BQ-123

Name: BQ-123
Brand: MedChemExpress
SKU: HY-12378
Rating: 5.0 (3 reviews)

Cat. No.: HY-12378 Purity: 99.91%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

BQ-123 is a potent and selective endothelin A (ETA) receptor antagonist with an IC₅₀ of 7.3 nM and a K_i of 25 nM. BQ-123 inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension.

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Custom Peptide Synthesis

BQ-123 화학구조

CAS No. : 136553-81-6

사이즈	재고	수량
1 mg	해외재고보유	Estimated Time of Arrival: December 31
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

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This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 3 publication(s) in Google Scholar

Other Forms of BQ-123:

BQ-123 TFA 견적 받기

3 Publications Citing Use of MCE BQ-123

Featured Recommendations

•Related Screening Libraries:

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View All Endothelin Receptor Isoform Specific Products:

View All Isoforms

ET_A ET_B

Biological Activity
순도&문서
References
고객리뷰

제품 설명

IC₅₀ & Target

ET_A

Cellular Effect

Cell Line	Type	Value	Description	References
A10	IC₅₀	14 1 Compound: 1	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor. In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	[PMID: 9667964]
SK-N-MC	IC₅₀	0.62 1 Compound: BQ-123	Antagonist activity at ETA receptor in human SKNMC cells assessed as inhibition of endothelin-1-mediated Ca2+ mobilization by fura-2/AM dye-based spectrofluorimetric method Antagonist activity at ETA receptor in human SKNMC cells assessed as inhibition of endothelin-1-mediated Ca2+ mobilization by fura-2/AM dye-based spectrofluorimetric method	[PMID: 27318985]
CHO	IC₅₀	> 1000 1 Compound: BQ-123	Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis	[PMID: 22862294]
CHO	IC₅₀	20.5 1 Compound: BQ-123	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	[PMID: 22862294]
CHO	IC₅₀	20.5 1 Compound: BQ-123	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	[PMID: 22862294]
CHO	IC₅₀	>1 3 Compound: BQ-123	Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis	[PMID: 22862294]
SK-N-MC	IC₅₀	0.62 1 Compound: BQ-123	Antagonist activity at ETA receptor in human SKNMC cells assessed as inhibition of endothelin-1-mediated Ca2+ mobilization by fura-2/AM dye-based spectrofluorimetric method Antagonist activity at ETA receptor in human SKNMC cells assessed as inhibition of endothelin-1-mediated Ca2+ mobilization by fura-2/AM dye-based spectrofluorimetric method	[PMID: 27318985]
A10	IC₅₀	14 1 Compound: 1	In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor. In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.	[PMID: 9667964]
CHO	IC₅₀	> 1000 1 Compound: BQ-123	Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis	[PMID: 22862294]
CHO	IC₅₀	20.5 1 Compound: BQ-123	Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis	[PMID: 22862294]
SK-N-MC	IC₅₀	0.62 1 Compound: BQ-123	Antagonist activity at ETA receptor in human SKNMC cells assessed as inhibition of endothelin-1-mediated Ca2+ mobilization by fura-2/AM dye-based spectrofluorimetric method Antagonist activity at ETA receptor in human SKNMC cells assessed as inhibition of endothelin-1-mediated Ca2+ mobilization by fura-2/AM dye-based spectrofluorimetric method	[PMID: 27318985]

In Vivo

Sustained infusions of BQ-123 (0.16-164 nmol/kg per min, intravenously, for 6 h) produces dose-dependent reductions in mean arterial pressure in spontaneously hypertensive rats (SHR), the maximal reduction being obtained with a dose of 16 nmol/kg per min^[4].
BQ-123 (3 mg/kg; i.v.; given 15 minutes before pentylenetetrazole (PTZ)) impedes the formation and spread of seizure to a great degree in PTZ (50 mg/kg; i.p.) +BQ-123 groups^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Wistar albino rats^[5]
Dosage:	3 mg/kg
Administration:	Intravenous injection; given 15 minutes before PTZ
Result:	Number of rats with major seizure decreased.

분자량

610.70

화학식

C₃₁H₄₂N₆O₇

CAS No.

136553-81-6

Appearance

Solid

Color

White to off-white

Sequence

Cyclo(d-Asp-Pro-d-Val-Leu-d-Trp)

Sequence Shortening

Cyclo(d-DP-d-VL-d-W)

선적

Room temperature in continental US; may vary elsewhere.

보관

Sealed storage, away from moisture and light

Powder	-80°C	2 years
	-20°C	1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

용액&용해도

In Vitro:

DMSO : 50 mg/mL (81.87 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.6375 mL	8.1873 mL	16.3747 mL
5 mM	0.3275 mL	1.6375 mL	3.2749 mL
10 mM	0.1637 mL	0.8187 mL	1.6375 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

몰농도 계산기
농도 희석 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (8.19 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (8.19 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (8.19 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

순도&문서

Purity: 99.91%

Select Batch:

Data Sheet (281 KB) SDS (396 KB)

COA (256 KB) HNMR (346 KB) RP-HPLC (255 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. Ihara M, et al. In vitro biological profile of a highly potent novel endothelin (ET) antagonist BQ-123 selective for the ETA receptor. J Cardiovasc Pharmacol. 1992;20 Suppl 12:S11-S14. [Content Brief]

[2]. Sakamoto A, et al. Distinct subdomains of human endothelin receptors determine their selectivity to endothelinA-selective antagonist and endothelinB-selective agonists. J Biol Chem. 1993 Apr 25;268(12):8547-53. [Content Brief]

[3]. Zamora MA, et al. BQ123, an ETA receptor antagonist, inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells. Am J Respir Cell Mol Biol. 1993;9(4):429-433. [Content Brief]

[4]. Douglas SA, et al. BQ-123, a selective endothelin subtype A-receptor antagonist, lowers blood pressure in different rat models of hypertension. J Hypertens. 1994;12(5):561-567. [Content Brief]

[5]. Erdogan H et al. The protective effects of endothelin-A receptor antagonist BQ-123 in pentylenetetrazole-induced seizure in rats. Hum Exp Toxicol, 2014 Oct, 33(10):1008-16. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.6375 mL	8.1873 mL	16.3747 mL	40.9366 mL
	5 mM	0.3275 mL	1.6375 mL	3.2749 mL	8.1873 mL
	10 mM	0.1637 mL	0.8187 mL	1.6375 mL	4.0937 mL
	15 mM	0.1092 mL	0.5458 mL	1.0916 mL	2.7291 mL
	20 mM	0.0819 mL	0.4094 mL	0.8187 mL	2.0468 mL
	25 mM	0.0655 mL	0.3275 mL	0.6550 mL	1.6375 mL
	30 mM	0.0546 mL	0.2729 mL	0.5458 mL	1.3646 mL
	40 mM	0.0409 mL	0.2047 mL	0.4094 mL	1.0234 mL
	50 mM	0.0327 mL	0.1637 mL	0.3275 mL	0.8187 mL
	60 mM	0.0273 mL	0.1365 mL	0.2729 mL	0.6823 mL
	80 mM	0.0205 mL	0.1023 mL	0.2047 mL	0.5117 mL

BQ-123 Related Classifications

Cardiovascular Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BQ-123136553-81-6BQ123BQ 123Endothelin ReceptorpulmonaryarterysmoothmusclecellsbloodpressureInhibitorinhibitorinhibit

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BQ-123

고객리뷰

Other Forms of BQ-123:

BQ-123 Related Antibodies

3 Publications Citing Use of MCE BQ-123

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Endothelin Receptor Isoform Specific Products:

Biological Activity

순도&문서

References

고객리뷰

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

BQ-123 Related Classifications

Keywords:

최근 본 상품:

고객리뷰

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report