Adrenorphin
(Synonyms: H2N-Tyr-Gly-Gly-Phe-Met-Arg-Arg-Val-amide ) 目录号 : GP10109Adrenorphin 是一种阿片样物质八肽,作为 μ-阿片样物质受体的有效激动剂,Ki 为 12 nM。
Cas No.:88377-68-8
Sample solution is provided at 25 µL, 10mM.
Adrenorphin (metorphamide) is a potent inhibitor of nicotine-induced adrenaline and noradrenaline release with IC50 value of 10 μM [1].
Adrenorphin (metorphamide) is an endogenous, C-terminally amidated, opioid octapeptide (Tyr-Gly-Gly-Phe-Met-Arg-Arg-Val-NH2) that is produced from proteolytic cleavage of proenkephalin A and is widely distributed throughout the mammalian brain [2].
Adrenorphin (metorphamide) is selective nicotine-induced adrenaline and noradrenaline release inhibitor and has higher than 100-fold more potent than the reported nicotine-induced adrenaline and noradrenaline release inhibitor Met5-enkephalin. When tested with bovine adrenal chromaffin cells, Adrenorphin (metorphamide) showed inhibition on 5 μM nicotine-induced ATP release by almost 50% at 5μM and the inhibition was not in a dose-dependent manner [1]. In bioassays and binding assays, Metorphamide exhibited high μ-binding activity, as well as κ-binding activity with nearly half percent toμ-binding activity, while showed no activity on δ-binding [2].
References:
[1]. Marley, P.D., K.I. Mitchelhill, and B.G. Livett, Metorphamide, a novel endogenous adrenal opioid peptide, inhibits nicotine-induced secretion from bovine adrenal chromaffin cells. Brain Res, 1986. 363(1): p. 10-7.
[2]. Weber, E., et al., Metorphamide: isolation, structure, and biologic activity of an amidated opioid octapeptide from bovine brain. Proc Natl Acad Sci U S A, 1983. 80(23): p. 7362-6.
Cas No. | 88377-68-8 | SDF | |
别名 | H2N-Tyr-Gly-Gly-Phe-Met-Arg-Arg-Val-amide | ||
化学名 | Adrenorphin | ||
Canonical SMILES | CC(C)C(C(=O)N)NC(=O)C(CCCN=C(N)N)NC(=O)C(CCCN=C(N)N)NC(=O)C(CCSC)NC(=O)C(CC1=CC=CC=C1)NC(=O)CNC(=O)CNC(=O)C(CC2=CC=C(C=C2)O)N | ||
分子式 | C44H69N15O9S | 分子量 | 984.18 |
溶解度 | ≥ 98.4mg/mL in DMSO | 储存条件 | Store 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。 |
||
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 | 1.0161 mL | 5.0804 mL | 10.1607 mL |
5 mM | 0.2032 mL | 1.0161 mL | 2.0321 mL |
10 mM | 0.1016 mL | 0.508 mL | 1.0161 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