>>Signaling Pathways>> Neuroscience>> mAChR>>(+)-Cevimeline hydrochloride hemihydrate

(+)-Cevimeline hydrochloride hemihydrate (Synonyms: (-)-SNI-2011; (-)-AF102B hydrochloride hemihydrate)

Catalog No.GC34957

(+)-Cevimeline hydrochloride hemihydrate ((+)-SNI-2011), 강력한 무스카린 수용체 작용제는 쇼그렌 증후군의 구강건조증에 대한 후보 치료제입니다.

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(+)-Cevimeline hydrochloride hemihydrate Chemical Structure

Cas No.: 153504-70-2

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

Cevimeline hydrochloride hemihydrate, a novel muscarinic receptor agonist, is a candidate therapeutic drug for xerostomia in Sjogren's syndrome. IC50 value:Target: mAChRThe general pharmacol. properties of this drug on the gastrointestinal, urinary, and reproductive systems and other tissues were investigated in mice, rats, guinea pigs, rabbits, and dogs. The in vitro metab. of SNI-2011 was also evaluated with rat and dog liver microsomes. After oral administration, plasma concns. of SNI-2011 reached to Cmax within 1 h in both species, suggesting that SNI-2011 was quickly absorbed, and then decreased with a t1/2 of 0.4-1.1 h. The bioavailability was 50% and 30% in rats and dogs, resp. Major metabolites in plasma were both S- and N-oxidized metabolites in rats and only N-oxidized metabolite in dogs, indicating that a large species difference was obsd. in the metab. of SNI-2011. Sex difference was also obsd. in the pharmacokinetics of SNI-2011 in rats, but not in dogs. In the in vitro study, chem. inhibition and pH-dependent studies revealed that the sulfoxidn. and N-oxidn. of SNI-2011 were mediated by cytochrome P 450 (CYP) and flavin-contg. monooxygenase (FMO), resp., in both species. In addn., CYP2D and CYP3A were mainly responsible for the sulfoxidn. in rat liver microsomes.

Chemical Properties

Cas No. 153504-70-2 SDF
Synonyms (-)-SNI-2011; (-)-AF102B hydrochloride hemihydrate
Canonical SMILES C[C@H](SC1)O[C@]21CN3CCC2CC3.Cl.[0.5H2O]
Formula C10H17NOS.HCl.1/2H2O M.Wt 244.78
Solubility 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

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1 mg 5 mg 10 mg
1 mM 4.0853 mL 20.4265 mL 40.853 mL
5 mM 0.8171 mL 4.0853 mL 8.1706 mL
10 mM 0.4085 mL 2.0427 mL 4.0853 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 29 reference(s) in Google Scholar.)

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