| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
MOR modulator-1 exhibits a sub-nanomolar binding affinity for MOR, a single-digit nanomolar binding affinity for KOR (κ opioid receptor), and a much lower binding affinity for DOR (δ opioid receptor), maintaining good selectivity for MOR relative to DOR [1]. MOR modulator-1 shows the highest δ/μ selectivity, approximately three times that of NAT [1]. MOR modulator-1 is linked to carboxylamide linkers μ, δ, and γ, with Ki values of 0.25, 41.1, and 1.30 nM, respectively [1]. The EC50 value of MOR modulator-1 binding to MOR[35S]GTPγS is 2.16 nM [1]. The EC50 values of MOR modulator-1 binding to KOR[35S]GTPγS and DOR[35S]GTPγS are 3.83 nM and 23.6 nM, respectively [1]. MOR regulator-1 has a potency in the nanomolar to sub-nanomolar range, but its potency is low, with a %Emax value of 11.3 [1]. MOR regulator-1 significantly antagonizes the increase in intracellular calcium ion concentration induced by DAMGO in Gαqi5-transfected mMORCHO cells [1]. The IC50 value of MOR regulator-1 for inhibiting the increase in intracellular calcium ion concentration in Gαqi5-transfected mMORCHO cells is 5.64 nM [1].
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| ln Vivo |
MOR modulator-1 (10 mg/kg, warm water tail dip, 20 min), containing a 2'-thiazole group, is the most potent member of the NAT analogue family for antagonizing morphine-mediated analgesia[1]. MOR modulator-1 (10 mg/kg, warm water tail dip, 20 min) has an AD50 of 0.043 mg/kg, which is 10 times more potent than NAT[1]. MOR modulator-1 (10 mg/kg, warm water tail dip, 20 min) is the most active epoximane molecule among all MOR modulators[1]. At all tested doses, MOR modulator-1 (0.05–10 mg/kg, subcutaneous injection, 20 min) induced fewer wet dog tremors and paw tremors than 1 mg/kg naloxone (NLX), even at the highest doses of 5 mg/kg and 10 mg/kg[1]. The mean counts of shaking, jumping and paw tremors induced by MOR modulator-1 (5 mg/kg, subcutaneous injection, 20 minutes) in wet dogs were 9.8, 36.8 and 30.2, respectively [1]. At 5, 10 and 30 minutes after administration, the concentrations of MOR modulator-1 in brain tissue were 0.187, 0.235 and 0.264 μg/g, respectively, indicating that MOR modulator-1 can rapidly enter brain tissue and remain in the brain for a long time after subcutaneous injection [1].
|
| References |
| Molecular Formula |
C24H27N3O4S
|
|---|---|
| Molecular Weight |
453.55
|
| CAS # |
2976336-81-7
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O[C@]12[C@@]34C5=C(C[C@@]2([H])N(CC4)CC6CC6)C=CC(O)=C5O[C@@]3([H])[C@H](CC1)NC(C7=NC=CS7)=O
|
| 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 | 2.2048 mL | 11.0241 mL | 22.0483 mL | |
| 5 mM | 0.4410 mL | 2.2048 mL | 4.4097 mL | |
| 10 mM | 0.2205 mL | 1.1024 mL | 2.2048 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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