Description
PRX-07034 hydrochloride is a highly selective and potent 5-HT6 receptor antagonist with a Ki= 4-8 nM and an IC50 of 19 nM. PRX-07034 can be used for the research of enhancing working memory and cognitive flexibility.
Product information
CAS Number: 903580-39-2
Molecular Weight: 490.44
Formula: C21H29Cl2N3O4S
Chemical Name: N-[1-(5-chloro-2,3-dimethoxyphenyl)ethyl]-2-methanesulfonyl-5-(piperazin-1-yl)aniline hydrochloride
Smiles: Cl.CC(NC1=CC(=CC=C1S(C)(=O)=O)N1CCNCC1)C1=CC(Cl)=CC(OC)=C1OC
InChiKey: PILCQJJJAFRKHO-UHFFFAOYSA-N
InChi: InChI=1S/C21H28ClN3O4S.ClH/c1-14(17-11-15(22)12-19(28-2)21(17)29-3)24-18-13-16(25-9-7-23-8-10-25)5-6-20(18)30(4,26)27;/h5-6,11-14,23-24H,7-10H2,1-4H3;1H
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 31.25 mg/mL (63.72 mM; ultrasonic and warming and heat to 60°C). H2O : 4.76 mg/mL (9.71 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:
PRX-07034 is both a potent and highly selective 5-HT6 receptor antagonist (≥100-fold selectivity for the 5-HT6 receptor compared to 68 other GPCRs, ion channels, and transporters. PRX-07034 inhibits 5-HT1A, 5-HT1B, 5-HT1D, Dopamine D3, Histamine H2, and Opioid μ receptor with Kis of 420 nM, 260 nM, 2.8 µM, 71 nM, 0.64 µM, and 0.45 µM, respectively. PRX-07034 inhibits 5-HT2A, 5-HT2B, and 5-HT2C receptors with IC50s of 2.5 µM, 2.5 µM, and 3.7 µM, respectively. In functional assays, PRX-07034 demonstrates low antagonist activity for the dopamine D3 receptor (IC50=4.8 µM) and very low agonistic activity for the opioid μ-receptor (EC50=19 µM) .
In Vivo:
PRX-07034 (0.1, 1, or 3 mg/kg; i.p.; 30 min prior to delayed spontaneous alternation testing) selectively enhances a switch to a place discrimination.
Products are for research use only. Not for human use.
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