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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Varenicline dihydrochloride is a nicotinic receptor partial agonist. Varenicline dihydrochloride is a partial agonist on the α4β2, α3β4, and α6β2 subtypes. Varenicline dihydrochloride displays full agonism on α7 nicotinic acetylcholine receptors.
ln Vitro |
RAW 264.7 macrophages' LPS-induced cytokine secretion (IL-1β, IL-6, and TNFα) and cell proliferation rate are inhibited by vannicline diHClide (1 μM, 24 h) [1]. Human adrenal chromaffin cells separated from male and female organ donors exhibit action potentials (Aps) stimulation in the absence of ACh stimulation when exposed to 250 nM vannicline diHClide [3]. By lowering VE-cadherin protein expression, vannicline diHClide (100 μM, 4 h) stimulates HUVEC migration [4].
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ln Vivo |
Nicotine conditioned place preference (CPP) is inhibited by vannicline disalk (0.01-1 mg/kg subcutaneously, 3 days), when administered 10 minutes prior to nicotine (0.5 mg/kg subcutaneously) [5]. Position aversion caused by vannicline diHClide (subcutaneous injection, 2.5 mg/kg, 3 days) is dependent on α5 nAChR but not β2 nAChR [5]. Subcutaneous injection of vannicline diHClide (0.1 and 0.5 mg/kg, 3 days) reverses the somatic symptoms and hyperalgesia associated with nicotine withdrawal, as well as withdrawal-induced aversion, in a dose-related manner [5].
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Cell Assay |
Cell proliferation assay [1]
Cell Types: RAW 264.7 mouse macrophages (treated with 4 μg/mL LPS for 24 h) Tested Concentrations: 1 μM Incubation Duration: 0-48 h Experimental Results: LPS-induced cell proliferation rate diminished. Western Blot Analysis[4] Cell Types: HUVEC Tested Concentrations: 1, 10, 100 μM Incubation Duration: 24 hrs (hours) or 30 minutes Experimental Results: diminished VE-cadherin protein expression, activation of ERK1/2, p38 and JNK signaling. |
Animal Protocol |
Animal/Disease Models: ICR male mice [5]
Doses: 0.01-1 mg/kg, 3 days Route of Administration: subcutaneous injection Experimental Results: Inhibited nicotine conditioned place preference (CPP) in a dose-dependent manner. |
References |
[1]. Elif Baris, et al. Varenicline Prevents LPS-Induced Inflammatory Response via Nicotinic Acetylcholine Receptors in RAW 264.7 Macrophages. Front Mol Biosci. 2021 Oct 12;8:721533.
[2]. Mihalak KB, et al. Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors.Mol Pharmacol. 2006 Sep;70(3):801-5. Epub 2006 Jun 9. [3]. Jin H, et al. Therapeutic concentrations of varenicline in the presence of nicotine increase action potential firing in human adrenal chromaffin cells. J Neurochem. 2017 Jan;140(1):37-52. [4]. Mitsuhisa Koga, et al. Varenicline promotes endothelial cell migration by lowering vascular endothelial-cadherin levels via the activated α7 nicotinic acetylcholine receptor-mitogen activated protein kinase axis. Toxicology. 2017 Sep 1;390:1-9. [5]. Bagdas D, et al. New insights on the effects of varenicline on nicotine reward, withdrawal and hyperalgesia in mice.Neuropharmacology. 2018 Aug;138:72-79. |
Molecular Formula |
C13H15CL2N3
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Molecular Weight |
284.1843
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Exact Mass |
283.06
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Elemental Analysis |
C, 54.94; H, 5.32; Cl, 24.95; N, 14.79
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CAS # |
866823-63-4
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Related CAS # |
Varenicline;249296-44-4;Varenicline-d4 hydrochloride;Varenicline-d4 dihydrochloride
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Appearance |
Solid powder
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SMILES |
Cl[H].Cl[H].N1([H])C([H])([H])C2([H])C3=C([H])C4C(C([H])=C3C([H])(C1([H])[H])C2([H])[H])=NC([H])=C([H])N=4
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Synonyms |
Varenicline dihydrochloride; HSDB7591; HSDB-7591; HSDB 7591; CP 526555; CP-526555; CP526555;
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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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
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) |
DMSO : ~62.5 mg/mL (~219.93 mM)
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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 | 3.5189 mL | 17.5945 mL | 35.1890 mL | |
5 mM | 0.7038 mL | 3.5189 mL | 7.0378 mL | |
10 mM | 0.3519 mL | 1.7594 mL | 3.5189 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.