(4E)-SUN9221 

(4E)-SUN9221 is a potent antagonist of α1-adrenergic receptor and 5-HT2 receptor, with antihypertensive and anti-platelet aggregation activities.

(4E)-SUN9221 potently inhibits collagen-, ADP- and epinephrine-induced platelet aggregation, with IC₅₀s of 10 nM, 35 nM, 14 nM, respectively, in human platelet-rich plasma (PRP). (4E)-SUN9221 displays potent α1-adrenergic antagonist activity (pA2 =8.89±0.21) and 5-HT2 antagonist activity (pA2 =8.74±0.22)^[1].

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

(4E)-SUN9221 (1, 3, 10 mg/kg, p.o.) reduces the blood pressure in a dose-dependent manner in conscious spontaneously hypertensive rats (SHR). (4E)-SUN9221 (3 mg/kg) exhibits antihypertensive activity in SHR^[1].

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

454.54

C₂₅H₃₁FN₄O₃

222318-55-0

O=C(C1=C/2C=CN1CCCCN3CCC(C(C4=CC=C(F)C=C4)=O)CC3)N(C)CCC2=N/O

Room temperature in continental US; may vary elsewhere.

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

• [1]. Mizuno A, et al. Synthesis and pharmacological evaluation of pyrroloazepine derivatives as potent antihypertensive agents with antiplatelet aggregation activity. Chem Pharm Bull (Tokyo). 1999 Feb;47(2):246-56.  [Content Brief]