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

Product information

CAS Number: 222318-55-0

Molecular Weight: 454.54

Formula: C25H31FN4O3

Chemical Name: (4E)-1-{4-[4-(4-fluorobenzoyl)piperidin-1-yl]butyl}-4-(hydroxyimino)-7-methyl-1H,4H,5H,6H,7H,8H-pyrrolo[2,3-c]azepin-8-one

Smiles: CN1CC/C(=N\O)/C2C=CN(CCCCN3CCC(CC3)C(=O)C3C=CC(F)=CC=3)C=2C1=O

InChiKey: NJODDWBWSIFQMT-HPNDGRJYSA-N

InChi: InChI=1S/C25H31FN4O3/c1-28-14-11-22(27-33)21-10-17-30(23(21)25(28)32)13-3-2-12-29-15-8-19(9-16-29)24(31)18-4-6-20(26)7-5-18/h4-7,10,17,19,33H,2-3,8-9,11-16H2,1H3/b27-22+

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

(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).

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.

Products are for research use only. Not for human use.