Convolamine
Based on 1 Customer Validation
Convolamine is a tropane alkaloid and a potent Sigma-1 receptor positive allosteric modulator with an IC50 value of 289 nM. Convolamine can be extracted from Convolvulus plauricalis. Convolamine exhibits cognitive-improving and neuroprotective properties. Convolamine can be used in research related to Wolfram syndrome and Alzheimer's disease.
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- Pureté : 99.89%
- CAS No.: 500-56-1
- Formule: C17H23NO4
- Masse moléculaire:305.37
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
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Sigma 1 Receptor 289 nM (IC50) |
Sigma 2 Receptor 13 μM (IC50) |
In Vitro
Convolamine (100 nM, 30 μM; 60-120 min) does not bind to the S1R agonist/antagonist binding site but has moderate affinity for S2R in Jurkat human leukemic T cell membranes, with an S2R IC50 of 13 μM[1].
Convolamine (0.1-30 μM; 30 min) acts as a positive modulator of S1R in GFP-S1R-oe CHO cells, with an IC50 of 289 nM for enhancing PRE-084-mediated S1R/BiP dissociation, but does not act as an S1R agonist on its own[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:GFP-S1R-overexpressing CHO (GFP-S1R-oe CHO) cells
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Concentration:30 μM (single-compound testing); 0.1, 0.3, 1, 3, 10 μM (positive modulation testing)
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Incubation Time:30 min at 37°C
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Result:Failed to dissociate S1R from BiP at concentrations up to 30 μM, confirming it is not an S1R agonist.
Shifted the PRE-084 IC50 from 468 nM to lower values (484 nM at 0.1 μM, 269 nM at 0.3 μM, 206 nM at 1 μM, 146 nM at 3 μM, 158 nM at 10 μM) when co-administered with increasing concentrations of PRE-084.
Had an IC50 of 289 nM for its positive modulatory effect.
In Vivo
Convolamine (1 mg/kg; i.p.) reverses learning and memory impairments in Wfs1ΔExon8 mice, restoring their performance in multiple behavioral tests to wild-type levels[1].
Convolamine (0.1-3 mg/kg; i.p.; single administration) exerts an anti-amnesic effect on dizocilpine-induced learning impairment via σ-1 receptor-mediated activity, with the peak efficacy observed at 1 mg/kg[1].
Convolamine (0.3-3 mg/kg; intraperitoneal injection; single administration) exerts neuroprotective effects against Amyloid-β[25-35]-induced learning impairment in mice, with the optimal efficacy observed at the dose of 1 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:wfs1abKO double-mutant line (5 days post-fertilization larvae); wfs1abWT wild-type line (5 days post-fertilization larvae)[1]
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Dosage:0.3 μM; 1 μM; 3 μM
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Administration:immersion; 24 hours
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Result:Dose-dependently abolished the hyperlocomotor response of wfs1abKO larvae without affecting basal locomotion in wfs1abWT larvae.
Co-treatment with 3 μM NE-100 attenuated convolamine's effect on wfs1abKO larvae (p = 0.07 vs. convolamine alone).
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Animal Model:Wfs1ΔExon8 (129S6/SvEvTac C57BL/6J background, 3 months old, male and female); Wfs1WT control littermates (3 months old, male and female)[1]
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Dosage:1 mg/kg
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Administration:i.p.; single dose
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Result:Significantly attenuated the deficit in spontaneous alternation in Wfs1ΔExon8 mice, bringing alternation percentages close to Wfs1WT levels.
Reversed the decreased step-through latency in passive avoidance and improved short-term memory index, latency to reach the platform location, and platform location crossings in the active avoidance probe test, with outcomes not significantly different from Wfs1WT controls.
Exploratory behavior (arm entries in Y-maze) was unaffected by treatment.
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Animal Model:Swiss CD-1 (RjOrl:SWISS, male, 7-9 weeks old)[1]
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Dosage:0.1 mg/kg; 0.3 mg/kg; 1 mg/kg; 3 mg/kg
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Administration:i.p.; single dose
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Result:Dose-dependently (bell-shaped curve) attenuated dizocilpine-induced deficits in spontaneous alternation in the Y-maze (significant at 0.1, 0.3, 1 mg/kg).
Reversed dizocilpine-induced decreases in step-through latency (significant at 1 mg/kg) and increases in escape latency (significant at 0.3, 1, 3 mg/kg) in passive avoidance.
Co-treatment with NE-100 blocked convolamine's effect on alternation and step-through latency.
Did not affect dizocilpine-induced hyperlocomotion in the Y-maze.
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Animal Model:Swiss CD-1 (RjOrl:SWISS, male, 7-9 weeks old)[1]
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Dosage:0.3 mg/kg; 1 mg/kg; 3 mg/kg
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Administration:i.p.; single dose
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Result:At 0.3, 1, and 3 mg/kg significantly attenuated amyloid-β[25-35]-induced deficits in spontaneous alternation in the Y-maze.
At 1 mg/kg, restored a significant short-term memory index in active avoidance, improved latency to reach the platform location, and reversed the amyloid-β[25-35]-induced decrease in platform location crossings in the active avoidance probe test.
No significant effect was observed in passive avoidance.
Chemical Information
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CAS No. 500-56-1
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Appearance Solid
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Masse moléculaire 305.37
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Formule C17H23NO4
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Color White to off-white
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SMILES
O=C(C(C=C1)=CC(OC)=C1OC)O[C@H](C[C@]2([H])CC3)C[C@]3([H])N2C
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Structure Classification
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Initial Source
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 20 mg/mL (65.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2 mg/mL (6.55 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
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.
Pureté et documentation
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Fiche technique (281 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 3.2747 mL | 16.3736 mL | 32.7472 mL | 81.8679 mL |
| 5 mM | 0.6549 mL | 3.2747 mL | 6.5494 mL | 16.3736 mL | |
| 10 mM | 0.3275 mL | 1.6374 mL | 3.2747 mL | 8.1868 mL | |
| 15 mM | 0.2183 mL | 1.0916 mL | 2.1831 mL | 5.4579 mL | |
| 20 mM | 0.1637 mL | 0.8187 mL | 1.6374 mL | 4.0934 mL | |
| 25 mM | 0.1310 mL | 0.6549 mL | 1.3099 mL | 3.2747 mL | |
| 30 mM | 0.1092 mL | 0.5458 mL | 1.0916 mL | 2.7289 mL | |
| 40 mM | 0.0819 mL | 0.4093 mL | 0.8187 mL | 2.0467 mL | |
| 50 mM | 0.0655 mL | 0.3275 mL | 0.6549 mL | 1.6374 mL | |
| 60 mM | 0.0546 mL | 0.2729 mL | 0.5458 mL | 1.3645 mL |
Convolamine Related Classifications
HY-N15339 Related Classifications
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