BVD 10
目录号 : GC14393NPY Y1 receptor antagonist,highly selective
Cas No.:262418-00-8
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Ki: 25.7 nM for Y1
Neuropeptide Y (NPY), a 36-residue peptide amide isolated originally from porcine brain, is a member of homologous hormone family including peptide YY (PYY) and pancreatic polypeptide (PP). It is the most abundant peptide in the mammalian brain and has been shown to exhibit a wide spectrum of central and peripheral activities. These actions are mediated by at least six G-protein coupled receptor subtypes denoted as Y1, Y2, Y3, Y4, Y5, and y6. BVD 10 is a highly selective and potent neuropeptide Y (NPY) Y1 receptor antagonists.
In vitro: The inability to form such hydrogen bonding in BVD 10 may prevent or perturb the C-terminus reverse turn, which may contribute, at least in part, to the increased Y1 selectivity [1]. Moreover, BVD 10 and its NPY analogue peptide BVD15 were characterized conformationally. The two peptides exhibit different secondary structure characteristics in trifluoroethanol. Molecular modeling studies suggested that the C-terminus Tyr9 is oriented in different directions in the two peptides. The difference in the structures observed may contribute to the Y1 selectivity of BVD 10 relative to BVD 15 [2].
In vivo: No animal in vivo data have been reported so far.
Clinical trial: Up to now, BVD 10 is still in the preclinical development stage.
References:
[1] Balasubramaniam A, Dhawan VC, Mullins DE, Chance WT, Sheriff S, Guzzi M, Prabhakaran M, Parker EM. Highly selective and potent neuropeptide Y (NPY) Y1 receptor antagonists based on [Pro(30), Tyr(32), Leu(34)]NPY(28-36)-NH2 (BW1911U90). J Med Chem. 2001 May 10;44(10):1479-82.
[2] Jois SD, Balasubramaniam A. Conformation of neuropeptide Y receptor antagonists: structural implications in receptor selectivity. Peptides. 2003 Jul;24(7):1035-43.
Cas No. | 262418-00-8 | SDF | |
化学名 | (S,Z)-1-((S)-2-((Z)-((2S,3S)-2-amino-1-hydroxy-3-methylpentylidene)amino)-4-hydroxy-4-iminobutanoyl)-N-((4S,5Z,7S,8Z,10S,11Z,13S,14Z,16S,17Z,19S,20S)-7,13-bis(3-guanidinopropyl)-6,9,12,15,18-pentahydroxy-4,16-bis(4-hydroxybenzyl)-10-isobutyl-20-methyl-3-o | ||
Canonical SMILES | CC[C@]([C@@](N)([H])/C(O)=N/[C@@](C(N1CCC[C@@]1([H])/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](C(OC)=O)([H])CC2=CC=C(O)C=C2)([H])CCCNC(N)=N)([H])CC(C)C)([H])CCCNC(N)=N)([H])CC3=CC=C(O)C=C3)([H])[C@@](CC)([H])C)=O)( | ||
分子式 | C58H92N16O13 | 分子量 | 1221.46 |
溶解度 | Soluble to 1 mg/ml in Water | 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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 0.8187 mL | 4.0935 mL | 8.1869 mL |
5 mM | 0.1637 mL | 0.8187 mL | 1.6374 mL |
10 mM | 0.0819 mL | 0.4093 mL | 0.8187 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 | |||
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% 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。
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