| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
GluN2B-NMDAR allosteric modulator 1 (compound 175) (0.001-100 μM) enhances glutamate-induced GluN1/GluN2B-NMDAR-gated currents in HEK293 cells with an EC50 of 43.7 nM (logEC50 = -7.36) [1]. GluN2B-NMDAR allosteric modulator 1 (0.0001-1 μM) selectively enhances aspartate-induced GluN2B-containing native NMDAR currents in primary rat hippocampal neurons in a dose-dependent manner with an EC50 of 18 nM [1]. GluN2B-NMDAR allosteric modulator 1 (1 μM; 3 h) does not induce cytotoxicity in primary cortical neurons [1].
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| ln Vivo |
GluN2B-NMDAR allosteric modulator 1 (compound 175) (1 mg/kg; intraperitoneal injection; 30 minutes before synaptic plasticity induction) promotes long-term inhibition induced by low-frequency stimulation in anesthetized rats via a GluN2B subunit-dependent NMDAR mechanism [1]. GluN2B-NMDAR allosteric modulator 1 (1 mg/kg; intraperitoneal injection; single dose) reverses anxiety-like behavior and social cognitive deficits in 7-month-old Mecp2-OE mice and transgenic mice carrying Disc1-N-inducible expression [1].
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| Animal Protocol |
Animal/Disease Models:Mecp2-OE mice (7 months old); a transgenic mouse strain capable of inducing Disc1-N expression (C57BL/6; 3-4 months old) [1]
Doses: 1 mg/kg Route of Administration: Intraperitoneal injection; single administration (30 minutes before each behavioral test) Experimental Results: Mecp2-OE mice recovered to wild-type levels in open field tests (reversing anxiety-like behavior) and showed a significant increase in social preference index. Disc1-N mice showed increased central dwell time in open field tests (reversing anxiety-like behavior), increased spontaneous alternation behavior in Y-maze tests (improving spatial working memory), and increased social preference index in three-chamber maze tests (reversing social deficits). |
| References |
| Molecular Formula |
C17H21N5
|
|---|---|
| Molecular Weight |
295.38
|
| CAS # |
2419700-58-4
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
CC(N1C=CN=C1CNCC2=CC=C(N3C=CN=C3)C=C2)C
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3855 mL | 16.9273 mL | 33.8547 mL | |
| 5 mM | 0.6771 mL | 3.3855 mL | 6.7709 mL | |
| 10 mM | 0.3385 mL | 1.6927 mL | 3.3855 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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