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(4E)-SUN9221 is a potent dual α1-adrenergic receptor and 5-HT2 receptor antagonist, exhibiting antihypertensive and antiplatelet aggregation activities in hypertensive rats.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $700 | In Stock | |
5 mg | $1,800 | In Stock |
Description | (4E)-SUN9221 is a potent dual α1-adrenergic receptor and 5-HT2 receptor antagonist, exhibiting antihypertensive and antiplatelet aggregation activities in hypertensive rats. |
Targets&IC50 | Platelet aggregation:14 nM, Collagen:10 nM, ADP:35 nM |
In vitro | In human platelet-rich plasma (PRP), (4E)-SUN9221 potently inhibits collagen-, ADP-, and epinephrine-induced platelet aggregation, with IC50s of 10 nM, 35 nM, and 14 nM, respectively. Additionally, (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 | In conscious spontaneously hypertensive rats (SHR), (4E)-SUN9221 reduces blood pressure in a dose-dependent manner when administered orally at doses of 1, 3, and 10 mg/kg. Specifically, (4E)-SUN9221 at a dose of 3 mg/kg exhibits antihypertensive activity in SHR[1]. |
Molecular Weight | 454.54 |
Formula | C25H31FN4O3 |
Cas No. | 222318-55-0 |
Smiles | C(CCCN1CCC(C(=O)C2=CC=C(F)C=C2)CC1)N3C4=C(\C(=N\O)\CCN(C)C4=O)C=C3 |
Relative Density. | 1.29 g/cm3 (Predicted) |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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