1. GPCR/G Protein Neuronal Signaling
  2. mAChR
  3. Cevimeline hydrochloride hemihydrate

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

Cat. No.: HY-76772 Purity: 99.52%
COA Handling Instructions

Cevimeline hydrochloride hemihydrate (SNI-2011) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride hemihydrate stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline hydrochloride hemihydrate can cross the blood-brain barrier (BBB).

For research use only. We do not sell to patients.

Cevimeline hydrochloride hemihydrate Chemical Structure

Cevimeline hydrochloride hemihydrate Chemical Structure

CAS No. : 153504-70-2

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10 mM * 1 mL in DMSO
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Other Forms of Cevimeline hydrochloride hemihydrate:

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  • Biological Activity

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Description

Cevimeline hydrochloride hemihydrate (SNI-2011) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride hemihydrate stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia[1][2][3][4]. Cevimeline hydrochloride hemihydrate can cross the blood-brain barrier (BBB)[5].

IC50 & Target

mAChR1

 

mAChR3

 

In Vitro

In digested parotid cells, Cevimeline (0.1-100 μM) increases the intracellular Ca2+ concentration[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Cevimeline (0.008-0.016 mg/kg; intraperitoneal injection; male Wistar rats) treatment shows slowly increasing and lasting salivation, and increased blood flow increment in the parotid gland and pressor response. Cevimeline inhibits angiotensin II-induced water intake and neuronal activity in the subfornical organ at 0.016 mg/kg[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Wistar rats (8-week-old) injected with angiotensin-II[1]
Dosage: 0.008 mg/kg, 0.016 mg/kg
Administration: Intraperitoneal injection
Result: Showed slowly increasing and lasting salivation, and increased blood flow increment in the parotid gland and pressor response.
Clinical Trial
Molecular Weight

244.78

Formula

C10H17NOS.HCl.1/2H2O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@H]1SC[C@@]2(CN3CCC2CC3)O1.[H]Cl.[H]O[H]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (408.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : ≥ 50 mg/mL (204.27 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0853 mL 20.4265 mL 40.8530 mL
5 mM 0.8171 mL 4.0853 mL 8.1706 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (10.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (10.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (408.53 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.52%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 4.0853 mL 20.4265 mL 40.8530 mL 102.1325 mL
5 mM 0.8171 mL 4.0853 mL 8.1706 mL 20.4265 mL
10 mM 0.4085 mL 2.0427 mL 4.0853 mL 10.2133 mL
15 mM 0.2724 mL 1.3618 mL 2.7235 mL 6.8088 mL
20 mM 0.2043 mL 1.0213 mL 2.0427 mL 5.1066 mL
25 mM 0.1634 mL 0.8171 mL 1.6341 mL 4.0853 mL
30 mM 0.1362 mL 0.6809 mL 1.3618 mL 3.4044 mL
40 mM 0.1021 mL 0.5107 mL 1.0213 mL 2.5533 mL
50 mM 0.0817 mL 0.4085 mL 0.8171 mL 2.0427 mL
60 mM 0.0681 mL 0.3404 mL 0.6809 mL 1.7022 mL
80 mM 0.0511 mL 0.2553 mL 0.5107 mL 1.2767 mL
100 mM 0.0409 mL 0.2043 mL 0.4085 mL 1.0213 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Cevimeline hydrochloride hemihydrate Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Cevimeline hydrochloride hemihydrate
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