Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
IC50: 14 μM (GRK2)[2]; Serotonin-reuptake[4]
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ln Vitro |
Paroxetine (1 μM and 10 μM; 4 h) inhibits GRK2, which in turn distinctly inhibits T cell migration stimulated by CX3CL1[2]. Paroxetine (16 h) prevents splenic T cells' GRK2-induced ERK activation[2]. In BV2 cells treated with LPS, paroxetine (10 μM) decreases pro-inflammatory cytokines[3]. In BV2 cells, paroxetine (0-5 μM) inhibits the generation of TNF-α and IL-1β produced by LPS in a dose-dependent manner[3]. additionally prevents the generation of nitric oxide (NO) and the expression of inducible nitric oxide synthase (iNOS) in BV2 cells when lipopolysaccharide (LPS) is present[3]. In BV2, paroxetine (5 μM) reduces baseline ERK1/2 activity and inhibits LPS-induced JNK activation. It also alleviates microglia-mediated neurotoxicity and inhibits LPS-stimulated pro-inflammatory cytokines and NO in primary microglial cells[3].
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ln Vivo |
In rats with collagen-induced arthritis (CIA), paroxetine (15 mg/kg/d; po; 15 d) clearly reduces the symptoms[2].
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Animal Protocol |
Animal/Disease Models: Collagen-induced arthritis (CIA) model in rats (around 14-day-old)[2]
Doses: 15 mg/kg Route of Administration: po (oral gavage); one time/day; 15 days Experimental Results: Helped CIA rats to restore more body weight. |
References |
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-223.
[2]. Wang Q, et al. Paroxetine alleviates T lymphocyte activation and infiltration to joints of collagen-induced arthritis. Sci Rep. 2017 Mar 28;7:45364. [3]. Liu RP, et al. Paroxetine ameliorates lipopolysaccharide-induced microglia activation via differential regulation of MAPK signaling. J Neuroinflammation. 2014 Mar 12;11:47. [4]. Hwang S, et al. Inhibitory effect of the selective serotonin reuptake inhibitor paroxetine on human Kv1.3 channels. Eur J Pharmacol. 2021 Dec 5;912:174567. |
Molecular Formula |
C19H17D4CLFNO3
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Molecular Weight |
369.85
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CAS # |
1217683-35-6
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SMILES |
N1CC[C@@H](C2=C([2H])C([2H])=C(F)C([2H])=C2[2H])[C@H](COC2=CC=C3OCOC3=C2)C1.[H]Cl
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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 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 | 2.7038 mL | 13.5190 mL | 27.0380 mL | |
5 mM | 0.5408 mL | 2.7038 mL | 5.4076 mL | |
10 mM | 0.2704 mL | 1.3519 mL | 2.7038 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.