| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| ln Vitro |
In functional assays, PRX-07034 exhibited low antagonistic activity against dopamine D3 receptors (IC50= 4.8 µM) and very low agonistic opioid μ-receptor activity (EC50=19 µM). PRX-07034 is a potent and highly selective 5-HT6 receptor antagonist (≥100-fold selective for 5-HT6 receptors compared to 68 other GPCRs, ion channels, and transporters). It also inhibits 5-HT1A, 5-HT1B, 5-HT1D, histamine H2, and opioid mu receptors with Kis of 420 nM, 260 nM, 2.8 µM, 71 nM, 0.64 µM, and 0.45 µM, respectively.
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| ln Vivo |
Switching to place discrimination is selectively enhanced by PRX-07034 (0.1, 1, or 3 mg/kg; i.p.; 30 min before delayed spontaneous alternation testing) [1].
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| Animal Protocol |
Animal/Disease Models: Male Long-Evans rat, body weight approximately 350 g[1]
Doses: 0.1, 1 or 3 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: 1 and 3 mg/kg (but not 0.1 mg/kg) demonstrated significant Enhanced delayed spontaneous alternations. The drug at 1 and 3 mg/kg also enhanced switching between place and response strategies but did not affect initial learning of place or response discrimination. |
| References |
[1]. Eric G Mohler, et al. The effects of PRX-07034, a novel 5-HT6 antagonist, on cognitive flexibility and working memory in rats. Psychopharmacology (Berl). 2012 Apr;220(4):687-96.
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| Additional Infomation |
Drug Indication
Investigated for use/treatment in alzheimer's disease, obesity, and schizophrenia and schizoaffective disorders. Mechanism of Action PRX-07034 is a novel, highly selective, small-molecule antagonist of a specific G-protein coupled receptor (GPCR) known as 5-HT6 being developed for the treatment of obesity, Alzheimer's disease and cognitive impairment associated with schizophrenia. PRX-07034 has also been shown to enhance cognitive function in preclinical animal models of memory impairment through a dual mechanism of action.It has an effect on both the acetylcholine and glutamate neurotransmitter systems in the brain, which makes it a potentially complementary therapy to cholinesterase inhibitors, a class of drugs approved for the treatment of Alzheimer's disease. |
| Molecular Formula |
C21H29CL2N3O4S
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|---|---|
| Molecular Weight |
490.44
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| Exact Mass |
489.126
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| CAS # |
903580-39-2
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| Related CAS # |
903580-16-5;903580-39-2 (HCl);
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| PubChem CID |
23653584
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
5.693
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
31
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| Complexity |
641
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.O=S(C)(C1C(NC(C)C2C(OC)=C(OC)C=C(Cl)C=2)=CC(N2CCNCC2)=CC=1)=O
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| InChi Key |
PILCQJJJAFRKHO-UHFFFAOYSA-N
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| InChi Code |
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
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| Chemical Name |
N-[1-(5-chloro-2,3-dimethoxyphenyl)ethyl]-2-methylsulfonyl-5-piperazin-1-ylaniline;hydrochloride
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| Synonyms |
PRX07034 PRX 07034PRX-07034 PRX-07034 HCl PRX-07034 hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~31.25 mg/mL (~63.72 mM)
H2O : ~4.76 mg/mL (~9.71 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.24 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.24 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.24 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0390 mL | 10.1949 mL | 20.3899 mL | |
| 5 mM | 0.4078 mL | 2.0390 mL | 4.0780 mL | |
| 10 mM | 0.2039 mL | 1.0195 mL | 2.0390 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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