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5mg |
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10mg |
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50mg |
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Other Sizes |
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Cevimeline HCl (AF-102B; SNK-508; FKS-508; SNI-2011; trade name Evoxac), the hydrochloride salt of Cevimeline, is a potent parasympathomimetic and
muscarinic agonist used for the treatment of
dry mouth and Sjögren's
syndrome, as well as Xerostomia symptoms.
ln Vitro |
Cevimeline (0.1-100 μM) raises the intracellular Ca2+ content in parotid gland cells that have been digested [1].
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ln Vivo |
Male Wistar rats administered with cevimeline (0.008-0.016 mg/kg intraperitoneally) exhibited increased pressor response, increased salivation, and a gradual and sustained rise in parotid gland blood flow. In the subfornical organ, cevimeline, at 0.016 mg/kg, reduces angiotensin II-induced water intake and neuronal activity [1].
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Animal Protocol |
Animal/Disease Models: Male Wistar rats (8 weeks old) were injected with angiotensin-II[1].
Doses: 0.008 mg/kg, 0.016 mg/kg. Route of Administration: intraperitoneal (ip) injection. Experimental Results: Salivation increased slowly and persistently, and blood flow increased. Increased in parotid and pressor responses. |
References |
[1]. Witsell DL, et al. Effectiveness of cevimeline to improve oral health in patients with postradiation xerostomia.Head Neck. 2012 Aug;34(8):1136-42. doi: 10.1002/hed.21894. Epub 2012 Jan 9.
[2]. Kondo Y, et al.Cevimeline-induced monophasic salivation from the mouse submandibular gland: decreased Na+ content in saliva results from specific and early activation of Na+/H+ exchange.J Pharmacol Exp Ther. 2011 Apr;337(1):267-74. Epub 2011 Jan 14. [3]. Ono K, et al. Distinct effects of cevimeline and pilocarpine on salivary mechanisms, cardiovascular response and thirst sensation in rats.Arch Oral Biol. 2012 Apr;57(4):421-8. Epub 2011 Nov 17. [4]. Voskoboynik B, et al.Cevimeline (Evoxac) overdose.J Med Toxicol. 2011 Mar;7(1):57-9. [5]. Mitoh Y, et al. Effects of cevimeline on excitability of parasympathetic preganglionic neurons in the superior salivatory nucleus of rats. Auton Neurosci. 2017 Sep;206:1-7. |
Molecular Formula |
C10H18CLOS
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Molecular Weight |
235.77
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CAS # |
107220-28-0
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Related CAS # |
Cevimeline hydrochloride hemihydrate;153504-70-2;(+)-Cevimeline hydrochloride hemihydrate;Cevimeline;107233-08-9
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
C[C@@H](SC1)O[C@@]21CN3CCC2CC3.[H]Cl
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InChi Key |
SURWTGAXEIEOGY-GHXDPTCOSA-N
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InChi Code |
InChI=1S/C10H17NOS.ClH/c1-8-12-10(7-13-8)6-11-4-2-9(10)3-5-11/h8-9H,2-7H2,1H31H/t8-,10-/m1./s1
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Chemical Name |
Spiro(1-azabicyclo(2.2.2)octane-3,5'-(1,3)oxathiolane), 2'-methyl-, hydrochloride, cis-
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Synonyms |
SNK 508FKS-508 SNI-2011FKS508 SNI 2011AF-102B AF
102BSNK-508AF102B SNI2011 SNK508 AF-102B, Cevimeline, FKS 508,
HSDB 7286, SNI 2011
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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, avoid exposure to moisture. |
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) |
H2O : ≥ 50 mg/mL (~212.07 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 | 4.2414 mL | 21.2071 mL | 42.4142 mL | |
5 mM | 0.8483 mL | 4.2414 mL | 8.4828 mL | |
10 mM | 0.4241 mL | 2.1207 mL | 4.2414 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.