| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Human Endogenous Metabolite Caspase-3 κ Opioid Receptor/KOR
|
|---|---|
| ln Vitro |
In mouse striatal neurons, dynorphin A TFA (10 μM, 4 h/72 h) increases the amount of cytochrome c released from mitochondria and caspase-3 activity, which results in neuronal death[3]. Neurons are significantly lost and [Ca2+]i is elevated at 33 μM for 4 hours when dynorphin A TFA is administered[4]. The release of vasopressin (VP) from the isolated neural lobe is inhibited by dynorphin A TFA (1 μM)[5].
|
| ln Vivo |
Male rats denied of water for 24 hours and are given 1 μg or 2 μL of dynorphin A TFA intracerebroventricular injection as a single dose, which decreases the release of vasopressin (VP)[5]. Intracerebroventricular injection of dynorphin A TFA (500 pmol/5 μL daily for 4 days) reduces behavioral deficits in ddY mice caused by stress, together with brain modulation of the 5-HTergic system[6].
|
| Cell Assay |
Cell Viability Assay[3]
Cell Types: Mouse Striatal neurons Tested Concentrations: 10 μM Incubation Duration: 0, 24, 48, 72 h Experimental Results: Induced neuronal death (identified by the fragmentation and destruction of the cell body and neurites). |
| Animal Protocol |
Animal/Disease Models: 24 h water-deprived male rats[5]
Doses: 1 μg of 2 μL Route of Administration: Intracerebroventricular injection Experimental Results: Inhibited vasopressin (VP) release 30 min upon injection. Animal/Disease Models: Male ddY mice[6] Doses: 15, 150, 1500 pmol/5 μL per day for 4 days Route of Administration: Intracerebroventricular injection Experimental Results: Attenuated the repeated stress -induced escape failures from the shock. |
| References |
|
| Molecular Formula |
C101H156F3N31O25
|
|---|---|
| Molecular Weight |
2261.50
|
| Related CAS # |
Dynorphin A;80448-90-4
|
| Appearance |
Typically exists as solid at room temperature
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 0.4422 mL | 2.2109 mL | 4.4218 mL | |
| 5 mM | 0.0884 mL | 0.4422 mL | 0.8844 mL | |
| 10 mM | 0.0442 mL | 0.2211 mL | 0.4422 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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