BQ-788 sodium salt
BQ-788 is a potent and selective antagonist of endothelin (ET) B-receptor with IC50 value of 1.2nM [1].
In the in vitro assay, BQ-788 prevents ET-1 from binding to ETB receptors in human Girardi heart cells with IC50 value of 1.2nM. The inhibition to ETA receptors is much weaker with IC50 value of 1300nM. BQ-788 also inhibits ET binding to ETB receptors with IC50 values of 0.9nM and 1.2nM in porcine cerebellar membranes and hGH cells, respectively. The inhibition effects are quite poor in pCASM cells and SK-N-MC cells with IC50 values of 280nM and 1300nM, respectively. BQ-788 is specific to ET receptors. It cannot significantly inhibit other peptide hormone receptors at concentration of 10μM. It is found that BQ-788 interacts with ETB receptors competitively in hGH cells. Moreover, the in vivo assay demonstrates that ETB receptors are responsible for ET-1-elicited bronchoconstriction in guinea pigs [1].
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.
- 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]: | |
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Cell lines |
hGH and pCASM cells |
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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. |
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Reacting condition |
100 μM |
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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]: | |
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Animal models |
Rats |
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Dosage form |
1 mg/kg; i.v. |
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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. |
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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. |
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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. | |
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