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.

Product information

CAS Number: 677305-02-1

Molecular Weight: 306.79

Formula: C15H19ClN4O

Chemical Name: N-[(3S)-1-azabicyclo[2.2.2]octan-3-yl]-1H-indazole-3-carboxamide hydrochloride

Smiles: Cl.O=C(N[C@@H]1CN2CCC1CC2)C1=NNC2=CC=CC=C21

InChiKey: CMRLNEYJEPELSM-BTQNPOSSSA-N

InChi: InChI=1S/C15H18N4O.ClH/c20-15(14-11-3-1-2-4-12(11)17-18-14)16-13-9-19-7-5-10(13)6-8-19;/h1-4,10,13H,5-9H2,(H,16,20)(H,17,18);1H/t13-;/m1./s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 125 mg/mL (407.44 mM; Need ultrasonic). H2O : 100 mg/mL (325.96 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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

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. RG3487 (0.1–10 mg/kg p.o.) selectively enhances object recognition memory.

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