BQ-123

Catalog No.S7883 Batch:S788303

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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 50 mg/mL (81.87 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 5.000mg/ml (8.19mM) Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 0.500mg/ml (0.82mM) Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <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, this compound 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, this compound (3 mg/kg, i.v.) potently impedes the formation and spread of seizure. [4] In pregnant C57BL/6 mice, this chemical (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.

References

  • https://pubmed.ncbi.nlm.nih.gov/1282942/
  • https://pubmed.ncbi.nlm.nih.gov/1318228/
  • https://pubmed.ncbi.nlm.nih.gov/20888175/
  • https://pubmed.ncbi.nlm.nih.gov/24449761/
  • https://pubmed.ncbi.nlm.nih.gov/25230003/

Customer Product Validation

Effects of 0.1% DMSO (as a vehicle), BQ-123 (a selective ETA receptor antagonist), BQ-788 (a selective ETB receptor antagonist), YM-254890 (a selective Gq protein inhibitor), PTX (a selective Gi protein inhibitor) and NF449 (a Gs protein inhibitor) on the ET-1-induced inhibition of insulinstimulated Akt phosphorylation in L6 myotubes. The cells were treated with 30 nM ET-1 for indicated times during treatment with 100 nM insulin for 60 min. The cells were treated with one of the drugs for 30 min (except PTX for 18 h) before treatment with 100 nM insulin for 60 min. (A) Representative immunoblots obtained using antibodies to phospho-Akt at Thr308 [p-Akt (T308)], phospho-Akt at Ser473 [p-Akt (S473)] and total Akt (t-Akt). (B) ET-1-induced changes in the ratio of phosphorylated Akt to t-Akt. Ordinate represents Akt phosphorylation responses, which are normalized to the level of insulin-stimulated Akt phosphorylation in L6 myotubes without treatment with ET-1, vehicle, antagonists or inhibitors. Data are presented as means ± SEM of the results obtained from five to six experiments. *P < 0.05 versus its control (100 nM insulin alone).

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

Selleck's BQ-123 Has Been Cited by 12 Publications

Jawbone-like organoids generated from human pluripotent stem cells [ Nat Biomed Eng, 2025, 10.1038/s41551-025-01419-3] PubMed: 40603745
Endogenous hydrogen sulfide persulfidates endothelin type A receptor to inhibit pulmonary arterial smooth muscle cell proliferation [ Redox Biol, 2025, 80:103493] PubMed: 39823888
Enhanced vascular contraction induced by exposure to angiotensin II mediated by endothelin-1 biosynthesis following PKCβ activation [ Am J Physiol Heart Circ Physiol, 2025, 328(3):H484-H495] PubMed: 39887322
Identification of ECE2 signaling in promoting non-small lung cancer progression through ET1/YAP1/MAGEA3 axis [ Sci Rep, 2025, 15(1):5626] PubMed: 39955423
Lead acetate deteriorates the improvement effect of L-arginine and tetrahydrobiopterin on endothelin-1 receptors activity in rat aorta [ Baghdad Sci J, 2023,  2023, 20(5 Suppl.)] PubMed: None
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

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

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.