| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| ln Vitro |
In calcium mobilization experiments, Sunobinop (1 pM-1 μM) TFA acted as a moderately potent partial agonist of human NOP receptors and was inactive against classical opioid receptors, indicating that it was highly selective for NOP receptors [2]. In cAMP inhibition experiments, Sunobinop (10 pM-10 μM; pre-incubated for 1 hour) TFA acted as a moderately potent partial agonist of human NOP receptors, reducing cAMP levels stimulated by forsklin, with an efficacy of approximately 72% of the maximum efficacy of N/OFQ [2]. In bioimpedance experiments using HEK293 cells expressing NOP receptors, Sunobinop (10 pM-10 μM) TFA acted as a low- to moderately potent partial agonist and as a competitive antagonist when co-incubated with N/OFQ [2]. Sunobinop TFA showed human pEC50 values of 7.99, 7.62, 7.22 and 8.07 in various NOP assays[2].
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| ln Vivo |
Sunobinop (30-300 mg/kg; oral; single dose) TFA significantly reduced wakefulness and increased non-rapid eye movement sleep in WT rats by activating NOP receptors, with no adverse effects on cognition, reward, respiration or gastrointestinal function at supertherapeutic doses [1].
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| Animal Protocol |
Animal/Disease Models: Insomnia wild-type rats (WT); NOP knockout rats (NOP-KO)[1]
Doses: 30 mg/kg; 300 mg/kg Route of Administration:Oral; Single Dosage Experimental Results:At doses of 30 mg/kg and 300 mg/kg, wakefulness time was reduced and non-rapid eye movement (NREM) sleep was increased. Compared with the control group, REM sleep was not significantly different at the 300 mg/kg dose. At the 300 mg/kg dose, the significant increase in non-REM sleep observed in WT rats in NOP-KO rats almost completely disappeared. At supratherapeutic doses, no statistically significant changes in learning and memory, reward, respiration, or intestinal transit were observed in relation to treatment. |
| References |
| Molecular Formula |
C28H34F3N3O5
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|---|---|
| Molecular Weight |
549.58
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| Related CAS # |
Sunobinop
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| Appearance |
White to off-white solid
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| SMILES |
O=C1N([C@@H]2C[C@H]3N([C@]4([H])C[C@@H]5C[C@@H](CCC5)C4)[C@H](CCC3)C2)C6=CC=CC=C6N=C1C(O)=O.O=C(O)C(F)(F)F
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| Synonyms |
S 117957 TFA; IMB 115 TFA
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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 Note: 请将本产品存放在密封且受保护的环境中（例如氮气下），避免暴露在潮湿环境中。 |
| 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 | 1.8196 mL | 9.0979 mL | 18.1957 mL | |
| 5 mM | 0.3639 mL | 1.8196 mL | 3.6391 mL | |
| 10 mM | 0.1820 mL | 0.9098 mL | 1.8196 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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