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250mg | ||
500mg |
ln Vitro |
The proteolytic amino acid precursor orexin, which is encoded by a gene found on human chromosome 17q21, is the source of orexin B. Orexin B has been shown to have a greater affinity for the OX2 receptor in radioligand binding tests [1]. In comparison to the rodent sequence, human orexin B contains two amino acid changes. With an EC50 of 60 nM in the [Ca2+]i transient experiment and an IC50 of 36 nM in the binding assay, the OX2 receptor does, in fact, have a high affinity for human orexin B. Human Orexin B exhibits a notably reduced affinity for human OX1; in the competitive binding experiment, its calculated IC50 was 420 nM, whereas in the [Ca2+]i transient assay, its EC50 was 2500 nM [2].
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ln Vivo |
Human orexin-B dramatically enhances food intake; at the 2-hour mark, 3 nM and 30 nM of orexin-B, respectively, were shown to stimulate food consumption five- and twelve-fold, respectively [2].
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References |
[1]. Smart D, et al. Orexins: a new family of neuropeptides. Br J Anaesth. 1999 Nov;83(5):695-7.
[2]. Sakurai T, et al. Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior. Cell. 1998 Feb 20;92(4):573-85 |
Molecular Formula |
C123H212N44O35S
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Molecular Weight |
2899.33817999999
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CAS # |
205640-91-1
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Related CAS # |
Orexin B, human TFA
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
[H]/N=C(/NCCC[C@@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(NCC(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(NCC(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(=O)N)CCSC)=O)[C@H](O)C)=O)CC(C)C)=O)[C@H](CC)C)=O)=O)C)=O)C)=O)CC1N=CNC=1)=O)CC(=O)N)=O)=O)CO)=O)C)=O)CCC(=O)N)=O)CC(C)C)=O)CC(C)C)=O)CCCN/C(=N/[H])/N)=O)CCC(=O)N)=O)CC(C)C)=O)NC(CNC([C@@H](NC([C@@H](NC(CNC([C@H]1N(C([C@H]2N(C(CNC([C@@H](NC([C@H](CCCN/C(=N/[H])/N)N)=O)CO)=O)=O)CCC2)=O)CCC1)=O)=O)CC(C)C)=O)CCC(=O)N)=O)=O)\N
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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 |
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) |
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
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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 | 0.3449 mL | 1.7245 mL | 3.4491 mL | |
5 mM | 0.0690 mL | 0.3449 mL | 0.6898 mL | |
10 mM | 0.0345 mL | 0.1725 mL | 0.3449 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.