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Chemical Structure| 156161-89-6 Chemical Structure| 156161-89-6

Structure of BQ-788 sodium salt
CAS No.: 156161-89-6

Chemical Structure| 156161-89-6

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BQ-788 sodium salt is a potent and selective ETB receptor antagonist, inhibiting ET-1 binding to ETB receptors in human Girrardi heart cells with an IC50 of 1.2 nM.

Synonyms: BQ-788 Sodium; BQ-788 (sodium salt); BQ788

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Product Details of BQ-788 sodium salt

CAS No. :156161-89-6
Formula : C34H50N5NaO7
M.W : 663.78
SMILES Code : CCCC[C@@H](NC([C@H](NC([C@@H](NC(N1[C@H](C)CCC[C@@H]1C)=O)CC(C)(C)C)=O)CC2=CN(C(OC)=O)C3=C2C=CC=C3)=O)C([O-])=O.[Na+]
Synonyms :
BQ-788 Sodium; BQ-788 (sodium salt); BQ788
MDL No. :MFCD00797882

Safety of BQ-788 sodium salt

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of BQ-788 sodium salt

GPCR

Isoform Comparison

Biological Activity

Description
BQ-788 sodium salt is a potent and selective ETB receptor antagonist, with an IC50 of 1.2 nM for inhibiting ET-1 binding to ETB receptors in human Girrardi heart cells.

In Vitro:

Cell Line
Concentration Treated Time Description References
Human umbilical vein endothelial cells (HUVECs) 10 μM 3 h BQ-788 significantly reduced parasite invasion of HUVECs Br J Pharmacol. 2012 Mar;165(5):1333-47
Human smooth muscle cells (HSMCs) 10 μM 3 h BQ-788 significantly reduced parasite invasion of HSMCs Br J Pharmacol. 2012 Mar;165(5):1333-47
CHO cells overexpressing ETBR 10 μM 3 h BQ-788 significantly reduced parasite uptake by CHO-ETBR cells Br J Pharmacol. 2012 Mar;165(5):1333-47
rat posterior cerebral arteries 100 nM 15 min The increased sensitivity to ET-1 in OSA rat posterior cerebral arteries was abolished by BQ-788, an ETBR antagonist J Cereb Blood Flow Metab. 2015 Mar;35(3):402-11
guineapig perfused lung 10 nM 15 min BQ-788 completely abolished the thromboxane A2 release induced by the selective ETB receptor agonist IRL1620. Br J Pharmacol. 1994 Dec;113(4):1257-62
guineapig perfused lung 1, 5, 10 nM 15 min BQ-788 significantly reduced endothelin-1-induced thromboxane A2 release by 17±2.5%, 70±5.0%, and 93±2.1% respectively. Br J Pharmacol. 1994 Dec;113(4):1257-62
Rabbit pulmonary arterial membranes 1μM 4 h To study the inhibitory effect of BQ-788 on [125I]-ET-1 specific binding. Results showed that BQ-788 completely inhibited the BQ-123-resistant component of [125I]-ET-1 specific binding. Br J Pharmacol. 1994 Oct;113(2):336-8

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Hamsters Hamster cheek pouch (HCP) Topical application 10 μM Single application, observed for 60 minutes BQ-788 significantly reduced TCT-induced leucocyte accumulation Br J Pharmacol. 2012 Mar;165(5):1333-47
Wistar rats Chronic unpredictable stress model Intraperitoneal injection 1 mg/kg Once daily for four weeks BQ-788, as a specific ETBR blocker, was co-administered with Dapagliflozin and partially negated the antidepressant effects of Dapagliflozin, verifying the importance of ETBR signaling in antidepressant action. Neurotherapeutics. 2021 Oct;18(4):2664-2681

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.51mL

0.30mL

0.15mL

7.53mL

1.51mL

0.75mL

15.07mL

3.01mL

1.51mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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