| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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Cevimeline hydrochloride hemihydrate (SNK-508; FKS-508; AF-102B; SNI-2011; trade name Evoxac), the hydrochloride salt and hemihydrated form of Cevimeline, is a parasympathomimetic and
muscarinic receptor agonist that was approved 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].
|
|---|---|
| ln Vivo |
The administration of cevimeline (0.008-0.016 mg/kg; i.p.; Arsenal Wistar Blood Pressure) resulted in a gradual rise and persistence of dead fluid, along with a rise in adrenal blood flow and an elevation in pressure response. At 0.016 mg/kg, cevimeline reduces vascular tone.
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| Animal Protocol |
Animal/Disease Models: Male Wistar rats (8 weeks old) injected with angiotensin-II[1]
Doses: 0.008mg/kg, 0.016mg/Angiotensin-II-induced water in the subfornical organ recognition and neuronal activity[1]. kg Mode of Route of Administration: intraperitoneal (ip) injection Experimental Results: Slow and sustained increase in salivation, increased parotid gland blood flow and increased pressor response. |
| References | |
| Additional Infomation |
Cevimeline Hydrochloride is a cholinergic analogue with glandular secretion stimulatory activity. Cevimeline binds to and activates muscarinic receptors, thereby increasing the secretions in exocrine salivary and sweat glands. This cholinergic agonist also increases the tone of smooth muscle in the gastrointestinal and urinary tracts. Cevimeline is being studied as a treatment for dry mouth caused by radiation therapy to the head and neck.
See also: Cevimeline Hydrochloride (annotation moved to). |
| Molecular Formula |
2(C10H17NOS).2(HCL).H2O
|
|---|---|
| Molecular Weight |
489.56
|
| Exact Mass |
488.17
|
| CAS # |
153504-70-2
|
| Related CAS # |
Cevimeline hydrochloride;107220-28-0;(+)-Cevimeline hydrochloride hemihydrate;(-)-Cevimeline hydrochloride hemihydrate;Cevimeline;107233-08-9
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| PubChem CID |
73416227
|
| Appearance |
White to off-white solid powder
|
| Density |
1.19g/cm3
|
| Boiling Point |
308.5ºC at 760mmHg
|
| Flash Point |
140.4ºC
|
| Vapour Pressure |
0.000676mmHg at 25°C
|
| LogP |
4.535
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
0
|
| Heavy Atom Count |
29
|
| Complexity |
215
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
C[C@H]1O[C@@]2(CN3CCC2CC3)CS1.C[C@H]1O[C@@]2(CN3CCC2CC3)CS1.O.Cl.Cl
|
| InChi Key |
ZSTLCHCDLIUXJE-ZGBAEQJLSA-N
|
| InChi Code |
InChI=1S/2C10H17NOS.2ClH.H2O/c2*1-8-12-10(7-13-8)6-11-4-2-9(10)3-5-11;;;/h2*8-9H,2-7H2,1H3;2*1H;1H2/t2*8-,10-;;;/m00.../s1
|
| Chemical Name |
(2S,5S)-2-methylspiro[1,3-oxathiolane-5,3'-1-azabicyclo[2.2.2]octane];hydrate;dihydrochloride
|
| Synonyms |
AF-102B AF 102BSNK-508AF102B SNI2011 SNK508 AF-102B,SNK 508FKS-508 SNI-2011FKS508 SNI 2011 Cevimeline, FKS 508,
HSDB 7286, SNI 2011
|
| 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 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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~408.53 mM)
H2O : ≥ 50 mg/mL (~204.27 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.21 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (10.21 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 to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (408.53 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0427 mL | 10.2133 mL | 20.4265 mL | |
| 5 mM | 0.4085 mL | 2.0427 mL | 4.0853 mL | |
| 10 mM | 0.2043 mL | 1.0213 mL | 2.0427 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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