Amdiglurax phosphate
Based on 1 Customer Validation
Amdiglurax (NSI-189) phosphate is an orally active chemical entity with enhanced neurogenic activity. Amdiglurax phosphate up-regulates neurogenic factors such as BDNF (brain derived-neurotrophic factor) and SCF. Amdiglurax phosphate exhibits anti-depressant effect. Amdiglurax enhances synaptic plasticity and reduces cognitive dysfunction. Amdiglurax phosphate holds potential for psychiatric disorder research.
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- Purity : 99.75%
- CAS No.: 1270138-41-4
- 화학식: C22H33N4O5P
- 분자량:464.49
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보관:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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
제품 설명
In Vitro
Amdiglurax phosphate enhances cell proliferation and neurogenesis in primary rat neurons (hippocampus) cells[2].
NSI-189 significantly attenuates OGD (oxygen glucose deprivation)-mediated hippocampal cell death and increases Ki67 and MAP2 expression[2].
Amdiglurax phosphate up-regulates VEGF, GDNF, BDNF, SCF, BDNF and SCF levels in the hippocampal cells[2].
Amdiglurax (1.0-3.0 μM, 24 h) phosphate augments neurite outgrowth and mitochondrial function in adult rat DRG (Dorsal root ganglia) sensory neurons[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:adult rat DRG sensory neurons cells
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Concentration:1.0-3.0 μM
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Incubation Time:24 h
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Result:Significantly increased 24 h total neurite outgrowth in neurons from normal or diabetic rats.
In Vivo
Amdiglurax (10 mg/kg, p.o., daily, 16 weeks) phosphate prevents PNS (peripheral nervous system) and CNS (central nervous system) neuropathy in type 1 diabetic mice[3].
Amdiglurax (30 mg/kg, p.o., daily, 26 weeks) phosphate prevents peripheral neuropathy and ameliorates CNS and PNS neuropathy indb/db mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult Sprague-Dawley, male rats, 250 g, received experimental stroke surgery using the middle cerebral artery occlusion (MCAo) model[2].
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Dosage:30 mg/kg
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Administration:p.o., at 6 h after stroke, daily, 12 weeks
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Result:Promoted robust behavioral effects at acute stage, which remained stable over chronic period.
Stroke animals displayed significant amelioration of stroke-induced motor and neurological deficits.
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Animal Model:Adult female Swiss Webster mice, adult male C57/BLKS/J and C57BLKSjBKS.Cg-Dock7m+/+ Leprdb/J (also called db/db) mice and adult male Sprague-Dawley rats. Type 1 diabetes was induced by injection of STZ (streptozotocin) (HY-13753) (90 mg/kg). Type 2 diabetes was modeled using db/db mice[3].
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Dosage:10 mg/kg (Female STZ-diabetic), 30 mg/kg (db/db mice, male control)
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Administration:p.o., daily, 16 weeks (Female STZ-diabetic), 26 weeks (db/db mice, male control)
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Result:Significantly protected long-term memory and attenuated reductions in the volume of the CA1 and DG regions in type 1 diabetic mice.
Significantly prevented or attenuated all deficits, such as paw tactile allodynia, paw heat hypoalgesia, reduced paw intraepidermal nerve fiber (IENF) density, and reduced corneal nerve density in the subbasal nerve plexus in type 1 diabetic mice.
Accelerated decline in nonfasted blood glucose of db/db mice in the terminal stages of the study.
Prevented loss of CA1 volume and increased BrdU-positive cell number in db/db mice.
Promoted a significant increase in corneal nerve density in the type2 diabetic mice.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1270138-41-4
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Appearance Solid
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분자량 464.49
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화학식 C22H33N4O5P
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Color White to off-white
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SMILES
O=C(N1CCN(CC1)CC2=CC=CC=C2)C3=CC=CN=C3NCCC(C)C.O=P(O)(O)O
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Synonyms
NSI-189 phosphate
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선적
Room temperature in continental US; may vary elsewhere.
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보관
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
In Vitro:
DMSO : 25 mg/mL (53.82 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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: ≥ 2.5 mg/mL (5.38 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 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. McIntyre RS, et al. The neurogenic compound, NSI-189 phosphate: a novel multi-domain treatment capable of pro-cognitive and antidepressant effects. Expert Opin Investig Drugs. 2017 Jun;26(6):767-770. [Content Brief]
[3]. olivalt CG, et al. Amelioration of Both Central and Peripheral Neuropathy in Mouse Models of Type 1 and Type 2 Diabetes by the Neurogenic Molecule NSI-189. Diabetes. 2019 Nov;68(11):2143-2154. [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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1529 mL | 10.7645 mL | 21.5290 mL | 53.8225 mL |
| 5 mM | 0.4306 mL | 2.1529 mL | 4.3058 mL | 10.7645 mL | |
| 10 mM | 0.2153 mL | 1.0764 mL | 2.1529 mL | 5.3822 mL | |
| 15 mM | 0.1435 mL | 0.7176 mL | 1.4353 mL | 3.5882 mL | |
| 20 mM | 0.1076 mL | 0.5382 mL | 1.0764 mL | 2.6911 mL | |
| 25 mM | 0.0861 mL | 0.4306 mL | 0.8612 mL | 2.1529 mL | |
| 30 mM | 0.0718 mL | 0.3588 mL | 0.7176 mL | 1.7941 mL | |
| 40 mM | 0.0538 mL | 0.2691 mL | 0.5382 mL | 1.3456 mL | |
| 50 mM | 0.0431 mL | 0.2153 mL | 0.4306 mL | 1.0764 mL |
Amdiglurax phosphate Related Classifications
HY-13999A1 Related Classifications
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