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  4. Cotinine

Cotinine  (Synonyms: (-)-Cotinine; (S)-Cotinine; NIH-10498)

Cat. No.: HY-B1178 Purity: 98.46%
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Cotinine ((-)-Cotinine) is an orally active alkaloid found in tobacco and is the primary metabolite of nicotine. Cotinine is metabolized by CYP2A13 into trans-3'-hydroxycotinine. Cotinine is used as a biomarker to measure exposure to tobacco smoke components. Cotinine has vasodepressor activity. The mixture of cotinine and nicotine (Nicotine) has antiproliferative activity against pterygium. (S)-(-)-Cotinine activates nicotinic acetylcholine receptors (nAChR) in a calcium-dependent manner, leading to the release of dopamine (Dopamine, HY-B0451). Cotinine ((-)-Cotinine) is used in research related to cardiovascular and inflammatory diseases.

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

Cotinine Chemical Structure

Cotinine Chemical Structure

CAS No. : 486-56-6

Size Price Stock Quantity
Solid or liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 34 In-stock
Solution
10 mM * 1 mL in DMSO USD 34 In-stock
Solid or liquid
25 mg USD 30 In-stock
50 mg USD 46 In-stock
100 mg USD 70 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

Other Forms of Cotinine:

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1 Publications Citing Use of MCE Cotinine

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Cotinine ((-)-Cotinine) is an orally active alkaloid found in tobacco and is the primary metabolite of nicotine. Cotinine is metabolized by CYP2A13 into trans-3'-hydroxycotinine. Cotinine is used as a biomarker to measure exposure to tobacco smoke components. Cotinine has vasodepressor activity. The mixture of cotinine and nicotine (Nicotine) has antiproliferative activity against pterygium. (S)-(-)-Cotinine activates nicotinic acetylcholine receptors (nAChR) in a calcium-dependent manner, leading to the release of dopamine (Dopamine, HY-B0451). Cotinine ((-)-Cotinine) is used in research related to cardiovascular and inflammatory diseases[1][2][3][4][5].

IC50 & Target

Human Endogenous Metabolite

 

In Vitro

Mixture of Cotinine and Nicotine (2 μM Cotinine + 0.15 μM Nicotine, 7 days) retards the proliferation rate of human primary pterygium cells[4].
(S)-(-)-Cotinine (1–100 μM) was inhibited by the nicotinic receptor antagonists Mecamylamine (HY-B1395A) and Dihydro-β-erythroidine (HY-N10497) in the inhibition of dopamine release from rat striatal slices[5].
(S)-(-)-Cotinine (10–1000 μM) was inhibited in the release of dopamine from rat striatal slices by treatment with a low calcium buffer[5].

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

Cell Proliferation Assay[5]

Cell Line: Human primary pterygium cells
Concentration: 2 μM (Cotinine) + 0.15 μM (Nicotine)
Incubation Time: 7 days
Result: Exhibited a significant reduction in MTT signal by 16.04% at day 7.
In Vivo

Cotinine (1 mg/kg (Nicotine), i.v., sampled at 5-60 min after administration) has a long biological half-life (19-24 hours) in Sprague-Dawley rats and is retained and accumulated in plasma for an extended period[2].

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

Animal Model: Mongrel male dogs (weighting 10.0 kg, pentobarbital anesthesia (30mg/kg))
Dosage: 25, 50, 100, 200, 500 mg/kg
Administration: Intravenous injection (i.v.)
Result: Caused a transient fall in blood pressure (in 10 ml of saline, at a rate of 0.5 ml/second).
Animal Model: Male Swiss-Webster strain albino mice (14 to 23 g)
Dosage: 0.01 mL/g
Administration: ntraperitoneal administration (i.v.), oral gavage(p.o.)
Result: Had an LD50 of 930 mg/kg for intraperitoneal administration and 1604 mg/kg for oral gavage.
Clinical Trial
Molecular Weight

176.22

Formula

C10H12N2O

CAS No.
Appearance

<40°C Solid,>42°C Liquid

Color

White to light brown

SMILES

O=C1N(C)[C@H](C2=CC=CN=C2)CC1

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

Ethanol : 120 mg/mL (680.97 mM; Need ultrasonic)

DMSO : 65 mg/mL (368.86 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.6747 mL 28.3736 mL 56.7472 mL
5 mM 1.1349 mL 5.6747 mL 11.3494 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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: ≥ 2.17 mg/mL (12.31 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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: ≥ 2.17 mg/mL (12.31 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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.
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.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.42%

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 (protect from light). 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
DMSO / Ethanol 1 mM 5.6747 mL 28.3736 mL 56.7472 mL 141.8681 mL
5 mM 1.1349 mL 5.6747 mL 11.3494 mL 28.3736 mL
10 mM 0.5675 mL 2.8374 mL 5.6747 mL 14.1868 mL
15 mM 0.3783 mL 1.8916 mL 3.7831 mL 9.4579 mL
20 mM 0.2837 mL 1.4187 mL 2.8374 mL 7.0934 mL
25 mM 0.2270 mL 1.1349 mL 2.2699 mL 5.6747 mL
30 mM 0.1892 mL 0.9458 mL 1.8916 mL 4.7289 mL
40 mM 0.1419 mL 0.7093 mL 1.4187 mL 3.5467 mL
50 mM 0.1135 mL 0.5675 mL 1.1349 mL 2.8374 mL
60 mM 0.0946 mL 0.4729 mL 0.9458 mL 2.3645 mL
80 mM 0.0709 mL 0.3547 mL 0.7093 mL 1.7734 mL
100 mM 0.0567 mL 0.2837 mL 0.5675 mL 1.4187 mL
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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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