| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
BQ-3020 ammonium is a selective agonist of the endothelin B (ETB) receptor [22L8-L9]. Endothelin receptors are G protein-coupled receptors (GPCRs) with two main subtypes, ETA and ETB. BQ-3020 specifically activates the ETB receptor, which is primarily located on endothelial cells (where it mediates vasodilation and clearance of ET-1), smooth muscle cells (where it can cause vasoconstriction), and other tissues like the kidney and bladder. By binding to the ETB receptor, it mimics the actions of the endogenous ligand, endothelin-1 (ET-1).
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| ln Vitro |
In vitro, BQ-3020 ammonium is a highly potent and selective ETB receptor agonist. It inhibits the binding of [¹2⁵I]-ET-1 to porcine cerebellum ETB receptors with an IC₅0 of 0.2 nM, demonstrating high affinity [21L16-L17]. It is widely used in functional assays to study ETB-mediated signaling pathways. For example, in isolated tissue bath experiments, BQ-3020 is used to characterize the receptor pharmacology of ETB in various tissue types.
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| ln Vivo |
In vitro, BQ-3020 ammonium induces specific pharmacological effects via ETB receptor activation. For instance, it has been shown to cause concentration-dependent relaxation of pre-constricted rabbit mesenteric arteries (if the endothelium is intact, as ETB on endothelium produces NO) or contraction in certain vascular beds (if ETB on smooth muscle is dominant). The specific response is tissue- and species-dependent. In rabbit pulmonary artery, BQ-3020 elicits vasoconstriction, while in pig bladder neck strips, it induces relaxation [22L10-L12]. These effects are blocked by an ETB antagonist but not by an ETA antagonist.
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| Enzyme Assay |
In vivo, the activity of BQ-3020 ammonium is utilized to study the ETB receptor's role in cardiovascular regulation. For example, in anesthetized rats, administration of BQ-3020 can cause a biphasic response: an initial, transient vasodilation followed by a prolonged pressor response depending on the vascular bed and dose. It can also be used to study renal function, where ETB activation promotes natriuresis and diuresis. In a porcine model, BQ-3020 causes relaxation of the bladder neck, indicating a role for ETB in micturition [22L10-L12]. These studies help dissect the complex roles of ETB in health and disease.
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| Cell Assay |
The binding selectivity of BQ-3020 for ETB over ETA is determined using non-cellular radioligand binding assays. In these assays, membrane preparations from cells expressing recombinant human ETB or ETA receptors are used. A fixed concentration of a radiolabeled ligand (e.g., [¹2⁵I]-ET-1) is incubated with increasing concentrations of BQ-3020. The reaction is filtered, and the radioactivity is counted. The IC₅0 value (0.2 nM for ETB) is calculated. BQ-3020 shows >1000-fold selectivity for ETB over ETA in these assays.
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| Animal Protocol |
For in vitro cellular functional assays, cells that naturally express ETB (e.g., endothelial cells, certain smooth muscle cell lines) or cells transfected with ETB are used. Cells are pre-loaded with a fluorescent dye to measure intracellular calcium concentration ([Ca2+]i). BQ-3020 is added, and the change in fluorescence is monitored. ETB activation leads to a rapid and transient increase in [Ca2+]i via Gq protein coupling, even though ETB primarily signals through Gi/o. BQ-3020 can also be used to monitor inhibition of cAMP production (ETB couples to Gi/o) via a FRET-based assay.
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| ADME/Pharmacokinetics |
In vivo animal studies with BQ-3020 are typically performed in rodents (rats or mice) or rabbits to assess its cardiovascular or renal effects. In a standard protocol, a rat is anesthetized, and catheters are placed in the carotid artery (for blood pressure measurement) and the jugular vein (for drug infusion). BQ-3020 is administered as an intravenous bolus or as a continuous infusion (e.g., 0.1-10 nmol/kg). The primary endpoints are changes in mean arterial pressure (MAP) and heart rate. Additionally, urine can be collected from the bladder to measure the natriuretic and diuretic effects.
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| Toxicity/Toxicokinetics |
Pharmacokinetic (PK) data for BQ-3020 ammonium are not detailed in standard product literature. As a 16-amino acid peptide (Ac-Leu-Met-Asp-Lys-Glu-Ala-Val-Tyr-Phe-Ala-His-Leu-Asp-Ile-Ile-Trp) [21L12-L13], it is subject to rapid proteolytic degradation in vivo, leading to a very short half-life (on the order of minutes). It is not orally bioavailable and is typically administered intravenously in research settings.
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| References |
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| Additional Infomation |
Comprehensive toxicological data for BQ-3020 ammonium are not provided in standard product literature. As a research-use compound, standard safety assessments for acute toxicity are not typically described. As a potent vasoactive peptide, it can cause significant and rapid changes in blood pressure if administered systemically. For laboratory use, standard chemical safety precautions for handling peptides should be followed.
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| Molecular Formula |
C96H140N20O25S.XNH3
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| Molecular Weight |
2006.32 (free base)
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| Related CAS # |
BQ-3020;143113-45-5
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| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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