| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
The primary target of SR-140603 is the neurokinin-1 (NK1) receptor, a G-protein coupled receptor that binds substance P. It acts as a competitive antagonist with a Ki of 7.40 nM, which is about 10-fold less potent than the active S-enantiomer. This defined affinity difference makes it a valuable negative control for stereospecificity assays. It is peripherally restricted, meaning it does not cross the blood-brain barrier. It is used as a reference compound for NK1 receptor pharmacology.
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|---|---|
| ln Vitro |
In vitro, SR-140603 is the less potent enantiomer of SR 140333, used as a negative control. It binds to the NK1 receptor with a Ki of 7.40 nM. It is used in radioligand binding assays to characterize stereoselectivity and in chiral HPLC method development for enantiomeric excess determination of SR-140333 batches. Specific binding affinity data are reported in the literature. It is typically tested at concentrations ranging from 0.1 to 100 nM.
|
| ln Vivo |
In vivo, SR-140603 serves as a peripherally restricted negative control in in vivo models where CNS penetration must be excluded. It is used in studies investigating the peripheral effects of NK1 receptor antagonism. Specific published in vivo efficacy data are limited as it is primarily used as a control compound. It helps differentiate central versus peripheral NK1 receptor-mediated effects in experimental models.
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| Enzyme Assay |
The NK1 receptor binding assay uses membranes from cells expressing recombinant NK1 receptors or NK1 receptor-expressing cell lines. Radiolabeled substance P or a selective NK1 antagonist (e.g., [3H]SP) is incubated with membranes and SR-140603 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 NK1 receptors are treated with SR-140603. Receptor activation is assessed by measuring intracellular calcium mobilization using fluorescent indicators or by IP3 production. For functional studies, isolated tissue preparations are used to assess NK1 receptor-mediated contractions. Cell viability is evaluated using standard reagents.
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| Animal Protocol |
In vivo studies with SR-140603 employ rodent models to assess peripheral NK1 receptor function. The compound is dissolved in saline and administered intraperitoneally or intravenously. Doses are selected based on pharmacokinetic studies. Key readouts include peripheral inflammatory responses and plasma extravasation. Due to its peripheral restriction, CNS-mediated effects are not expected.
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| References |
| Molecular Formula |
C37H45CL3N2O2
|
|---|---|
| Molecular Weight |
656.124407529831
|
| Exact Mass |
654.254
|
| CAS # |
154728-59-3
|
| PubChem CID |
5311449
|
| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
44
|
| Complexity |
913
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
CC(C)OC1=CC=CC(=C1)CC(=O)N2CCC[C@@](C2)(CC[N+]34CCC(CC3)(CC4)C5=CC=CC=C5)C6=CC(=C(C=C6)Cl)Cl.[Cl-]
|
| InChi Key |
NQHFSECYQAQZBN-SJYHNBSJSA-M
|
| InChi Code |
InChI=1S/C37H45Cl2N2O2.ClH/c1-28(2)43-32-11-6-8-29(24-32)25-35(42)40-19-7-14-37(27-40,31-12-13-33(38)34(39)26-31)18-23-41-20-15-36(16-21-41,17-22-41)30-9-4-3-5-10-30;/h3-6,8-13,24,26,28H,7,14-23,25,27H2,1-2H3;1H/q+1;/p-1/t36?,37-,41?;/m0./s1
|
| Chemical Name |
1-[(3R)-3-(3,4-dichlorophenyl)-3-[2-(4-phenyl-1-azoniabicyclo[2.2.2]octan-1-yl)ethyl]piperidin-1-yl]-2-(3-propan-2-yloxyphenyl)ethanone;chloride
|
| Synonyms |
SR140603; SR 140603; SR-140603
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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 | 1.5241 mL | 7.6206 mL | 15.2411 mL | |
| 5 mM | 0.3048 mL | 1.5241 mL | 3.0482 mL | |
| 10 mM | 0.1524 mL | 0.7621 mL | 1.5241 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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