| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg | ||
| Other Sizes |
| Targets |
pKi: 8.65 (NOP receptor); 6.60 (μ-opioid receptor); 6.14 (κ-opioid receptor); < 5 (δ-opioid receptor)[1]
|
|---|---|
| ln Vitro |
In the range of 3-300 nM, trap-101 hydrochloride (3, 30, and 300 nM) causes a concentration-dependent rightward shift of the concentration-response curve to N/OFQ without changing the peak response to the agonist. Up to 10 μM, trap-101 hydrochloride is inert per se. Trap101's receptor binding affinities (pKi values) at traditional opioid receptors expressed in CHO cell membranes, recombinant human NOP receptors, and μ-, κ-, and δ-opioid receptors are 6.14, 8.65, 6.60, and less than five, respectively[1].
|
| ln Vivo |
In addition to causing a delayed increase in immobility time in the bar test at 30 mg/kg, trap-101 hydrochloride (10–30 mg/kg; identified after 90 min) alters motor activity in naïve rats. It also increases stepping activity and rotarod performance at 10 mg/kg and decreases both at 30 mg/kg[1]. 6-OHDA lesioning results in decreased motor function overall and motor asymmetry that mostly affects the contralateral paw. In hemiparkinsonian rats, intraperitoneal injection of Trap-101 hydrochloride (10–30 mg/kg; 90 min detection) ameliorates akinesia/bradykinesia and enhances gait overall; it is efficacious at 1 mg/kg and does not increase motor deficit at 30 mg/kg[1].
|
| Animal Protocol |
Animal/Disease Models: 6-OHDA hemilesioned rats[1]
Doses: 10-30 mg/kg Route of Administration: intraperitoneal (ip) injection; 10-30 mg/kg; detected after 90 min Experimental Results: Attenuated parkinsonian-like motor deficits in rat. |
| References |
[1]. Matteo Marti, et al. The novel nociceptin/orphanin FQ receptor antagonist Trap-101 alleviates experimental parkinsonism through inhibition of the nigro-thalamic pathway: positive interaction with L-DOPA. J Neurochem. 2008 Dec;107(6):1683-96.
|
| Molecular Formula |
C24H36CLN3O2
|
|---|---|
| Molecular Weight |
434.01
|
| CAS # |
1216621-00-9
|
| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
| SMILES |
CCN1C2=CC=CC=C2N(C3=C(CN(CC3)CC4CCCCCCC4)CO)C1=O.Cl
|
| 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 | 2.3041 mL | 11.5205 mL | 23.0409 mL | |
| 5 mM | 0.4608 mL | 2.3041 mL | 4.6082 mL | |
| 10 mM | 0.2304 mL | 1.1520 mL | 2.3041 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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