Facinicline hydrochloride (Synonyms: RG3487 hydrochloride)

Name: Facinicline hydrochloride
Brand: MedChemExpress
SKU: HY-108057A
Rating: 4.5 (1 reviews)

Cat. No.: HY-108057A Purity: 99.93%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Facinicline hydrochloride (RG3487 hydrochloride) is an orally active nicotinic α7 receptor partial agonist, with a K_i of 6 nM for α7 human nAChR. Facinicline hydrochloride (RG3487 hydrochloride) improves cognition and sensorimotor gating in rodents. Facinicline hydrochloride (RG3487 hydrochloride) shows high affinity (antagonist) to 5-HT₃Rs with a K_i value of 1.2 nM.

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

Facinicline hydrochloride Chemical Structure

CAS No. : 677305-02-1

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 264	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 264	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 240	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 385	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 635	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 880	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1230	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

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

Customer Review

Based on 1 publication(s) in Google Scholar

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All 5-HT Receptor Isoform Specific Products:

View All Isoforms

5-HT₁ Receptor 5-HT₂ Receptor 5-HT₃ Receptor 5-HT₄ Receptor 5-HT₅ Receptor 5-HT₆ Receptor 5-HT₇ Receptor 5-HT Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

5-HT₃ Receptor

1.2 nM (Ki)

α7

6 nM (Ki)

In Vitro

Facinicline (RG3487) activates human α7 nAChRs with an EC₅₀ of 0.8 μM (oocytes) and 7.7 μM (QM7 cells)^[1].
Facinicline (RG3487) exhibits antagonist properties at the serotonin 3 receptor (IC₅₀ 2.8 nM (oocytes), 32.7 nM (N1E-115 cells))^[1].

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

In Vivo

Facinicline (RG3487) improves object recognition memory in rats after acute [minimally effective dose (MED) 1.0 mg/kg p.o.] or repeated (10 day) administration at brain and plasma concentrations in the low-nanomolar range^[1].
RG3487 (0.1–10 mg/kg p.o.) selectively enhances object recognition memory^[1].

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

Animal Model:	Male Sprague-Dawley rats^[1].
Dosage:	0.1-10 mg/kg (Pharmacokinetic Analysis).
Administration:	Orally.
Result:	The mean C_max was typically observed between 0.5 and 4 h.

Molecular Weight

306.79

Formula

C₁₅H₁₉ClN₄O

CAS No.

677305-02-1

Appearance

Solid

Color

White to off-white

SMILES

[H]Cl.O=C(C1=NNC2=C1C=CC=C2)N[C@@H]3CN4CCC3CC4

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 : 125 mg/mL (407.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 100 mg/mL (325.96 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.2596 mL	16.2978 mL	32.5956 mL
5 mM	0.6519 mL	3.2596 mL	6.5191 mL
10 mM	0.3260 mL	1.6298 mL	3.2596 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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: ≥ 6.25 mg/mL (20.37 mM); Clear solution

This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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: ≥ 6.25 mg/mL (20.37 mM); Clear solution

This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 6.25 mg/mL (20.37 mM); Clear solution

This protocol yields a clear solution of ≥ 6.25 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 (62.5 mg/mL) to 900 μL Corn oil, and mix evenly.

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 (325.96 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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: 99.93%

Select Batch:

Data Sheet (277 KB) SDS (252 KB)

COA (252 KB) HNMR (216 KB) LCMS (142 KB)

Handling Instructions (2659 KB)

References

[1]. Tanya L Wallace, et al. RG3487, a Novel Nicotinic α7 Receptor Partial Agonist, Improves Cognition and Sensorimotor Gating in Rodents. J Pharmacol Exp Ther. 2011 Jan;336(1):242-53. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	3.2596 mL	16.2978 mL	32.5956 mL	81.4890 mL
	5 mM	0.6519 mL	3.2596 mL	6.5191 mL	16.2978 mL
	10 mM	0.3260 mL	1.6298 mL	3.2596 mL	8.1489 mL
	15 mM	0.2173 mL	1.0865 mL	2.1730 mL	5.4326 mL
	20 mM	0.1630 mL	0.8149 mL	1.6298 mL	4.0744 mL
	25 mM	0.1304 mL	0.6519 mL	1.3038 mL	3.2596 mL
	30 mM	0.1087 mL	0.5433 mL	1.0865 mL	2.7163 mL
	40 mM	0.0815 mL	0.4074 mL	0.8149 mL	2.0372 mL
	50 mM	0.0652 mL	0.3260 mL	0.6519 mL	1.6298 mL
	60 mM	0.0543 mL	0.2716 mL	0.5433 mL	1.3581 mL
	80 mM	0.0407 mL	0.2037 mL	0.4074 mL	1.0186 mL
	100 mM	0.0326 mL	0.1630 mL	0.3260 mL	0.8149 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.

Facinicline hydrochloride 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.

Keywords:

Facinicline677305-02-1RG3487RG 3487RG-3487nAChR5-HT ReceptorNicotinic acetylcholine receptorsSerotonin Receptor5-hydroxytryptamine Receptornicotinicα7receptorserotonin 3 receptorrecognitionmemoryInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks

Product Name			Lot #
Applicant Name *			Email Address *
Phone Number			Department *
Organization Name *			Country or Region *
Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

Facinicline hydrochloride (Synonyms: RG3487 hydrochloride)

Customer Review

Facinicline hydrochloride Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All 5-HT Receptor Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Facinicline hydrochloride Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Facinicline hydrochloride Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

Request for HNMR Report