| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| Other Sizes |
|
| Targets |
NMDA receptor[1]; CYP450 2B[2]; Cholinesterase (ChE)[3]
|
|---|---|
| ln Vitro |
Orphenadrine (30-300 μM) exhibits relatively fast concentration-dependent open channel blockade kinetics with a Koff of 0.013[1].
|
| ln Vivo |
In a study of the tumor-promoting effects of orphenadrine, male rats were pretreated with a single intraperitoneal injection of N-diethylnitrosamine (DEN) for 2 weeks. Orphenadrine (0, 750, 1500 ppm; po; 6 wk) accelerated hepatocyte proliferation and induced liver tumor-promoting activity[2]. Orphenadrine (30 mg/kg; po; 3 d) protected rats from the effects of 3-nitropropionic acid (3-NPA) (30 mg/kg; 3 d), which resulted in increased expression of neuronal damage markers [(3)H]-PK 11195 and HSP27 in astrocytes[3].
|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: NMDA open-channel Tested Tested Concentrations: 30, 100 and 300 μM Incubation Duration: 5 seconds; with 200 μM NMDA Experimental Results: Nearly completely inhibited [3H]MK-801 binding at 100 μM. Exhibited relatively fast, Tested Tested Concentrations-dependent open channel blocking kinetics. |
| Animal Protocol |
Animal/Disease Models: Liver tumor model in male rats pre-treated by N-diethylnitrosamine[2]
Doses: 0, 750, 1500 ppm Route of Administration: PO; for 6 weeks Experimental Results: Increased mRNA expression levels of Cyp2b1/2, Mrp2 and Cyclin D1. Increased microsomal reactive oxygen species (ROS) production and oxidative stress markers such as thiobarbituric acid-reactive substances and 8-hydroxydeoxyguanosine. |
| References |
|
| Molecular Formula |
C18H23NO
|
|---|---|
| Molecular Weight |
269.38
|
| CAS # |
83-98-7
|
| Related CAS # |
Orphenadrine citrate;4682-36-4;Orphenadrine hydrochloride
|
| Appearance |
Light yellow to brown <25°C solid powder,>25°C liquid
|
| SMILES |
CC1=CC=CC=C1C(C2=CC=CC=C2)OCCN(C)C
|
| Synonyms |
(±)-Orphenadrine
|
| 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) |
DMSO : ~100 mg/mL (~371.22 mM; with ultrasonication)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.28 mM)(saturation unknown) in 10% DMSO 40% PEG300 5% Tween-80 45% Saline (add these co-solvents sequentially from left to right, and one by one),clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution and add it to 400 μL PEG300, mix well; then add 50 μL Tween-80 to the above system, mix well; then continue to add 450 μL of normal saline to make up to 1 mL. Preparation of normal saline: Dissolve 0.9 g of sodium chloride in ddH₂O and make up to 100 mL to obtain a clear and transparent normal saline solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.28 mM)(saturation unknown) in 10% DMSO 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one),clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution and add it to 900 μL of 20% SBE-β-CD saline solution and mix well. 2 g SBE-β-CD (sulfobutyl ether β-cyclodextrin) powder is diluted to 10 mL of saline and completely dissolved until clear and transparent. Solubility in Formulation 3: ≥ 2.5 mg/mL (9.28 mM)(saturation unknown) in 10% DMSO 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one),clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution and add it to 900 μL corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7122 mL | 18.5611 mL | 37.1223 mL | |
| 5 mM | 0.7424 mL | 3.7122 mL | 7.4245 mL | |
| 10 mM | 0.3712 mL | 1.8561 mL | 3.7122 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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