trans-ACPD
Based on 1 Customer Validation
trans-ACPD, a metabotropic receptor agonist, produces calcium mobilization and an inward current in cultured cerebellar Purkinje neurons.
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- Pureza: 98.0%
- No. CAS: 67684-64-4
- Fòrmula: C7H11NO4
- Peso molecular:173.17
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Actividad biológica
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mGluR |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
>100 μM
Compound: 16
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Stimulation of [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells; Inactive
Stimulation of [3H]phosphatidylinositol accumulation by rat Metabotropic glutamate receptor 4 co-expressed with Gqi9 protein in HEK 293 cells; Inactive
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[PMID: 15801843] |
| HEK293 | EC50 |
>1000 μM
Compound: 1/ (1S,3R -)-ACPD
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Agonist activity against Metabotropic glutamate receptor 4 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation
Agonist activity against Metabotropic glutamate receptor 4 expressed in HEK 293 cells was evaluated by measuring total inositol phosphate accumulation
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[PMID: 9301676] |
Excitatory amino acid (EAA) analogues activate receptors that are coupled to the increased hydrolysis of phosphoinositides (PIs). In these studies, hippocampal slices are prepared from neonatal rats (6-11 days old) to characterize the effects of EAA analogues on these receptors. The concentrations of trans-ACPD required to evoke half-maximal stimulation (EC50 value) is 51 μM. DL-2-Amino-3-phosphonopropionate (DL-AP3) is also equipotent as an inhibitor of PI hydrolysis stimulated by ibotenate, quisqualate, and trans-ACPD (IC50 values are 480-850 μM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 67684-64-4
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Appearance Solid
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Peso molecular 173.17
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Fòrmula C7H11NO4
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Color White to off-white
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SMILES
O=C([C@]1(N)C[C@@H](C(O)=O)CC1)O
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Synonyms
Trans-(±)-ACP
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvente y solubilidad
DMSO : 50 mg/mL (288.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 3.57 mg/mL (20.62 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (14.44 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 5 mg/mL (28.87 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
Mice[3]
Male Swiss mice (25-35 g) are used. Intrathecal injections are given to fully conscious mice. Briefly, the animals are manually restrained, and a 30-gauge needle connected by a polyethylene tube to a 25 μL Hamilton gas-tight syringe is inserted through the skin and between the vertebrae into the subdural space of the L5-L6 spinal segments. Intrathecal injections (5 μL/site) are administered over a period of 5 s. Biting behaviour is defined as a single head movement directed at the flanks or hind limbs, resulting in contact of the animal's snout with the target organ. The nociceptive response is elicited by NMDA (450 pmol/site, a selective agonist of the NMDA glutamatergic ionotropic receptor), kainate (110 pmol/site, a selective agonist of the kainate subtype of glutamatergic ionotropic receptors), and trans-ACPD (50 nmol/site, a non-selective agonist of metabotropic glutamate receptors, which is active at group I and group II), TNF-α (0.1 pmol/site) and IL-1β (1 pmol/site) or saline (5 μL/site, i.t.). The amount of time the animal spent biting or licking the caudal region is taken as evidence of nociception and is evaluated following local post injections of the following agonists: NMDA (5 min), kainate (4 min), and trans-ACPD TNF-α, and IL-1β (15 min). Animals received GM (100 mg/kg, i.p.) 0.5 h before intrathecal injection of 5 μL of the drugs, while control animals received a similar volume of saline (10 mL/kg, i.p.).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Linden DJ, et al. Trans-ACPD, a metabotropic receptor agonist, produces calcium mobilization and an inward current in cultured cerebellar Purkinje neurons. J Neurophysiol. 1994 May;71(5):1992-8. [Content Brief]
[2]. Littman L, et al. Multiple mechanisms for inhibition of excitatory amino acid receptors coupled to phosphoinositide hydrolysis. J Neurochem. 1992 Nov;59(5):1893-904. [Content Brief]
[3]. Córdova MM, et al. Polysaccharide glucomannan isolated from Heterodermia obscurata attenuates acute and chronic pain in mice. Carbohydr Polym. 2013 Feb 15;92(2):2058-64. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 5.7747 mL | 28.8737 mL | 57.7474 mL | 144.3685 mL |
| 5 mM | 1.1549 mL | 5.7747 mL | 11.5495 mL | 28.8737 mL | |
| 10 mM | 0.5775 mL | 2.8874 mL | 5.7747 mL | 14.4368 mL | |
| 15 mM | 0.3850 mL | 1.9249 mL | 3.8498 mL | 9.6246 mL | |
| 20 mM | 0.2887 mL | 1.4437 mL | 2.8874 mL | 7.2184 mL | |
| DMSO | 25 mM | 0.2310 mL | 1.1549 mL | 2.3099 mL | 5.7747 mL |
| 30 mM | 0.1925 mL | 0.9625 mL | 1.9249 mL | 4.8123 mL | |
| 40 mM | 0.1444 mL | 0.7218 mL | 1.4437 mL | 3.6092 mL | |
| 50 mM | 0.1155 mL | 0.5775 mL | 1.1549 mL | 2.8874 mL | |
| 60 mM | 0.0962 mL | 0.4812 mL | 0.9625 mL | 2.4061 mL | |
| 80 mM | 0.0722 mL | 0.3609 mL | 0.7218 mL | 1.8046 mL | |
| 100 mM | 0.0577 mL | 0.2887 mL | 0.5775 mL | 1.4437 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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