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BQ-788 sodium salt

Name: BQ-788 sodium salt
Brand: TargetMol
SKU: T10595L
Price: 106 USD
Availability: InStock
Rating: 5 (10 reviews)

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Purity: 98.11%

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BQ-788 sodium salt is a potent and selective antagonist of the Endothelin receptor type B, inhibiting the binding of Endothelin-1 to the receptor at nanomolar concentrations (reported IC₅₀ ≈ 1.2 nM).

Cas No. 156161-89-6

Pack Size	Price	USA Stock	Global Stock
1 mg	$106	-	In Stock
5 mg	$247	-	In Stock
10 mg	$355	-	In Stock
25 mg	$712	-	In Stock
50 mg	$1,130	-	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:98.11%

Appearance:Solid

Color:White

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COA HNMR MS HPLC

Product Introduction

Bioactivity

Description	BQ-788 sodium salt is a potent and selective antagonist of the Endothelin receptor type B, inhibiting the binding of Endothelin-1 to the receptor at nanomolar concentrations (reported IC₅₀ ≈ 1.2 nM).
Targets & IC50	ETB:1.2 nM
In vitro	BQ-788 sodium salt potently and competitively inhibits 125I-labeled ET-1 binding to ETB receptors in human Girrardi heart cells (hGH) with an IC50 of 1.2 nM, while poorly inhibiting ETA receptor binding in human neuro-blastoma cell line SK-N-MC cells (IC50, 1300 nM). BQ-788 sodium salt inhibits ET-1 bioactivities, including bronchoconstriction, cell proliferation, and clearance of perfused ET-1[1], and shows no agonistic activity up to 10 μM. BQ-788 sodium salt competitively inhibits vasoconstriction induced by an ETB-selective agonist (pA2, 8.4).
In vivo	Administered intravenously at a dosage of 3 mg/kg/h, BQ-788 sodium salt effectively blocks the ETB receptor-mediated depressor responses induced by pharmacological levels of ET-1 or sarafotoxin6c (0.5 nmol/kg) in conscious rats, without affecting pressor responses. In Dahl salt-sensitive hypertensive rats, this dosage of BQ-788 sodium salt Results: in a significant increase in blood pressure, approximately 20 mm Hg. BQ-788 sodium salt is noted to inhibit ET-1-induced bronchoconstriction, tumor proliferation, and lipopolysaccharide-triggered organ failure [1]. BQ-788 sodium salt shifts the ET-1 dose-response curve eightfold to the left, highlighting a substantial role of ETB dilator receptors [2]. BQ-788 sodium salt significantly raises plasma ET-1 levels, indicating its potential as an ETB receptor blocker in vivo. In mice, intraplantar administration of 30 nmol BQ-788 sodium salt reduces mechanical and thermal hyperalgesia, oedema, and myeloperoxidase activity by significant margins, alongside diminishing overt pain-like behaviors.

Chemical Properties

Molecular Weight	664.80
Formula	C₃₄H₅₁N₅NaO₇
Cas No.	156161-89-6
Smiles	O=C(N1[C@H](CCC[C@H]1C)C)N[C@@H](CC(C)(C)C)C(N[C@@H](C(N[C@@H](C([O-])=O)CCCC)=O)CC2=CN(C(OC)=O)C3=CC=CC=C23)=O.[Na+]
Relative Density.	no data available

Storage & Solubility Information

Storage

Keep away from direct sunlight,Store under nitrogen Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 20.00 mg/mL (30.08 mM), Sonication is recommended.

H2O: 40.00 mg/mL (60.17 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.30 mg/mL (4.96 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO/H2O

	1mg	5mg	10mg	50mg
1 mM	1.5042 mL	7.5211 mL	15.0421 mL	75.2106 mL
5 mM	0.3008 mL	1.5042 mL	3.0084 mL	15.0421 mL
10 mM	0.1504 mL	0.7521 mL	1.5042 mL	7.5211 mL
20 mM	0.0752 mL	0.3761 mL	0.7521 mL	3.7605 mL

H2O

	1mg	5mg	10mg	50mg
50 mM	0.0301 mL	0.1504 mL	0.3008 mL	1.5042 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Keywords

ETBBQ788 sodium saltBQ-788 sodiumBQ 788 sodium salt

Related Tags: BQ-788 sodium salt chemical structure | BQ-788 sodium salt in vivo | BQ-788 sodium salt in vitro | BQ-788 sodium salt formula | BQ-788 sodium salt molecular weight