Antihypertensive agent 7
Antihypertensive agent 7 is a vasodilator. Antihypertensive agent 7 acts on vascular endothelial cells to activate the PI3K/AKT signaling axis, increase phosphorylated eNOS, release NO, activate the sGC/cGMP pathway in smooth muscle cells, and synergistically activate multiple K+ channels in vascular smooth muscle (Kir/Kv/KCa/KATP, thereby inducing endothelium-dependent vasodilation. Antihypertensive agent 7 can be used in the research of hypertension.
For research use only. We do not sell to patients.
- Formula: C20H22FN3O3
- Molecular Weight:371.41
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Antihypertensive agent 7 (Compound A24) at concentrations of 3.75-60 μM induces potent, concentration-dependent relaxation in endothelium-intact rat thoracic aortic rings, with an EC50 of 21.47 μM and a maximum relaxation rate of 97.24%[1].
The vasodilatory effect of Antihypertensive agent 7 (3.75-60 μM) is mainly endothelium-dependent, as the maximum relaxation amplitude of endothelium-denuded rat thoracic aortic rings is significantly reduced to 38.49%[1].
The vasodilatory effect of Antihypertensive agent 7 (3.75-60 μM; 20 min) on intact endothelium rat thoracic aortic rings is mediated by the PI3K/AKT signaling pathway, as pretreatment with pathway inhibitors significantly attenuates this response[1].
The vasodilatory effect of Antihypertensive agent 7 (3.75-60 μM; 20 min) on rat thoracic aortic rings with intact endothelium involves the eNOS/NO/sGC signaling pathway, as pretreatment with pathway inhibitors significantly attenuates this response[1].
Antihypertensive agent 7 (60 μM; 15-60 min) activates AKT in a time-dependent manner in human umbilical vein endothelial cells, with the maximum phosphorylation level observed after treatment with 60 μM for 30 min[1].
Antihypertensive agent 7 (15-60 μM; 30 min) increases the phosphorylation levels of AKT and eNOS in human umbilical vein endothelial cells in a concentration-dependent manner[1].
The vasodilatory effect of Antihypertensive agent 7 (3.75-60 μM; 20 min) on endothelium-intact rat thoracic aortic rings is independent of the activation of muscarinic receptors and β-adrenergic receptors[1].
Antihypertensive agent 7 (3.75-60 μM; 20 min) exerts vasodilatory effects on rat thoracic aortic rings with intact endothelium independent of the PGI2 signaling pathway[1].
The vasodilatory effect of Antihypertensive agent 7 (3.75-60 μM; 20 min) on endothelium-intact rat thoracic aortic rings involves the activation of multiple potassium channel subtypes, including KATP, KCa, KV and KIR channels[1].
Antihypertensive agent 7 (60 μM) does not affect ROCCs- or VDCCs-mediated vasoconstriction in rat thoracic aortic rings[1].
Antihypertensive agent 7 (60 μM) does not affect vasoconstriction mediated by sarcoplasmic reticulum Ca2+ release in rat thoracic aortic rings[1].
Antihypertensive agent 7 (2.5-80 μM; 24 h) exhibits no significant cytotoxicity against human umbilical vein endothelial cells at concentrations up to 80 μM following 24 h of treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Sprague-Dawley (SD) (male, 250-300 g, L-NAME-induced hypertension)[1]
-
Dosage:20 mg/kg; 40 mg/kg; 60 mg/kg
-
Administration:i.p.; daily; 5 weeks
-
Result:Reduced systolic blood pressure (SBP) to ~115 mmHg by week 9 in the 60 mg/kg group, with SBP significantly lower than the L-NAME model group at all measured time points.
Exerted dose-dependent reductions in diastolic blood pressure (DBP), with the 60 mg/kg group showing effects comparable to positive control CPT (10 mg/kg, i.p. daily).
Attenuated reduced body weight gain impairment and improved growth status at 20, 40, or 60 mg/kg doses.
Showed dose-dependent protective effects against multi-organ pathological damage: 20 mg/kg group showed partial improvement in heart, liver, spleen, and kidney tissue morphology; 40 mg/kg and 60 mg/kg progressively restored tissue structural integrity; 60 mg/kg group had histological outcomes comparable to CPT (10 mg/kg, i.p. daily) group.
Chemical Information
-
Molecular Weight 371.41
-
Formula C20H22FN3O3
-
SMILES
CC(N1CCC(CC1)NC(C2=CC(C3=C(OC)C=C(F)C=C3)=CC=N2)=O)=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
- Antihypertensive agent 7
- Antihypertensive agent7
- Antihypertensive agent-7
- PI3K
- Akt
- NO Synthase
- Guanylate Cyclase
- Potassium Channel
- ATP-sensitive K+ channels
- PI3K/AKT signaling pathway
- eNOS/NO/sGC signaling pathway
- L-NAME-induced hypertensive rats
- PI3K/AKT cascade
- rat thoracic aortic rings
- inward rectifier K+ channels
- calcium-activated K+ channels
- human umbilical vein endothelial cells
- voltage-gated K+ channels
- Inhibitor
- inhibitor
- inhibit