BIBP 3226 trifluoroacetate是一种强效的非肽类neuropeptide Y (NPY) Y1 受体拮抗剂，对rNPY Y1、hNPFF2和rNPFF的Ki值分别为1.1、79和108nM。
Cas No.:1068148-47-9
Sample solution is provided at 25 µL, 10mM.
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BIBP 3226 trifluoroacetate is a potent non-peptide neuropeptide Y (NPY) Y1 receptor antagonist with Ki values of 1.1, 79, and 108nM for rNPY Y1, hNPFF2, and rNPFF, respectively [1]. BIBP 3226 trifluoroacetate can bind to Y1 receptor by mimicking the C-terminal region of the native ligand NPY, and is regulation of feeding behavior and energy homeostasis [2]. BIBP 3226 trifluoroacetate has been widely used to characterize NPY receptor subtypes and to alleviate stress-induced hypertension[3].
In vitro, BIBP 3226 trifluoroacetate (30μM) treatment for 30 minutes significantly induced an increase in inositol phosphate accumulation in CHO-K1 cells expressing the human NPY Y1 receptor [4].
In vivo, BIBP 3226 trifluoroacetate via intravenous injection at a dose of 6mg/kg/h for 1.5 hours can alleviate the stress-induced tachycardia in awake spontaneously hypertensive rats[5]. In rats with spinal cord transection, a single intravenous injection of 0.5mg/kg dose of BIBP 3226 trifluoroacetate significantly inhibited the pressor response induced by exogenous NPY [6]. Intraperitoneal injection of 100μg/kg dose of BIBP 3226 trifluoroacetate every other day for 8 weeks stimulated excessive production of IL-12 in ApoE−/− mice fed with a high-fat diet and promoted the development of atherosclerosis[7].
References:
[1] Mollereau C, Gouardères C, Dumont Y, et al. Agonist and antagonist activities on human NPFF2 receptors of the NPY ligands GR231118 and BIBP3226[J]. British journal of pharmacology, 2001, 133(1): 1-4.
[2] Barreiros L, Silva E M P, Alencastre I S, et al. Determination of neuropeptide Y Y1 receptor antagonist BIBP 3226 and evaluation of receptor expression based on liquid chromatography coupled with tandem mass spectrometry[J]. Analytical and Bioanalytical Chemistry, 2020, 412(24): 6625-6632.
[3] Doods H N, Wieland H A, Engel W, et al. BIBP 3226, the first selective neuropeptide Y1 receptor antagonist: a review of its pharmacological properties[J]. Regulatory peptides, 1996, 65(1): 71-77.
[4] Vanderheyden P M L, Van Liefde I, DeBacker J P, et al. Effect of BIBP3226 on inositol phosphate accumulation and cytosolic calcium level in control and NPY Y1 receptor expressing CHO-K1 cells[J]. Regulatory peptides, 1998, 75: 191-199.
[5] Zhang W, Lundberg J M, Thorén P. Neuropeptide Y Y1 receptor antagonist (BIBP 3226) attenuates stress evoked tachycardia in conscious spontaneously hypertensive rats[J]. Cardiovascular drugs and therapy, 1997, 11(6): 801-806.
[6] Zhao X H, Sun X Y, Bergdahl A, et al. Renal and cardiovascular role of the neuropeptide Y Y1 receptor in ischaemic heart failure rats[J]. Journal of pharmacy and pharmacology, 1999, 51(11): 1257-1265.
[7] Jääskeläinen A E, Seppälä S, Kakko T, et al. Systemic treatment with neuropeptide Y receptor Y1-antagonist enhances atherosclerosis and stimulates IL-12 expression in ApoE deficient mice[J]. Neuropeptides, 2013, 47(2): 67-73.
BIBP 3226 trifluoroacetate是一种强效的非肽类neuropeptide Y (NPY) Y1 受体拮抗剂，对rNPY Y1、hNPFF2和rNPFF的Ki值分别为1.1、79和108nM[1]。BIBP 3226 trifluoroacetate可通过模拟天然配体NPY的C末端区域与 Y1 受体结合，并调节摄食行为和能量稳态[2]。BIBP 3226 trifluoroacetate已被广泛用于表征NPY受体亚型以及减轻应激诱导的高血压[3]。
在体外，30μM的BIBP 3226 trifluoroacetate处理表达人NPY Y1受体的CHO-K1细胞30分钟，显著诱导了肌醇磷酸积累的增加 [4]。
在体内，静脉注射6mg/kg/h剂量的BIBP 3226 trifluoroacetate 1.5小时，可减轻清醒自发性高血压大鼠的应激诱导的心动过速[5]。在脊髓切断大鼠中，单次静脉注射0.5mg/kg剂量的BIBP 3226 trifluoroacetate，显著抑制了外源性NPY诱导的升压反应[6]。每隔一天腹腔注射100μg/kg剂量的BIBP 3226 trifluoroacetate，持续8周，刺激了高脂饮食喂养的ApoE−/−小鼠过量产生IL-12，并促进了动脉粥样硬化的发展[7]。
| Cell experiment [1]: | |
Cell lines | CHO-K1 cells expressing the human NPY Y1 receptor |
Preparation Method | CHO-K1 cells were cultured in 75cm2 flasks in Dulbecco's Modified Essential Medium (DMEM) supplemented with l-glutamine (2mM), 2% of a stock solution containing 5000I.U./ml penicillin and 5000μg/ml streptomycin and 10% fetal bovine serum in a humidified incubator at 37°C and 5% CO2. The cells were plated in 12 well plates and cultured until almost confluent. The medium was replaced by DMEM containing only 10μM unlabelled myo-inositol and 1μCi/ml myo-[3H]-inositol and the cells were further grown for 20h in 5% CO2 at 37°C. Just before the incubation, the cells are washed three times with DMEM (2ml per well). After the last wash step, 1ml of IP incubation buffer (i.e. DMEM containing 0.1% BSA and 10mM LiCl) is added to each well, and the cells are preincubated for 15min at 37°C. Hereafter, the medium was removed and 900μl of IP incubation buffer was added in each well. Subsequently the incubation was started for 30min at 37°C, after addition of 100μl of IP buffer (basal value) or BIBP 3226 trifluoroacetate (0, 1, 10, and 30μM). The accumulation of inositol phosphates was determined. |
Reaction Conditions | 0, 1, 10, and 30μM; 30min |
Applications | BIBP 3226 trifluoroacetate treatment significantly induced an increase in inositol phosphate accumulation in CHO-K1 cells in a dose and time-dependent manner. |
| Animal experiment [2]: | |
Animal models | ApoE−/− mice |
Preparation Method | ApoE−/− mice (five weeks old) were housed in large polycarbonate maternity cages on ventilated racks at 22-23°C and kept under a 12:12 light/dark cycle, and were fed atherogenic high cholesterol diet for 8 weeks. The mice were divided into four treatment groups; the mice were injected intraperitoneally (i.p) with NPY (100μg/kg), BIBP 3226 trifluoroacetate (100μg/kg) or water (50μl) every other day. After 8 weeks’ diet, on the second day after the last injection, the mice were anesthetized with ketamine (7.5mg) and xylazine (3mg) i.p. Blood was collected with heart puncture and serum was separated by centrifugation and stored at -70°C until analyzed. The organs (spleen, liver, heart and aorta) were collected for analysis. |
Dosage form | 100μg/kg; every other day for 8 weeks; i.p. |
Applications | BIBP 3226 trifluoroacetate treatment significantly enhanced the IL-12 levels in serum and organs of ApoE−/− mice, and increased atherosclerotic lesion areas in ApoE−/− mice. |
References: | |
| Cas No. | 1068148-47-9 | SDF | |
| 化学名 | (R)-2-(2,2-diphenylacetamido)-5-guanidino-N-(4-hydroxybenzyl)pentanamide bis(2,2,2-trifluoroacetate) | ||
| Canonical SMILES | FC(F)(C(O)=O)F.OC1=CC=C(C=C1)CNC([C@@H](CCCNC(N)=N)NC(C(C2=CC=CC=C2)C3=CC=CC=C3)=O)=O.FC(F)(C(O)=O)F | ||
| 分子式 | C27H31N5O3.2CF3CO2H | 分子量 | 701.61 |
| 溶解度 | <7.02mg/ml in Water; <70.16mg/ml in DMSO | 储存条件 | Store at -20°C, protect from light |
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.4253 mL | 7.1265 mL | 14.2529 mL |
| 5 mM | 285.1 μL | 1.4253 mL | 2.8506 mL |
| 10 mM | 142.5 μL | 712.6 μL | 1.4253 mL |
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