Size | Price | Stock | Qty |
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5mg |
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10mg |
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Other Sizes |
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Targets |
κ Opioid Receptor/KOR
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ln Vivo |
In Wistar Kyoto rats, DIPPA (2.5 and 5 mg/kg; sc) hydrochloride reduces the latency to feed; however, therapy had no effect on approach latencies in SD rats[2]. The high dose of DIPPA (1 and 5 mg/kg; sc) hydrochloride causes an increase in immobility in SD rats as compared to the group of rats treated with saline[2]. Compared to the 5 mg/kg group of Wistar Kyoto rats, SD rats consume less DIPPA (5 mg/kg) hydrochloride. In both strains, DIPPA hydrochloride dramatically reduces burying time. Burying is reduced in both strains by DIPPA hydrochloride (5 mg/kg) as compared to the within-strain control groups. In SD rats, DIPPA hydrochloride tends to reduce consumption in the home cage but dramatically boosts feeding in the novel cage, where possible anxiolytic-like effects of the substance may counteract its hypophagic effects[2].
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Animal Protocol |
Animal/Disease Models: Wistar Kyoto rats and SD rats (250–300 g)[2]
Doses: 2.5 and 5 mg/kg Route of Administration: Sc Experimental Results: diminished the latency to feed in Wistar Kyoto rats, but treatment did not alter approach latencies in SD rats. Animal/Disease Models: Wistar Kyoto rats and SD rats (250–300 g)[2] Doses: 1 and 5 mg/kg Route of Administration: Sc Experimental Results: High dose increased immobility in SD rats compared to the saline-treated strain control group. |
References |
[1]. Jones DC, et al. Identification of a κ-opioid agonist as a potent and selective lead for drug development against human African trypanosomiasis. Biochem Pharmacol. 2010;80(10):1478-1486.
[2]. Carr GV, et al. Comparison of the kappa-opioid receptor antagonist DIPPA in tests of anxiety-like behavior between Wistar Kyoto and Sprague Dawley rats. Psychopharmacology (Berl). 2010;210(2):295-302. [3]. Costello GF, et al. 2-(3,4-Dichlorophenyl)-N-methyl-N-[2-(1-pyrrolidinyl)-1-substituted- ethyl]-acetamides: the use of conformational analysis in the development of a novel series of potent opioid kappa agonists. J Med Chem. 1991;34(1):181-189. [4]. Chang AC, et al. kappa Opioid receptor selective affinity labels: electrophilic benzeneacetamides as kappa-selective opioid antagonists. J Med Chem. 1994;37(26):4490-4498. |
Molecular Formula |
C22H24CL3N3OS
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Molecular Weight |
484.87
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CAS # |
155512-52-0
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
Cl.S=C=NC1C=CC=C([C@H](N(C(CC2=CC=C(Cl)C(Cl)=C2)=O)C)CN2CCCC2)C=1
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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)
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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.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.0624 mL | 10.3120 mL | 20.6241 mL | |
5 mM | 0.4125 mL | 2.0624 mL | 4.1248 mL | |
10 mM | 0.2062 mL | 1.0312 mL | 2.0624 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.