| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
NGD 94-1 (dimaleate) showed more than 600-fold higher selectivity for the D4.2 receptor than for many other targets, but its selectivity for the 5-HT1A receptor (about 50-fold lower selectivity) and the 5-HT3 receptor (about 200-fold lower selectivity) was significantly lower[2]. NGD 94-1 (dimaleate) can induce the inhibition of cAMP accumulation in HEK293/D4 cells, but does not affect Forskolin-stimulated cAMP production in untransfected HEK293 cells, indicating that its inhibitory effect is specifically mediated by the transfected dopamine D4 receptor[3].
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|---|---|
| ln Vivo |
NGD 94-1 (1-5 mg/kg, surgical injection, 45 minutes before testing) (dimaleic acid) reversed PCP to repair cognitive deficits in monkeys and increased HVA accumulation in cerebrospinal fluid in the cisterns [1].
|
| Animal Protocol |
Animal/Disease Models: Young-adult vervet (Cercopithecus aethiops sabaeus) monkeys[1]
Doses: 1 and 5 mg/kg Route of Administration: i.m., 45 min prior to testing Experimental Results: Significantly reversed the impaired successful performance of PCP-treated subjects (from 58% to 79% accuracy) at 1 mg/kg. Ameliorated the PCP-induced impairments (from 73% to 86% accuracy) at 5 mg/kg. Reduced barrier reaching and perseverative responding at both doses in PCP-treated monkeys. Unaffected response initiation latencies and motor problems in PCP-treated monkeys. Unaffected accurate performance at 1 mg/kg in saline pretreated monkeys. Slightly impaired successful performance at 5 mg/kg in saline pretreated monkeys. Failed to affect response initiation latencies or motor problems at both doses in saline pretreated monkeys. Failed to affect HVA levels relative to saline in control subjects. Significantly increased HVA concentrations in the CSF in PCP-treated subjects. |
| References |
| Molecular Formula |
C26H28N6O8
|
|---|---|
| Molecular Weight |
552.54
|
| CAS # |
179333-18-7
|
| Related CAS # |
NGD94-1
|
| Appearance |
Typically exists as solids at room temperature
|
| HS Tariff Code |
2934.99.9001
|
| 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
|
|---|---|
| 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 | 1.8098 mL | 9.0491 mL | 18.0982 mL | |
| 5 mM | 0.3620 mL | 1.8098 mL | 3.6196 mL | |
| 10 mM | 0.1810 mL | 0.9049 mL | 1.8098 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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