| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
The primary target of SR57227A is the 5-HT3 receptor, a ligand-gated ion channel that mediates fast excitatory serotonergic neurotransmission. It acts as a highly selective agonist at both central and peripheral 5-HT3 receptors. It also inhibits NMDA receptor-mediated responses in rat cortical pyramidal cells. By activating 5-HT3 receptors, it modulates neurotransmitter release and neuronal excitability. It is used to study 5-HT3 receptor function in nausea, anxiety, and pain.
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|---|---|
| ln Vitro |
In vitro, SR57227A is a highly selective 5-HT3 receptor agonist. It activates 5-HT3 receptor-mediated currents in electrophysiological assays. It also inhibits NMDA receptor-mediated responses in rat cortical pyramidal cells. The compound is used in radioligand binding assays and functional assays to characterize 5-HT3 receptor pharmacology. Specific EC50 values for 5-HT3 receptor activation are reported in the literature. It is typically tested at concentrations ranging from 0.1 to 100 µM.
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| ln Vivo |
In vivo, SR57227A has been evaluated in animal models for its effects on nausea, anxiety, and pain. As a 5-HT3 receptor agonist, it may modulate these behaviors. Specific published in vivo efficacy data, including dosing regimens and behavioral outcomes, are reported in preclinical literature. It is primarily used as a research tool for studying 5-HT3 receptor function in the CNS and periphery.
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| Enzyme Assay |
The 5-HT3 receptor binding assay uses membranes from cells expressing recombinant 5-HT3 receptors or rat brain homogenates. Radiolabeled 5-HT3 antagonist (e.g., [3H]GR65630) is incubated with membranes and SR57227A at serial dilutions. Bound radioactivity is separated by filtration and quantified by scintillation counting. Ki values are calculated from competition curves.
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| Cell Assay |
For cell-based assays, cells expressing 5-HT3 receptors are treated with SR57227A. Receptor activation is assessed by measuring intracellular calcium mobilization using fluorescent indicators or by patch-clamp electrophysiology. Cell viability is evaluated using standard reagents.
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| Animal Protocol |
In vivo studies with SR57227A employ rodent models of nausea (emesis), anxiety (elevated plus maze), or pain (tail-flick). The compound is dissolved in saline and administered intraperitoneally or intravenously. Key readouts include emetic responses, anxiolytic-like behavior, and antinociception. Doses are selected based on pharmacokinetic studies.
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| Additional Infomation |
1-(6-chloro-2-pyridyl)-4-piperidinamine is a tertiary amine compound and also a dialkyl aromatic amine.
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| Molecular Formula |
C10H14CLN3
|
|---|---|
| Molecular Weight |
211.69
|
| Exact Mass |
211.088
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| CAS # |
77145-51-8
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| Related CAS # |
77145-51-8;77145-61-0 (HCl);
|
| PubChem CID |
131747
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| Appearance |
Typically exists as solid at room temperature
|
| LogP |
2.427
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
|
| Heavy Atom Count |
14
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| Complexity |
180
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
ClC1N=C(N2CCC(N)CC2)C=CC=1
|
| InChi Key |
WPVVMKYQOMJPIN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H14ClN3/c11-9-2-1-3-10(13-9)14-6-4-8(12)5-7-14/h1-3,8H,4-7,12H2
|
| Chemical Name |
1-(6-chloropyridin-2-yl)piperidin-4-amine
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| Synonyms |
SR-57227A; SR 57227A; SR57227A
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.7239 mL | 23.6194 mL | 47.2389 mL | |
| 5 mM | 0.9448 mL | 4.7239 mL | 9.4478 mL | |
| 10 mM | 0.4724 mL | 2.3619 mL | 4.7239 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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