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Purity: = 98.28%
Orexin A human, rat, mouse is a novel and potent peptide consisting of 33 amino acids, acting as a highly specific and high-affinity agonist for OX1/2R (Ki of 20 and 38 nM for OX1 and OX2 receptors respectively), which is a G-protein-coupled receptor. It is an endogenous agonist of OX1 and OX2 receptors by nature.
| Targets |
OX1 Receptor
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|---|---|
| ln Vitro |
Orexin A (human, rat, mouse) exhibits a high affinity for OX1R, with 38 nM IC50 and 34 nM EC50 values in the the [Ca2﹢]i transient assay[1].
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| ln Vivo |
Orexin A (human, rat, and mouse) (3–30 mg/kg; i.v.; 5-min pre-test) dramatically lengthens the time to response at 10 and 30 mg/kg i.v. when administered to vehicle-treated mice, increasing it from 24.8±2.0 s to 35.0±3.7 s and 45.7±4.5 s, respectively[2].
Orexin A (human, rat, mouse) (3, 10 and 30 mg/kg; i.v.) was administered right before phenylp-quinone (PPQ), and in mice treated with vehicle, it increased the latency to the first PPQ-induced constriction from 357.4±35.2 s to 500.3±31.2 s at 10 mg/kg and 594.5±5.5 s at 30 mg/kg[2].
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| Animal Protocol |
Female mice (mouse carrageenan-induced thermal hyperalgesia test)
3, 10 and 30 mg/kg i.v.; 5 min pre-test |
| References |
| Molecular Formula |
C₁₅₂H₂₄₃N₄₇O₄₄S₄
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|---|---|
| Molecular Weight |
3561.10
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| CAS # |
205640-90-0
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| Related CAS # |
Orexin A (human, rat, mouse) (TFA); Orexin A (human, rat, mouse) (acetate)
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| Appearance |
Powder
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| SMILES |
[XPLPDCCRQKTCSCRLYELLHGAGNHAAGILTL cyclic (6-12),(7-14)-bis(disulfide)]
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| Synonyms |
Hypocretin-1 (human, rat, mouse); Orexin A (human, rat, mouse)
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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: Please store this product in a sealed and protected environment, 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 (~14.0 mM)
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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 | 0.2808 mL | 1.4041 mL | 2.8081 mL | |
| 5 mM | 0.0562 mL | 0.2808 mL | 0.5616 mL | |
| 10 mM | 0.0281 mL | 0.1404 mL | 0.2808 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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