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| ln Vitro |
In SH-SY5Y human dopaminergic neuroblastoma cells, orexin A (human, rat, mouse) acetate (0.1, 1, 10, 100 nM; 24 h) stimulates the expression of BDNF in a dose-dependent manner[1]. Time-dependently, orexin A (human, rat, mouse) acetate (1 nM; 1, 3, 6, 12, 24 h) raises the expression of TH, PI3K, and BDNF in SH-SY5Y cells[1].
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| ln Vivo |
Orexin A (human, rat, mouse) acetate (300 ng/mouse; icv; once daily for 8 days) normalizes the striatal dopaminergic fibers, inhibits the depletion of dopamine and its metabolites in the striatum, and attenuates the loss of dopaminergic neurons and the decrease of tyrosine hydroxylase (TH) expression in the substantia nigra[1]. In both the PPQ-induced mice abdominal constriction paradigm and the carrageenan-induced heat hyperalgesia model, orexin A (human, rat, mouse) acetate (10, 30 mg/kg; iv; single) has analgesic properties[2].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: SH-SY5Y cells Tested Concentrations: 0.1, 1, 10, 100 nM Incubation Duration: 24 h Experimental Results: Increased the expression of PI3K and TH in a dose-dependent manner. Dramatically induced BDNF expression at the dose of 1 and 10 nM. Western Blot Analysis[1] Cell Types: SH-SY5Y cells Tested Concentrations: 1 nM Incubation Duration: 1, 3, 6, 12, 24 h Experimental Results: demonstrated the expression of PI3K rapidly increased by 72.6 % as soon as 3 h, which maintained at high levels in the following 24 h. Increased the protein level of BDNF and the increased rate was 44.8%, and the protein level of TH Dramatically increased at 12 h by 48.5%. |
| Animal Protocol |
Animal/Disease Models: Male C57BL/6 mice (10weeks old; 22-26 g; MPTP-Induced Mouse Model of PD)[1].
Doses: 300 ng/ mouse Route of Administration: Intracerebroventricular injection; single daily for 8 days Experimental Results: Reversed MPTP-induced motor impairments via OX1R and increased the protein expression of BDNF in nigral dopaminergic neurons. Improved MPTP-induced impairments in spatial Learning and memory and protected dopaminergic neurons against MPTP- induced neurotoxicity. Attenuated the reduction of dopaminergic neurons in the substantia nigra and restored the reduction of dopaminergic fibers in the striatum. Animal/Disease Models: Female ICR mice (17-28 g; carrageenan-induced thermal hyperalgesia model)[2]. Doses: 10 , 30 mg/kg Route of Administration: intravenous (iv) injection; single; 5 min pre-test Experimental Results: Increased paw withdrawal latency to the thermal stimulus back to baseline levels. Animal/Disease Models: Male ICR mice (17-20 g; phenyl-p-quinone ( PPQ)-induced mouse abdominal constriction model)[2]. Doses: 3, 10, 30 mg/kg A |
| References |
| Molecular Formula |
C152H243N47O44S4.XC2H4O2
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| Related CAS # |
Orexin A (human, rat, mouse);205640-90-0;Orexin A (human, rat, mouse) (TFA)
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| Appearance |
Solid powder
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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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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) |
H2O :≥ 50 mg/mL
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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.) |
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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