| Company Name: |
Dalian Meilun Biotech Co., Ltd.
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| Tel: |
0411-62910999 13889544652 |
| Email: |
sales@meilune.com |
| Products Intro: |
Product Name:RG3487 hydrochloride
CAS:677305-02-1
Purity:＞99%,BR Package:10mg/RMB 1670;25mg/RMB 2750;50mg/RMB 3810 Remarks:MC17707
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| | S-Facinicline Basic information |
| Product Name: | S-Facinicline | | Synonyms: | S-Facinicline;Facinicline hydrochloride;RG3487;RG3487 hydrochloride;Inhibitor,nAChR,serotonin 3 receptor,Nicotinic acetylcholine receptors,Serotonin Receptor,5-HT Receptor,inhibit,recognition,5-hydroxytryptamine Receptor,Facinicline,Facinicline hydrochloride,receptor,RG-3487,memory,RG 3487,nicotinic;Facinicline hydrochloride, 10 mM in DMSO | | CAS: | 677305-02-1 | | MF: | C15H19ClN4O | | MW: | 306.79056 | | EINECS: | | | Product Categories: | | | Mol File: | 677305-02-1.mol |  |
| | S-Facinicline Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO: 125 mg/mL (407.44 mM); Methanol: 25 mg/mL (81.49 mM) | | form | Solid | | color | White to off-white |
| | S-Facinicline Usage And Synthesis |
| Uses | 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]. | | Biological Activity | Facinicline hydrochloride (RG3487 hydrochloride) is an orally active partial agonist of the nicotinic α7 receptor with a Ki of 6 nM for human nAChR. It (RG3487 hydrochloride) improves cognition and sensorimotor gating in rodents. Facinicline hydrochloride has a Ki value of 1.2 nM for the 5-HT3 receptor (antagonist). | | in vitro | Facinicline (RG3487) activates human α7 nAChRs with an EC 50 of 0.8 μM (oocytes) and 7.7 μM (QM7 cells).
It (RG3487) exhibits antagonist properties at the serotonin 3 receptor (IC 50 2.8 nM (oocytes), 32.7 nM (N1E-115 cells)).
< /p> | | in vivo | Facinicline (RG3487) improves object recognition memory in rats after acute [minimally effective dose (MED) 1.0 mg/kg po] or repeated (10 day) administration at brain and plasma concentrations in the low-nanomolar range.
RG3487 (0.1–10 mg/kg po) selectively enhances object recognition memory.
| Animal Model: | Male Sprague-Dawley rats. | | Dosage: | 0.1-10 mg/kg (Pharmacokinetic Analysis ). | | Administration: | Orally. | < td class="col1 fwb"> Result: | The mean C max was typically observed between 0.5 and 4 h. | | | target | | 5-HT 3 Receptor 1.2 nM (Ki) | α7 < span> 6 nM (Ki) | | | IC 50 | 5-HT3 Receptor: 1.2 nM (Ki); α7: 6 nM (Ki) | | 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. DOI:10.1124/jpet.110.171892 |
| | S-Facinicline Preparation Products And Raw materials |
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