Ercanetide
Based on 1 Customer Validation
Ercanetide (NNZ 2591) is a synthetic analogue of a small peptide of cyclic glycine proline (cGP). Ercanetide shows orally active and cross the blood-brain barrier. Ercanetide shows neuroprotective after ischemic brain injury. NNZ 2591 improves motor function in a rat model of Parkinson's disease. Ercanetide has the potential for the research of ischemic brain injury and angelman syndrome.
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- Purity: 99.67%
- CAS No.: 847952-38-9
- 화학식: C10H14N2O2
- 분자량:194.23
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보관: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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
Ercanetide (2, 20, 100 ng/rat; i.c.v.) shows neuroprotection in rats[2].
Ercanetide (3 mg/kg; s.c.; daily for 5 days) completely preventes brain damage and significantly reduces the L/R ratio of time taken to touch to the patch at 5 d after injury in rats[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:4 months, male young adult Wistar rats[1].
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Dosage:30 mg/kg
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Administration:P.o.; 10 min after the (scopolamine) i.p. administration.
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Result:Significantly reduced the number of M2AchR positive neurons, significantly reduced the density of synaptophysin in the CA3 and CA4 sub-regions, and altered TH terminal staining in the striatum.
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Animal Model:280-310 g adult male Wistar rats[2].
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Dosage:2, 20, 100 ng/rat
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Administration:I.c.v.; 2 h after HI injury
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Result:Reduced overall tissue damage in the sub-regions of the hippocampus, DG, cerebral cortex and the striatum.
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Animal Model:280-310 g adult male Wistar rats[2].
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Dosage:3 mg/kg
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Administration:S.c.; daily for 5 days
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Result:Significantly reduced the median of tissue damage scores in the CA1-2, CA3 and CA4 sub-regions of the hippocampus, the DG.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 847952-38-9
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Appearance Solid
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분자량 194.23
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화학식 C10H14N2O2
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Color White to off-white
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Synonyms
NNZ-2591
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 18.75 mg/mL (96.54 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)
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: ≥ 1.5 mg/mL (7.72 mM); Clear solution
This protocol yields a clear solution of ≥ 1.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (15.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 1.5 mg/mL (7.72 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (15.0 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.
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.
순도&문서
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Data Sheet (278 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Guan J, et al. NNZ-2591, a novel diketopiperazine, prevented scopolamine-induced acute memory impairment in the adult rat. Behav Brain Res. 2010 Jul 11;210(2):221-8. [Content Brief]
[2]. Guan J, et al. Peripheral administration of a novel diketopiperazine, NNZ 2591, prevents brain injury and improves somatosensory-motor function following hypoxia-ischemia in adult rats. Neuropharmacology. 2007 Nov;53(6):749-62. [Content Brief]
[3]. Copping NA, et al. Emerging Gene and Small Molecule Therapies for the Neurodevelopmental Disorder Angelman Syndrome. Neurotherapeutics. 2021 Jul;18(3):1535-1547. [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, 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 | 5.1485 mL | 25.7427 mL | 51.4854 mL | 128.7134 mL |
| 5 mM | 1.0297 mL | 5.1485 mL | 10.2971 mL | 25.7427 mL | |
| 10 mM | 0.5149 mL | 2.5743 mL | 5.1485 mL | 12.8713 mL | |
| 15 mM | 0.3432 mL | 1.7162 mL | 3.4324 mL | 8.5809 mL | |
| 20 mM | 0.2574 mL | 1.2871 mL | 2.5743 mL | 6.4357 mL | |
| 25 mM | 0.2059 mL | 1.0297 mL | 2.0594 mL | 5.1485 mL | |
| 30 mM | 0.1716 mL | 0.8581 mL | 1.7162 mL | 4.2904 mL | |
| 40 mM | 0.1287 mL | 0.6436 mL | 1.2871 mL | 3.2178 mL | |
| 50 mM | 0.1030 mL | 0.5149 mL | 1.0297 mL | 2.5743 mL | |
| 60 mM | 0.0858 mL | 0.4290 mL | 0.8581 mL | 2.1452 mL | |
| 80 mM | 0.0644 mL | 0.3218 mL | 0.6436 mL | 1.6089 mL |
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