1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. nAChR
  3. Cytisinicline

シチシン  (Synonyms: Cytisine; Sophorine; Baptitoxine; Cytisinicline)

製品番号: HY-N0175 純度: 99.98%
COA 取扱説明書 Technical Support

Cytisinicline (Cytisine) is an alkaloid. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs, and partial to full agonist at β4 containing receptors and α7 receptors. Has been used medically to help with smoking cessation.

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Cytisinicline

シチシン 構造式

CAS 番号 : 485-35-8

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 26 在庫あり
Solution
10 mM * 1 mL in DMSO USD 26 在庫あり
Solid
5 mg $24 在庫あり
10 mg $35 在庫あり
50 mg $70 在庫あり
100 mg $98 在庫あり
500 mg $196 在庫あり
1 g $255 在庫あり
5 g $434 在庫あり
10 g $565 在庫あり
25 g $848 在庫あり
50 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 1 publication(s) in Google Scholar

Other Forms of Cytisinicline:

Top Publications Citing Use of Products
  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

Cytisinicline (Cytisine) is an alkaloid. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs[1], and partial to full agonist at β4 containing receptors and α7 receptors[2]. Has been used medically to help with smoking cessation[3].

IC50 & Target

α4β2 nAChRs[1].

Cellular Effect
Cell Line Type Value Description References
MDCK CC50
> 80 μM
Compound: 5
Cytotoxicity against MDCK cells assessed as reduction in cell viability after 48 hrs by CellTiter-Glo assay
Cytotoxicity against MDCK cells assessed as reduction in cell viability after 48 hrs by CellTiter-Glo assay
[PMID: 25147619]
MDCK EC50
> 80 μM
Compound: 5
Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in MDCK cells assessed as inhibition of virus-induced cytocidal activity after 48 hrs by CellTiter-Glo assay
Antiviral activity against Influenza A virus (A/Puerto Rico/8/34(H1N1)) infected in MDCK cells assessed as inhibition of virus-induced cytocidal activity after 48 hrs by CellTiter-Glo assay
[PMID: 25147619]
Oocyte EC50
0.9 μM
Compound: 5
Effective concentration against Nicotinic acetylcholine receptor alpha4-beta4 expressed in xenopus oocytes
Effective concentration against Nicotinic acetylcholine receptor alpha4-beta4 expressed in xenopus oocytes
[PMID: 16033252]
Oocyte EC50
2.7 μM
Compound: 5
Effective concentration against Nicotinic acetylcholine receptor alpha4-beta2 expressed in xenopus oocytes
Effective concentration against Nicotinic acetylcholine receptor alpha4-beta2 expressed in xenopus oocytes
[PMID: 16033252]
Oocyte EC50
39 μM
Compound: 5
Effective concentration against Nicotinic acetylcholine receptor alpha2-beta4 expressed in xenopus oocytes
Effective concentration against Nicotinic acetylcholine receptor alpha2-beta4 expressed in xenopus oocytes
[PMID: 16033252]
Oocyte EC50
67 μM
Compound: 5
Effective concentration against Nicotinic acetylcholine receptor alpha3-beta2 expressed in xenopus oocytes
Effective concentration against Nicotinic acetylcholine receptor alpha3-beta2 expressed in xenopus oocytes
[PMID: 16033252]
Oocyte EC50
71 μM
Compound: 5
Effective concentration against Nicotinic acetylcholine receptor alpha 7 expressed in xenopus oocytes
Effective concentration against Nicotinic acetylcholine receptor alpha 7 expressed in xenopus oocytes
[PMID: 16033252]
Oocyte EC50
72 μM
Compound: 5
Effective concentration against Nicotinic acetylcholine receptor alpha3-beta4 expressed in xenopus oocytes
Effective concentration against Nicotinic acetylcholine receptor alpha3-beta4 expressed in xenopus oocytes
[PMID: 16033252]
PC-12 EC50
10 μM
Compound: 7
Compound was evaluated for functional potencies and efficacies at rat Nicotinic acetylcholine receptor subtype PC12 (ganglionic)
Compound was evaluated for functional potencies and efficacies at rat Nicotinic acetylcholine receptor subtype PC12 (ganglionic)
[PMID: 9435889]
TE-671 EC50
11 nM
Compound: Cytisine (1)
Change in membrane potential in TE-671 cells expressing acetylcholine neuromuscular receptors
Change in membrane potential in TE-671 cells expressing acetylcholine neuromuscular receptors
[PMID: 15686946]
体外実験

Cytisinicline (Cytisine) (2.5, 5 and 10 mM) is capable of inducing apoptosis in HepG2 cells[4].
Treatment with Cytisinicline (Cytisine) increases the percentage of cells in the sub-G1 phase (P<0.01). The preincubation of HepG2 cells with Cytisinicline (Cytisine) (2.5, 5 and 10 mM) significantly increases the sub-G1 cell population[4].

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

体内実験

Cytisinicline (Cytisine) (5 mg/kg, i.p.) eat less and gain less weight than those that receive the vehicle[2].
Total pellet intake increases during Cytisinicline (Cytisine) substitution relative to nicotine and animals self-administered Cytisine significantly less than nicotine[2].

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

臨床実験
分子量

190.25

分子式

C11H14N2O

CAS 番号
Appearance

Solid

Color

White to light yellow

SMILES

O=C1N(C[C@@]2([H])C[C@]3([H])CNC2)C3=CC=C1

Structure Classification
Initial Source
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

H2O : ≥ 100 mg/mL (525.64 mM)

DMSO : 100 mg/mL (525.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.2564 mL 26.2818 mL 52.5635 mL
5 mM 1.0513 mL 5.2564 mL 10.5127 mL
10 mM 0.5256 mL 2.6282 mL 5.2564 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* 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)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始)

C1

×
体積 (開始)

V1

=
濃度 (終了)

C2

×
体積 (終了)

V2

体内:

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: ≥ 2.08 mg/mL (10.93 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (10.93 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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).
純度とドキュメンテーション

純度: 99.98%

参考文献

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 5.2564 mL 26.2818 mL 52.5635 mL 131.4088 mL
5 mM 1.0513 mL 5.2564 mL 10.5127 mL 26.2818 mL
10 mM 0.5256 mL 2.6282 mL 5.2564 mL 13.1409 mL
15 mM 0.3504 mL 1.7521 mL 3.5042 mL 8.7606 mL
20 mM 0.2628 mL 1.3141 mL 2.6282 mL 6.5704 mL
25 mM 0.2103 mL 1.0513 mL 2.1025 mL 5.2564 mL
30 mM 0.1752 mL 0.8761 mL 1.7521 mL 4.3803 mL
40 mM 0.1314 mL 0.6570 mL 1.3141 mL 3.2852 mL
50 mM 0.1051 mL 0.5256 mL 1.0513 mL 2.6282 mL
60 mM 0.0876 mL 0.4380 mL 0.8761 mL 2.1901 mL
80 mM 0.0657 mL 0.3285 mL 0.6570 mL 1.6426 mL
100 mM 0.0526 mL 0.2628 mL 0.5256 mL 1.3141 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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  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
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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製品名:
Cytisinicline
製品番号:
HY-N0175
数量:
MCE 日本正規代理店: