| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
KOR agonist 6 (Compound 5i) exhibits super-high binding affinity for κ-opioid receptors (KOR (Ki = 0.00025 nM)) and excellent subtype selectivity for μ-opioid receptors (MOR (Ki = 14.1 nM)) and δ-opioid receptors (DOR (Ki = 120.7 nM)) [1]. KOR agonist 6 showed agonist activity against MOR (EC50 = 44.78 nM, Emax = 88.71%) and DOR (EC50 = 15.26 nM, Emax = 85.16%) in CHO cells and inhibited Forskolin-stimulated cAMP accumulation (EC50 = 200.3 nM, Emax = 99.51%) [1]. KOR agonist 6 exhibits potent activity in stimulating KOR-mediated [35S]GTPγS binding in KOR-expressing cell membranes (EC50 = 0.024 nM, Emax = 106.9%), strongly inhibits cAMP accumulation in KOR-expressing HEK293 cells (EC50 = 0.43 pM, Emax = 63.63%), and induces β-arrestin protein recruitment with low potency in HTLA cells transfected with KOR-Tango plasmid (EC50 = 0.143 nM, Emax = 42.89%) [1].
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|---|---|
| ln Vivo |
KOR agonist 6 (compound 5i) (0.4–8.0 mg/kg, intraperitoneal injection, followed by 6 hours monitoring) produced the desired analgesic effect in the simulated hot plate test (ED50 = 0.6 mg/kg)[1]. KOR agonist 6 (0.08–8.0 mg/kg, intraperitoneal injection, followed by 6 hours monitoring) showed the desired analgesic activity in the simulated hot plate test (ED50 = 0.6 mg/kg)[1]. 1.5 mg/kg)[1]. KOR agonist 6 (0.8–8.0 mg/kg, intraperitoneal injection, conditioned for 6 consecutive days, followed by a 15-minute free exploration test on day 8) did not show significant conditioned positional originality in container CD1[1]. KOR agonist 6 (0.8–8.0 mg/kg, intraperitoneal injection, followed by 6 hours monitoring) did not induce a significant reduction in spontaneous movement activity (total distance traveled) in the Kunming protocol[1].
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| Animal Protocol |
Animal/Disease Models: Female Kunming mice (18-22 g) were used, with the nociceptive response (latency to licking back paws) assessed on a 55 °C heated smooth surface; mice with no response within 30 s before administration were excluded, and a 60 s cutoff time was set to prevent tissue damage[1]
Doses: 0.4, 0.8, 1.2, 1.6, 8.0 mg/kg Route of Administration: i.p., detected at 6 h post-administration Experimental Results: Showed dose-dependent antinociceptive efficacy in mice hot plate test (ED50 = 0.6 mg/kg). Animal/Disease Models: Male Kunming mice (18-22 g)[1] Doses: 0.08, 0.8, 3.2, 6.4, 8.0 mg/kg Route of Administration: i.p., detected at 6 h post-administration followed by 0.6% acetic acid injection Experimental Results: Showed dose-dependent antinociceptive activity in mice abdominal constriction test(ED50 = 1.5 mg/kg). |
| References |
| Molecular Formula |
C35H40N4O4
|
|---|---|
| Molecular Weight |
580.72
|
| Appearance |
Typically exists as solids at room temperature
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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)
|
| 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 | 1.7220 mL | 8.6100 mL | 17.2200 mL | |
| 5 mM | 0.3444 mL | 1.7220 mL | 3.4440 mL | |
| 10 mM | 0.1722 mL | 0.8610 mL | 1.7220 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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