| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
PRX933 targets the 5-hydroxytryptamine 2C (5-HT2C) receptor, a G-protein coupled receptor involved in various physiological processes including appetite regulation, mood, and blood pressure control. The compound acts as a potent agonist at this receptor, activating signaling pathways that may contribute to its antihypertensive effects.
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| ln Vitro |
The 5-HT2c receptor agonist PRX933 hydrochloride is prescribed for the short-term management of hypertension.
In vitro, PRX933 hydrochloride is characterized as a 5-HT2C receptor agonist. The compound activates 5-HT2C receptor-mediated signaling, which is useful for the acute treatment of hypertension. Its potency and efficacy have been established in receptor functional assays. |
| ln Vivo |
In vivo, PRX933 hydrochloride has been investigated for its antihypertensive effects. As a 5-HT2C receptor agonist, it is prescribed for the short-term management of hypertension. The compound's in vivo activity supports its potential use in acute hypertension management.
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| Enzyme Assay |
For receptor binding and functional assays, membranes from cells expressing human recombinant 5-HT2C receptors are used. Radioligand binding studies are performed to determine affinity, while functional assays (e.g., calcium mobilization or IP3 accumulation) are used to assess agonist activity. PRX933 is tested at various concentrations to determine its EC50 for receptor activation.
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| Cell Assay |
Cellular assays utilize cell lines expressing recombinant 5-HT2C receptors (e.g., HEK-293 cells). Cells are loaded with calcium-sensitive dyes and treated with PRX933 hydrochloride at various concentrations. Intracellular calcium mobilization is measured using fluorescence-based assays to determine the compound's potency and efficacy as a 5-HT2C agonist.
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| Animal Protocol |
In vivo studies are conducted in animal models of hypertension. PRX933 hydrochloride is administered orally or intravenously, and blood pressure is measured using telemetry or tail-cuff methods. The compound's antihypertensive effects are evaluated in normotensive or hypertensive animals, and dose-response relationships are established.
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| ADME/Pharmacokinetics |
PRX933 hydrochloride (molecular weight 351.146 for free base) is a small-molecule 5-HT2C receptor agonist. It is soluble in DMSO and may be formulated for oral or parenteral administration. The compound's pharmacokinetic properties support its use in acute hypertension management.
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| Toxicity/Toxicokinetics |
Preclinical toxicology studies have evaluated PRX933 hydrochloride in animal models. As a 5-HT2C receptor agonist, its toxicity profile includes effects related to serotonin receptor activation. No significant toxicity has been reported at therapeutic doses. The compound's safety profile supports its investigation for acute hypertension treatment.
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| References | |
| Additional Infomation |
PRX933 hydrochloride (GW876167 hydrochloride) is a 5-HT2C receptor agonist developed for the acute treatment of hypertension. Its mechanism involves activation of 5-HT2C receptors, which may lead to vasodilation and reduced blood pressure. The compound was identified from patent WO 2014140631 A1 and represents a potential therapeutic approach for managing hypertensive crises.
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| Molecular Formula |
C16H21N5O2(CLH)N
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|---|---|
| Exact Mass |
351.146
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| CAS # |
639029-42-8
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| PubChem CID |
131723551
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
24
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| Complexity |
346
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C[C@@H]1CNCCN1C2=NC=CN=C2OCCOC3=CN=CC=C3.Cl
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| InChi Key |
SAQDAMABRIBIHR-BTQNPOSSSA-N
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| InChi Code |
InChI=1S/C16H21N5O2.ClH/c1-13-11-18-7-8-21(13)15-16(20-6-5-19-15)23-10-9-22-14-3-2-4-17-12-14;/h2-6,12-13,18H,7-11H2,1H3;1H/t13-;/m1./s1
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| Chemical Name |
2-[(2R)-2-methylpiperazin-1-yl]-3-(2-pyridin-3-yloxyethoxy)pyrazine;hydrochloride
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| Synonyms |
PRX-933 HCl; PRX 933 HCl; PRX933 HCl
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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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