BWX 46
目录号 : GC14789
NPY Y5 receptor agonist,potent and highly selective
Cas No.:172997-92-1
Sample solution is provided at 25 µL, 10mM.
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IC50: 0.5 nM for Y5
The actions of neuropeptide Y (NPY) are mediated by at least six G-protein coupled receptors denoted as Y1, Y2, Y3, Y4, Y5, and y6. Investigations using receptor selective ligands and receptor knock-out mice show that NPY effects on feeding are mediated by both Y1 and Y5 receptors. BWX 46 is a Y5 receptor selective agonist.
In vitro: BWX 46 selectively bound Y5 receptors, and inhibited cAMP synthesis by Y5 cells with potencies comparable to that of NPY. In addition, BWX 46 (10 μM) exhibited no significant effect on the cAMP synthesis by Y1, Y2, and Y4 cells. Thus, BWX 46 constitutes the lowest molecular weight Y5 selective agonist reported to date [1].
In vivo: Intrahypothalamic-injection of 30 and 40 μg of BWX 46 stimulated the food intake by rats in a gradual manner, reaching maximal level 8 h after injection. This response was similar to that exhibited by other Y5 selective agonists, but differed from that of NPY, which exhibited a rapider orexigenic stimulus within 1 h [1].
Clinical trial: Up to now, BWX 46 is still in the preclinical development stage.
Reference:
[1] Ambikaipakan Balasubramaniam, Sulaiman Sheriff, Weixu Zhai, William T. Chance. Bis(31/31’){[Cys31, Nva34]NPY(27–36)-NH2}: a neuropeptide Y (NPY) Y5 receptor selective agonist with a latent stimulatory effect on food intake in rats. Peptides 23 (2002) 1485–1490
| Cas No. | 172997-92-1 | SDF | |
| 化学名 | (S,S,S,1Z,1'Z,2S,2'S)-N'1,N''1'-((R,S,6S,6'S,7Z,7'Z,9S,9'S,10Z,10'Z,12S,12'S,13Z,13'Z,15S,15'S,16Z,16'Z,18R,18'R,19Z,19'Z,21S,21'S)-18,18'-(disulfanediylbis(methylene))bis(1-amino-12-(3-guanidinopropyl)-8,11,14,17,20-pentahydroxy-6-((Z)-hydroxy(((S)-1-hyd | ||
| Canonical SMILES | CCC[C@@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](N)([H])CC1=CC=C(O)C=C1)([H])[C@@](CC)([H])C)([H])CC(O)=N)([H])CC(C)C)([H])CSSC[C@@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](N)([H])CC2=CC=C(O)C | ||
| 分子式 | C116H186N36O28S2 | 分子量 | 2597.07 |
| 溶解度 | ≥ 260.4 mg/mL in DMSO with ultrasonic, <12.99 mg/mL in Water, <12.99 mg/mL in EtOH | 储存条件 | Desiccate at -20°C |
| 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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.385 mL | 1.9252 mL | 3.8505 mL |
| 5 mM | 0.077 mL | 0.385 mL | 0.7701 mL |
| 10 mM | 0.0385 mL | 0.1925 mL | 0.385 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet