Cotinine
Based on 3 publication(s) in Google Scholar
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.
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- Purity: 99.98%
- CAS No.: 486-56-6
- 화학식: C10H12N2O
- 분자량:176.22
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보관:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Cotinine
MoreAll Endogenous Metabolite Isoforms
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Biological Activity
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.
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Cell Line:Human primary pterygium cells
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Concentration:2 μM (Cotinine) + 0.15 μM (Nicotine)
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Incubation Time:7 days
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Result:Exhibited a significant reduction in MTT signal by 16.04% at day 7.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mongrel male dogs (weighting 10.0 kg, pentobarbital anesthesia (30 mg/kg))
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Dosage:25, 50, 100, 200, 500 mg/kg
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Administration:Intravenous injection (i.v.)
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Result:Caused a transient fall in blood pressure (in 10 ml of saline, at a rate of 0.5 ml/second).
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Animal Model:Male Swiss-Webster strain albino mice (14 to 23 g)
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Dosage:0.01 mL/g
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Administration:ntraperitoneal administration (i.v.), oral gavage(p.o.)
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Result:Had an LD50 of 930 mg/kg for intraperitoneal administration and 1604 mg/kg for oral gavage.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 486-56-6
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Appearance <40°C Solid,>42°C Liquid
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분자량 176.22
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화학식 C10H12N2O
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Color White to light brown
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SMILES
O=C1N(C)[C@H](C2=CC=CN=C2)CC1
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Synonyms
(-)-Cotinine; (S)-Cotinine; NIH-10498
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Structure Classification
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Initial Source
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (3)
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Journal Impact Factor
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Most Recent
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (283 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Dolcini MM, et al. An assessment of the validity of adolescent self-reported smoking using three biological indicators. Nicotine Tob Res. 2003 Aug;5(4):473-83. [Content Brief]
[2]. Sastry BV, et al. Distribution and retention of nicotine and its metabolite, cotinine, in the rat as a function of time. Pharmacology. 1995 Feb;50(2):128-36. [Content Brief]
[3]. Borzelleca J F, et al. Studies on the respiratory and cardiovascular effects of (-)-cotinine[J]. Journal of Pharmacology and Experimental Therapeutics, 1962, 137(3): 313-318. [Content Brief]
[4]. Yang Q, et al. Continuous exposure of nicotine and cotinine retards human primary pterygium cell proliferation and migration. [Content Brief]
[5]. Dwoskin L P, et al. (S)-(−)-Cotinine, the major brain metabolite of nicotine, stimulates nicotinic receptors to evoke [3H] dopamine release from rat striatal slices in a calcium-dependent manner[J]. Journal of pharmacology and experimental therapeutics, 1999, 288(3): 905-911. [Content Brief]
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 | 5.6748 mL | 28.3738 mL | 56.7476 mL | 141.8689 mL |
| 5 mM | 1.1350 mL | 5.6748 mL | 11.3495 mL | 28.3738 mL | |
| 10 mM | 0.5675 mL | 2.8374 mL | 5.6748 mL | 14.1869 mL | |
| 15 mM | 0.3783 mL | 1.8916 mL | 3.7832 mL | 9.4579 mL | |
| 20 mM | 0.2837 mL | 1.4187 mL | 2.8374 mL | 7.0934 mL | |
| 25 mM | 0.2270 mL | 1.1350 mL | 2.2699 mL | 5.6748 mL | |
| 30 mM | 0.1892 mL | 0.9458 mL | 1.8916 mL | 4.7290 mL | |
| 40 mM | 0.1419 mL | 0.7093 mL | 1.4187 mL | 3.5467 mL | |
| 50 mM | 0.1135 mL | 0.5675 mL | 1.1350 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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