AP5
目录号 : GC35364
AP5 是一种有效的选择性 GPR40 受体激动剂，在大鼠 hIP1 实验中，AP5 作用于 GPR40 受体，EC50 为 0.49±0.28 nM。
Cas No.:1623194-37-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
AP5 exhibits potent and selective agonism for the GPR40 receptor with positive allosteric modulation of endogenous ligands (AgoPAM). AP5 demonstrates a rat hIP1 EC50 of 0.49±0.28 nM against the GPR40 receptor[1]. EC50: 0.49±0.28 nM (GPR40 Receptor)[1]
AP5 is a potent and selective GPR40 AgoPAM that demonstrates excellent in vivo efficacy. In the GK rat oral glucose tolerance test (oGTT), oral administration of AP5 1 h before an oral dextrose challenge shows that AP5 significantly reduces blood glucose levels compared to the vehicle. AP5 is determined to be more efficacious in this model, demonstrating maximally efficacious glucose lowering at a plasma concentration of 4.9 μM at 10 mg/kg[1].
[1]. Chen HY, et al. Structure-Activity Relationship of Novel and Selective Biaryl-Chroman GPR40 AgoPAMs. ACS Med Chem Lett. 2018 Jun 14;9(7):685-690.
| Cas No. | 1623194-37-5 | SDF | |
| Canonical SMILES | FC1=CC(C2=CC(OC)=NC=C2)=CC=C1[C@@H]3CCC(C=CC([C@H](C4CC4)[C@H](C)C(O)=O)=C5)=C5O3 | ||
| 分子式 | C28H28FNO4 | 分子量 | 461.52 |
| 溶解度 | Soluble 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。 |
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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 | 2.1668 mL | 10.8338 mL | 21.6675 mL |
| 5 mM | 0.4334 mL | 2.1668 mL | 4.3335 mL |
| 10 mM | 0.2167 mL | 1.0834 mL | 2.1668 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。
Hippocampal AP5 treatment impairs both spatial working and reference memory in radial maze performance in rats
Eur J Pharmacol 2015 Jul 5;758:137-41.PMID:25863255DOI:10.1016/j.ejphar.2015.03.080.
The possible involvement of hippocampal N-methyl-d-aspartate (NMDA) receptors in spatial reference and working memory was investigated. Rats were first trained in a four-baited/four-unbaited version of the eight-arm radial maze task in which only predetermined four arms for each rat were baited with a food pellet. After rats reached the learning criterion, their performance was tested under the treatment of a NMDA antagonist, AP5 (d,l-2-amino-5-phosphonopentanoic acid, 20-40nmol), or vehicle into the dorsal hippocampus through the bilaterally implanted guide cannulae. AP5 produced dose-dependent increments on both reference and working memory errors, but did not have any effect on the running speed. Additionally, there were significant correlations between the number of trials to criterion in acquisition and the number of reference and working memory errors induced by AP5 treatment. The results suggest that hippocampal NMDA receptors are involved in both spatial reference and working memory.
The Chemical Profiling, Docking Study, and Antimicrobial and Antibiofilm Activities of the Endophytic fungi Aspergillus sp. AP5
Molecules 2022 Mar 5;27(5):1704.PMID:35268806DOI:10.3390/molecules27051704.
Growing data suggest that Aspergillus niger, an endophytic fungus, is a rich source of natural compounds with a wide range of biological properties. This study aimed to examine the antimicrobial and antibiofilm capabilities of the Phragmites australis-derived endophyte against a set of pathogenic bacteria and fungi. The endophytic fungus Aspergillus sp. AP5 was isolated from the leaves of P. australis. The chemical profile of the fungal crude extract was identified by spectroscopic analysis using LC-HRESIMS. The fungal-derived extract was evaluated for its antimicrobial activity towards a set of pathogenic bacterial and fungal strains including Staphylococcus aureus, Pseudomonas aeruginosa, Proteus vulgaris, Klebsiella sp., Candida albicans, and Aspergillus niger. Moreover, antibiofilm activity toward four resistant biofilm-forming bacteria was also evaluated. Additionally, a neural-networking pharmacophore-based visual screening predicted the most probable bioactive compounds in the obtained extract. The AP5-EtOAc extract was found to have potent antibacterial activities against S. aureus, E. coli, and Klebsiella sp., while it exhibited low antibacterial activity toward P. Vulgaris and P. aeruginosa and displayed anticandidal activity. The AP5-EtOAc extract had significant antibiofilm activity in S. aureus, followed by P. aeruginosa. The active metabolites' antifungal and/or antibacterial activities may be due to targeting the fungal CYP 51 and/or the bacterial Gyr-B.
Intrastriatal AP5 differentially affects behaviors induced by local infusions of D1 vs. D2 dopamine agonists
Brain Res 1996 Nov 11;739(1-2):19-25.PMID:8955920DOI:10.1016/s0006-8993(96)00630-0.
Using bilateral infusions into the rat striatum, the effects of the competitive NMDA receptor antagonist 2-amino-5-phosphopentanoic acid (AP5) on behaviors induced by the dopamine (DA) D1 receptor agonist SKF 82526 (fenoldopam) or the D2 receptor agonist quinpirole were determined. These effects were tested in DA-replete (intact) rats and in rats that were receiving injections of the monoamine-depleting drug reserpine. In both intact and reserpinized rats, fenoldopam induced significant sniffing. This effect was attenuated by simultaneous co-infusion of AP5 in the reserpinized rats. Quinpirole induced locomotion, sniffing, and oral behaviors, all of which were attenuated by AP5 co-infusion in the intact rats. In contrast, AP5 enhanced the quinpirole-induced sniffing of reserpinized rats. These findings suggest that distinct D1/glutamate and D2/glutamate relationships exist in the striatum, and that the nature of the latter is influenced by DA tone.
Purification and characterization of peptides Ap2, Ap3 and AP5 (ω-toxins) from the venom of the Brazilian tarantula Acanthoscurria paulensis
Peptides 2021 Nov;145:170622.PMID:34363923DOI:10.1016/j.peptides.2021.170622.
Peptides isolated from spider venoms are of pharmacological interest due to their neurotoxic activity, acting on voltage-dependent ion channels present in different types of human body tissues. Three peptide toxins titled as Ap2, Ap3 and AP5 were purified by RP-HPLC from Acanthoscurria paulensis venom. They were partially sequenced by MALDI In-source Decay method and their sequences were completed and confirmed by transcriptome analysis of the venom gland. The Ap2, Ap3 and AP5 peptides have, respectively, 42, 41 and 46 amino acid residues, and experimental molecular masses of 4886.3, 4883.7 and 5454.7 Da, with the Ap2 peptide presenting an amidated C-terminus. Amongst the assayed channels - NaV1.1, NaV1.5, NaV1.7, CaV1.2, CaV2.1 and CaV2.2 - Ap2, Ap3 and AP5 inhibited 20-30 % of CaV2.1 current at 1 μM concentration. Ap3 also inhibited sodium current in NaV1.1, Nav1.5 and Nav1.7 channels by 6.6 ± 1.91 % (p = 0.0276), 4.2 ± 1.09 % (p = 0.0185) and 16.05 ± 2.75 % (p = 0.0282), respectively. Considering that Ap2, Ap3 and AP5 belong to the 'U'-unknown family of spider toxins, which has few descriptions of biological activity, the present work contributes to the knowledge of these peptides and demonstrates this potential as channel modulators.
Effects of intrahippocampal AP5 treatment on radial-arm maze performance in rats
Brain Res 1998 Jan 19;781(1-2):300-6.PMID:9507170DOI:10.1016/s0006-8993(97)01256-0.
The purpose of the present study was to investigate the possible involvement of hippocampal NMDA (N-methyl-d-aspartate) receptors in spatial memory in rats by means of intrahippocampal injection of an NMDA antagonist, AP5 (D,L-2-amino-5-phosphonopentanoic acid). In Expt. 1, spontaneous motor activity (locomotor activity and rearing) was measured in an open-field after bilateral AP5 injection into the hippocampus, and it was shown that AP5 did not affect general activities within the dosage used in the present study. In Expt. 2, radial-maze performance was observed after the intrahippocampal injection of AP5. Rats were required to consume all the pellets which were put on each of the eight arms of the maze without revisiting the arms. AP5 produced dose-dependent impairment on the choice performance in the radial-arm maze, but did not have any effect on their running time. These results suggest that hippocampal NMDA receptors are involved in spatial memory.