Art. -Nr.: HY-N0175

Cytisinicline

(Synonyms: Cytisine; Sophorine; Baptitoxine)

1 Cited Publications

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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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Reinheit: 99.98%
CAS. Nr.: 485-35-8
Formel: C₁₁H₁₄N₂O
Molecular Weight:190.25

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Cytisinicline Chemical Structure

CAS. Nr.: 485-35-8

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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]

In Vitro

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.

In Vivo

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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 485-35-8
Appearance Solid
Molecular Weight 190.25
Formel C₁₁H₁₄N₂O
Color White to light yellow
SMILES

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

Cytisine; Sophorine; Baptitoxine
Structure Classification
- Alkaloids
- Pyridine Alkaloids
Initial Source
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Journal Impact Factor

J Ethnopharmacol

Isoxanthohumol, a component of Sophora flavescens, promotes the activation of the NLRP3 inflammasome and induces idiosyncratic hepatotoxicity. [Abstract]

2022 Mar 1:285:114796. PMID: 34740771

Lösungsmittel & Löslichkeit

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 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) .

Reinheit & Dokumentation

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Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (420 KB)
- English - EN (420 KB)
- Français - FR (420 KB)
- Deutsch - DE (420 KB)
- Norwegian - NO (420 KB)
- Español - ES (420 KB)
- Swedish - SV (420 KB)
- Italian - IT (420 KB)
- Korean - KR (420 KB)
- Portuguese - PT (420 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Pabreza LA, et al. [3H]cytisine binding to nicotinic cholinergic receptors in brain. Mol Pharmacol. 1991 Jan;39(1):9-12. [Content Brief]

[2]. Grebenstein PE, et al. The effects of noncontingent and self-administered cytisine on body weight and meal patterns in male Sprague-Dawley rats. Pharmacol Biochem Behav. 2013 Sep;110:192-200. [Content Brief]

[3]. Walker N, et al. Cytisine versus nicotine for smoking cessation. N Engl J Med. 2014 Dec 18;371(25):2353-62. [Content Brief]

[4]. Yu L, et al. Cytisine induces endoplasmic reticulum stress caused by calcium overload in HepG2 cells. Oncol Rep. 2018 Mar;39(3):1475-1484. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Keywords

Cytisinicline

1 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) Cytisinicline

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Cytisinicline Related Classifications

HY-N0175 Related Classifications