Bioactivity | (4E)-SUN9221 is a potent antagonist of α1-adrenergic receptor and 5-HT2 receptor, with antihypertensive and anti-platelet aggregation activities. |
Invitro | (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]. |
In Vivo | (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]. |
Name | (4E)-SUN9221 |
CAS | 222318-55-0 |
Formula | C25H31FN4O3 |
Molar Mass | 454.54 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |