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Cevimeline

カタログ番号GC14215

ムスカリン受容体作動薬

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Cevimeline 化学構造

Cas No.: 107233-08-9

サイズ 価格 在庫数 個数
5mg
$73.00
在庫あり
10mM (in 1mL DMSO)
$81.00
在庫あり
10mg
$137.00
在庫あり
50mg
$539.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Description of Cevimeline

Cevimeline is a muscarinic receptor agonist especially on the M1 and M3 receptors. [1]

Cevimeline has been approved for use against symptoms of dry mouth by activating the M3 receptors of the parasympathetic nervous system. Cevimeline is effective and safe in improving symptoms of dry eye with 20 mg three times per day [2]. Cevimeline increased the intracellular Ca+ level in parotid gland acinar cells over 1 μM and rat, enhanced the excitability via muscarinic receptors, thereby, cevimeline alleviates dry mouth symptoms by stimulating secretion by the salivary glands. Cevimeline has a longer duration of salivation[3]. Cevimeline plays a part in Alzheimer’s disease. Cevimeline decreased Aβ (1–40) level in the cerebrospinal fluid (CSF) at 1 mg/kg without changing α-APPs in rabbit and significantly decreased CSF Aβ in AD patients.[4]

References:
1. F. B. Vivino, I. Al-Hashimi, Z. Khan, F. G. LeVeque, P. L. Salisbury, 3rd, T. K. Tran-Johnson, C. C. Muscoplat, M. Trivedi, B. Goldlust and S. C. Gallagher, Arch Intern Med 1999, 159, 174-181.
2. M. Ono, E. Takamura, K. Shinozaki, T. Tsumura, T. Hamano, Y. Yagi and K. Tsubota, Am J Ophthalmol 2004, 138, 6-17.
3. K. Ono, T. Inagaki, T. Iida, R. Hosokawa and K. Inenaga, J Med Invest 2009, 56 Suppl, 375.
4. A. Fisher, Z. Pittel, R. Haring, N. Bar-Ner, M. Kliger-Spatz, N. Natan, I. Egozi, H. Sonego, I. Marcovitch and R. Brandeis, J Mol Neurosci 2003, 20, 349-356.

Chemical Properties of Cevimeline

Cas No. 107233-08-9 SDF
Chemical Name (2R,5R)-2-methylspiro[1,3-oxathiolane-5,3'-1-azabicyclo[2.2.2]octane]
Canonical SMILES CC1OC2(CN3CCC2CC3)CS1
Formula C10H17NOS M.Wt 199.32
溶解度 Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Cevimeline

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 5.0171 mL 25.0853 mL 50.1706 mL
5 mM 1.0034 mL 5.0171 mL 10.0341 mL
10 mM 0.5017 mL 2.5085 mL 5.0171 mL
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計算

In vivo Formulation Calculator (Clear solution) of Cevimeline

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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