BIBO3304 TFA
目录号 : GC61530
BIBO3304 TFA 对人和大鼠神经肽 Y (NPY) Y1 受体具有亚纳摩尔亲和力，IC50 值分别为 0.38±0.06 nM 和 0.72±0.42 nM。
Cas No.:191868-14-1
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
|
Cell lines |
The thoracic aortic smooth muscle cell line of rats, A10 cells |
|
Preparation Method |
In experiments with BIBO3304 TFA, cells were incubated with indicated concentration of BIBO3304 TFA for 1 h prior to NPY stimulation. A10 cells stimulated with 200 nM NPY in 0.5% serum or 10% serum were incubated with NPY Y1 receptor antagonist 10 µM BIBO3304 TFA for 24 h. |
|
Reaction Conditions |
10 µM for 24h |
|
Applications |
Levels of Geminin were not significantly different between vehicle (0.5% serum) and 200 nM NPY (0.5% serum) groups, expression of Geminin was significantly up-regulated in 10% serum-cultured VSMCs co-incubated with 200 nM NPY compared with vehicle (10% serum) group. This modulation was effectively blocked by BIBO3304 TFA. |
| Animal experiment [2]: | |
|
Animal models |
Male Wistar rats |
|
Preparation Method |
BIBO3304 TFA and BIBP 3226 (1 and 10 nmol) were injected i.c.v. 5 min before apomorphine injection (0.5 mg/kg, s.c.). At least one day elapsed between successive treatments. |
|
Dosage form |
1 and 10 nmol, i.c.v. |
|
Applications |
Pretreatment with BIBO3304 TFA significantly inhibited amphetamine-induced hyperactivity. Both the increases in time moving, distance travelled and number of rearings was inhibited by BIBO3304 TFA pretreatment. |
|
References: [1]: Jiang Z, Zhou Y, Chen X, et al. Different effects of neuropeptide Y on proliferation of vascular smooth muscle cells via regulation of Geminin[J]. Molecular and cellular biochemistry, 2017, 433(1): 205-211. |
|
BIBO3304 TFA has subnanomolar affinity for both the human and the rat neuropeptide Y (NPY) Y1 receptor with IC50 values of 0.38±0.06 nM and 0.72±0.42 nM, respectively [1].
BIBO3304 TFA(10 μM, 24h) effectively blocked Geminin upregulation in 10% serum-cultured vascular smooth muscle cells (VSMC) induced by 200 nM NPY [2].
BIBO3304 TFA (5 μmol)-treated mice showed a significant increase in whole body bone mineral content after 4- and 8-weeks of treatment, and this effect was not observed in vehicle-treated mice [3]. BIBO3304 TFA treatment improved β-cell function and preserved functional β-cell mass, thereby resulting in better glycaemic control in both high-fat-diet/multiple low-dose streptozotocin- and db/db type 2 diabetic mice [4]. Periphery specific antagonism of Y1R signalling via the non-brain penetrable Y1R antagonist BIBO3304 TFA prevents diet-induced obesity via stimulating energy expenditure and whole-body thermogenesis [5].
References:
[1]. Wieland H A, Engel W, Eberlein W, et al. Subtype selectivity of the novel nonpeptide neuropeptide Y Y1 receptor antagonist BIBO 3304 and its effect on feeding in rodents[J]. British journal of pharmacology, 1998, 125(3): 549-555.
[2]. Jiang Z, Zhou Y, Chen X, et al. Different effects of neuropeptide Y on proliferation of vascular smooth muscle cells via regulation of Geminin[J]. Molecular and cellular biochemistry, 2017, 433(1): 205-211.
[3]. Sousa D M, Baldock P A, Enriquez R F, et al. Neuropeptide Y Y1 receptor antagonism increases bone mass in mice[J]. Bone, 2012, 51(1): 8-16.
[4]. Yang C H, Ann-Onda D, Lin X, et al. Elevated Neuropeptide Y1 Receptor Signaling Contributes to β-cell Dysfunction and Failure in Type 2 Diabetes[J]. bioRxiv, 2021.
[5]. Yan C, Zeng T, Lee K, et al. Peripheral-specific Y1 receptor antagonism increases thermogenesis and protects against diet-induced obesity[J]. Nature communications, 2021, 12(1): 1-20.
BIBO3304 TFA 对人和大鼠神经肽 Y (NPY) Y1 受体具有亚纳摩尔亲和力，IC50 值分别为 0.38±0.06 nM 和 0.72±0.42 nM[1]。
BIBO3304 TFA（10 μM，24 小时）有效阻断 200 nM NPY [2] 诱导的 10% 血清培养的血管平滑肌细胞 (VSMC) 中的 Geminin 上调。
BIBO3304 TFA（5 μmol）处理的小鼠在处理 4 周和 8 周后全身骨矿物质含量显着增加，而在载体处理的小鼠中未观察到这种效果 [3]< /sup>。 BIBO3304 TFA 治疗可改善 β 细胞功能并保留功能性 β 细胞群，从而在高脂肪饮食/多种低剂量链脲佐菌素和 db/db 2 型糖尿病小鼠中实现更好的血糖控制 [4] 。通过不可穿透的 Y1R 拮抗剂 BIBO3304 TFA 对 Y1R 信号的外周特异性拮抗作用可通过刺激能量消耗和全身产热来预防饮食诱导的肥胖[5]。
| Cas No. | 191868-14-1 | SDF | |
| Canonical SMILES | O=C(N[C@@H](C(NCC1=CC=C(CNC(N)=O)C=C1)=O)CCCNC(N)=N)C(C2=CC=CC=C2)C3=CC=CC=C3.O=C(O)C(F)(F)F | ||
| 分子式 | C31H36F3N7O5 | 分子量 | 643.66 |
| 溶解度 | DMSO: 100 mg/mL (155.36 mM) | 储存条件 | Store at -20°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.5536 mL | 7.7681 mL | 15.5362 mL |
| 5 mM | 0.3107 mL | 1.5536 mL | 3.1072 mL |
| 10 mM | 0.1554 mL | 0.7768 mL | 1.5536 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。