BQ-788 sodium salt
BQ-788 sodium salt (CAS 156161-89-6) is a selective antagonist targeting endothelin B (ETB) receptors. In vitro studies demonstrate that BQ-788 inhibits ET-1 binding to human ETB receptors with an IC50 of approximately 1.2 nM, displaying significantly lower affinity for ETA receptors (IC50 ≈1300 nM). Competitive binding assays also confirm potent ETB receptor antagonism in porcine cerebellar membranes and human hGH cells (IC50 ≈ 0.9-1.2 nM). BQ-788 exhibits minimal activity towards other peptide hormone receptors tested at concentrations up to 10 μM. Its notable selectivity and potency for ETB receptors make BQ-788 valuable for investigating ET receptor-mediated physiological processes, such as bronchoconstriction.
- 1. Juliano T. Freitas, Jesus Lopez, et al. "The immunosuppressive role of Edn3 over‐expression in the melanoma microenvironment." Pigment Cell Melanoma Res. 2021 Nov;34(6):1084-1093. PMID:34288510
- 2. Huang X, Chen C, et al. "Transdermal BQ-788/EA@ZnO quantum dots as targeting and smart tyrosinase inhibitors in melanocytes." Mater Sci Eng C Mater Biol Appl. 2019 Sep;102:45-52. PMID:31147016
| Physical Appearance | A solid |
| Storage | Desiccate at RT |
| M.Wt | 663.78 |
| Cas No. | 156161-89-6 |
| Formula | C34H50N5NaO7 |
| Solubility | ≥33.2 mg/mL in DMSO; ≥2.71 mg/mL in H2O with gentle warming and ultrasonic; ≥16.2 mg/mL in EtOH |
| Chemical Name | sodium;(2R)-2-[[(2R)-2-amino-3-(1-methoxycarbonylindol-3-yl)propanoyl]-[(2S)-2-[[(2R,6S)-2,6-dimethylpiperidine-1-carbonyl]amino]-4,4-dimethylpentanoyl]amino]hexanoate |
| SDF | Download SDF |
| Canonical SMILES | CCCCC(C(=O)[O-])N(C(=O)C(CC1=CN(C2=CC=CC=C21)C(=O)OC)N)C(=O)C(CC(C)(C)C)NC(=O)N3C(CCCC3C)C.[Na+] |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
|
Cell lines |
hGH and pCASM cells |
|
Preparation method |
The solubility of this compound in DMSO is > 33.2 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
|
Reacting condition |
100 μM |
|
Applications |
BQ-788 (100 μM) did not increase [Ca2+]i in both hGH and pCASM cells. However, BQ-788 significantly inhibited ET-1-induced increases in [Ca2+]i in both cell lines. |
| Animal experiment [1]: | |
|
Animal models |
Rats |
|
Dosage form |
1 mg/kg; i.v. |
|
Applications |
BQ-788 (1 mg/kg) i.v. administered 5 mins before ET-1 injection completely inhibited the depressor response, correspondingly, causing a rapid onset of apparently enhanced pressor response. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1]. Ishikawa K, Ihara M, Noguchi K, et al. Biochemical and pharmacological profile of a potent and selective endothelin B-receptor antagonist, BQ-788. Proceedings of the National Academy of Sciences, 1994, 91(11): 4892-4896. | |
Quality Control & MSDS
- View current batch:
Chemical structure
Related Biological Data
Related Biological Data
