1. Membrane Transporter/Ion Channel
    Neuronal Signaling
    GPCR/G Protein
  2. nAChR
    5-HT Receptor
  3. Facinicline hydrochloride

Facinicline hydrochloride (Synonyms: RG3487 hydrochloride)

Cat. No.: HY-108057A Purity: 99.93%
Handling Instructions

Facinicline hydrochloride (RG3487 hydrochloride) is an orally active nicotinic α7 receptor partial agonist, with a Ki 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 Ki value of 1.2 nM.

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

Facinicline hydrochloride Chemical Structure

Facinicline hydrochloride Chemical Structure

CAS No. : 677305-02-1

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 330 In-stock
Estimated Time of Arrival: December 31
5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 500 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1400 In-stock
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100 mg USD 2200 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Facinicline hydrochloride (RG3487 hydrochloride) is an orally active nicotinic α7 receptor partial agonist, with a Ki 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 Ki value of 1.2 nM[1].

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].

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].

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

306.79

Formula

C₁₅H₁₉ClN₄O

CAS No.

677305-02-1

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (407.44 mM; Need ultrasonic)

Methanol : 25 mg/mL (81.49 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Keywords:

FaciniclineRG3487RG 3487RG-3487nAChR5-HT ReceptorNicotinic acetylcholine receptorsSerotonin Receptor5-hydroxytryptamine Receptornicotinicα7receptorserotonin 3 receptorrecognitionmemoryInhibitorinhibitorinhibit

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Product Name:
Facinicline hydrochloride
Cat. No.:
HY-108057A
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