between left mechanosensory neuromasts and an adaptive foraging behavior [Fernandes VFL Dev Biol, 2018, 441(2):262-271] PubMed: 29782817

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.