1. GPCR/G Protein
  2. Endothelin Receptor
  3. BQ-123 TFA

BQ-123 TFA 

Cat. No.: HY-12378A
Handling Instructions

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

For research use only. We do not sell to patients.

BQ-123 TFA Chemical Structure

BQ-123 TFA Chemical Structure

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Description

BQ-123 TFA is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 TFA inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension[1][2][3].

IC50 & Target

IC50: 7.3 nM (Endothelin A receptors)[1]
Ki: 25 nM (Endothelin A receptors)[2]

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].

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.
Molecular Weight

724.72

Formula

C₃₃H₄₃F₃N₆O₉

SMILES

O=C(N[[email protected]](C(N(CCC1)[[email protected]]1([H])C2=O)=O)([H])CC(O)=O)[[email protected]](NC([[email protected]@H](NC([[email protected]](N2)C(C)C)=O)CC(C)C)=O)CC3=CNC4=CC=CC=C34.OC(C(F)(F)F)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

BQ-123BQ123BQ 123Endothelin ReceptorpulmonaryarterysmoothmusclecellsbloodpressureInhibitorinhibitorinhibit

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Product Name:
BQ-123 TFA
Cat. No.:
HY-12378A
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