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250mg |
Purity: ≥98%
DORA-22 is a novel, potent and selective dual orexin receptor antagonist that may be useful for insomnia and AD-relevant symptoms. It can lower histamine levels in the lateral hypothalamus and prefrontal cortex without lowering hippocampal acetylcholine. DORA-22 suppresses the release of the wake neurotransmitter histamine in the lateral hypothalamus, prefrontal cortex, and hippocampus with no significant alterations in acetylcholine levels. Compared with the GABAA modulator eszopiclone, DORA-22 elicits a neurotransmitter profile consistent with wake reduction that does not impinge on neurotransmitter levels associated with cognition and rapid eye movement sleep. DORAs may improve sleep in AD patients. Further investigations should optimize the dose and duration of DORA-22 treatment and explore additional AD-relevant animal models and cognitive tests.
References |
Alzheimers Dement (N Y).2019 Feb 28;5:70-80;J Neurochem.2017 Jul;142(2):204-214.
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Molecular Formula |
C23H22F2N4O2
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Molecular Weight |
424.45
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CAS # |
1088991-95-0
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SMILES |
N/A
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Chemical Name |
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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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 | 2.3560 mL | 11.7800 mL | 23.5599 mL | |
5 mM | 0.4712 mL | 2.3560 mL | 4.7120 mL | |
10 mM | 0.2356 mL | 1.1780 mL | 2.3560 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.
Comparison of sleep percent before and after chronic treatment withDORA-22(100mg/kg per day for 5weeks).Alzheimers Dement (N Y).2019 Feb 28;5:70-80. th> |
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Effects of sex and chronicDORA-22treatment (100mg/kg per day for 5weeks) on sleep percent in WT and 5XFAD mice. Effect of chronicDORA-22treatment (100mg/kg per day for 5weeks) on amyloid β plaques in 5XFAD mice.Alzheimers Dement (N Y).2019 Feb 28;5:70-80. td> |
Cortical gene expression of neuroinflammatory markers in 5XFAD mice treated withDORA-22(100mg/kg per day for 5weeks).Gene expression analysis was conducted using custom TaqMan Microfluidic Arrays on RNA isolated from neocortical tissue. The inflammatory markers chosen were selected to represent five discrete classes of neuroinflammatory responses based on the presumed function of the markers. The categories included (A) complement system, (B) cytokines, (C) chemokines, (D) reactive microglia markers, and (E) reactive astrocyte markers.Alzheimers Dement (N Y).2019 Feb 28;5:70-80. td> |