Orexin A (human, rat, mouse) (acetate) (Hypocretin-1 (human, rat, mouse) (acetate))

Cat No.:V76678 Purity: ≥98%
Orexin A (Hypocretin-1) (human, rat, mouse) acetate is a hypothalamic neuropeptide with analgesic properties (crosses the BBB (blood-brain barrier)).
Orexin A (human, rat, mouse) (acetate) (Hypocretin-1 (human, rat, mouse) (acetate)) Chemical Structure Product category: OX Receptor
This product is for research use only, not for human use. We do not sell to patients.
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Other Forms of Orexin A (human, rat, mouse) (acetate) (Hypocretin-1 (human, rat, mouse) (acetate)):

  • Orexin A human, rat, mouse
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Product Description
Orexin A (Hypocretin-1) (human, rat, mouse) acetate is a hypothalamic neuropeptide with analgesic properties (crosses the BBB (blood-brain barrier)). Orexin A (human, rat, mouse) acetate is also an OX1R agonist and can induce the expression of BDNF and TH proteins in SH-SY5Y cells in a time- and dose-dependent manner. Orexin A (human, rat, mouse) acetate may be used in studies of appetite regulation, neurodegenerative diseases, and modulation of nociceptive messaging.
Biological Activity I Assay Protocols (From Reference)
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].
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].
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
[1]. Liu MF, et al. Orexin-A Exerts Neuroprotective Effects via OX1R in Parkinson's Disease. Front Neurosci. 2018 Nov 15;12:835.
[2]. Bingham S, et al. Orexin-A, an hypothalamic peptide with analgesic properties. Pain. 2001 May;92(1-2):81-90.
[3]. Rodgers RJ, et al. Orexins and appetite regulation. Neuropeptides. 2002 Oct;36(5):303-25.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C152H243N47O44S4.XC2H4O2
Related CAS #
Orexin A (human, rat, mouse);205640-90-0;Orexin A (human, rat, mouse) (TFA)
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)
Solubility Data
Solubility (In Vitro)
H2O :≥ 50 mg/mL
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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 : PEG300Tween 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).
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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)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
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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.
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