| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
BQ-123 (Cyclo(D-trp-D-asp-pro-D-val-leu); BQ123; BQ 123) is a potent and selective antagonist of endothelin A receptor (ETAR) with an IC50 of 7.3 nM. It has been demonstrated that endothelin-1 increases the activity of neurons and glutaminergic synaptic transmission through endothelin-A receptors (ETAR) in the nucleus tractus solitarius neurons, which are crucial in epileptic seizures. Consequently, BQ-123, an ETAR antagonist, may reduce glutaminergic synaptic transmission and neuronal excitability. BQ123 decreases myocardial infarction after focal cerebral ischemia in rats and amplifies hypothermia induced by acetaminophen. In LPS-treated rats, BQ123 Activates Nrf2 to Stimulate Skeletal Muscle Antioxidant Defense. Following surgery for congenital heart disease, BQ123 lowers pulmonary vascular resistance. BQ123 shields against endothelial and myocardial reperfusion damage.
| Targets |
Endothelin A receptor ( IC50 = 7.3 nM )
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| ln Vivo |
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| Enzyme Assay |
BQ-123 is a potent and selective endothelin A receptor (ETAR) antagonist with IC50 of 7.3 nM.
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| Cell Assay |
BQ123 (10-6 M) blocked endothelin-1 (ET-1) (10-6 M)-induced [Ca2+]i increase in ETA-expressing cells by 95%. BQ-123 prevented ET-1-induced cellular contraction, [Ca2+ ]i mobilization, [3H]thymidine incorporation, MAP kinase activation, and MTT reduction in rat vascular smooth muscle cells (VSMC). However, MAP kinase activity and [Ca2+]i mobilization were not inhibited by BQ-123 in response to angiotensin II (Ang II) or arginine vasopressin (AVP).
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| Animal Protocol |
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| References |
| Molecular Formula |
C31H42N6O7
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| Molecular Weight |
610.7
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| Exact Mass |
610.31
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| Elemental Analysis |
C, 60.97; H, 6.93; N, 13.76; O, 18.34
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| CAS # |
136553-81-6
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| Related CAS # |
BQ-123 TFA
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| Appearance |
Solid powder
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| SMILES |
CC(C)C[C@H]1C(=O)N[C@@H](C(=O)N[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C(=O)N1)C(C)C)CC(=O)O)CC3=CNC4=CC=CC=C43
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| InChi Key |
VYCMAAOURFJIHD-PJNXIOHISA-N
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| InChi Code |
InChI=1S/C31H42N6O7/c1-16(2)12-21-27(40)33-22(13-18-15-32-20-9-6-5-8-19(18)20)28(41)35-23(14-25(38)39)31(44)37-11-7-10-24(37)29(42)36-26(17(3)4)30(43)34-21/h5-6,8-9,15-17,21-24,26,32H,7,10-14H2,1-4H3,(H,33,40)(H,34,43)(H,35,41)(H,36,42)(H,38,39)/t21-,22+,23+,24-,26+/m0/s1
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| Chemical Name |
2-[(3R,6R,9S,12R,15S)-6-(1H-indol-3-ylmethyl)-9-(2-methylpropyl)-2,5,8,11,14-pentaoxo-12-propan-2-yl-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-3-yl]acetic acid
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| Synonyms |
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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. |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (8.19 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (8.19 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5 mg/mL (8.19 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02966665 | Recruiting | Drug: BQ-123 Drug: BQ-123, MitoQ, BH4 |
Heart Failure Hypertension |
Russell Richardson | September 2008 | Phase 1 |
| NCT03679780 | Recruiting | Drug: BQ-123 Drug: BQ-788 Drug: L-Arginine |
Cardiovascular Diseases Vasoconstrictiony |
The University of Texas at Arlington |
October 1, 2018 | Phase 1 |
| NCT00759408 | Completed | Drug: BQ-123 | Pulmonary Hypertension | Brigham and Women's Hospital | February 1999 | Phase 2 |
| NCT02086253 | Completed | Drug: BQ-788 and/or BQ-123 | Healthy Conditions | University Hospital, Rouen | February 2014 | Not Applicable |
| NCT02124824 | Completed | Drug: BQ-123 | Heart Failure | VA Office of Research and Development |
September 1, 2014 | Early Phase 1 |
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