| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
SR 140333 targets the neurokinin-1 (NK1) receptor, the primary receptor for substance P. It binds with high affinity (Ki = 0.74 nM) and shows competitive inhibition. The R enantiomer SR 140603 has a Ki of 7.40 nM. The compound blocks NK1 receptor activation, inhibiting pain signaling.
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|---|---|
| ln Vitro |
In vitro, SR 140333 shows potent NK1 receptor antagonism with an IC50 of 1.6 nM. Radioligand binding studies using 125I-Bolton-Hunter substance P reveal competitive inhibition. The compound blocks activation of rat thalamic neurons in response to nociceptive stimulation. It shows high selectivity for NK1 over other receptors.
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| ln Vivo |
In vivo, SR 140333 blocks the activation of rat thalamic neurons following noxious stimulation. It is used in research on pain mechanisms and neurokinin signaling. The compound is valuable for studying the role of NK1 receptors in various neurophysiological processes.
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| Enzyme Assay |
NK1 receptor binding is assessed using radioligand binding assays with 125I-Bolton-Hunter substance P. Membrane preparations from cells expressing human NK1 receptors are incubated with the radioligand and varying concentrations of SR 140333. Nonspecific binding is determined using excess cold ligand. Ki values are calculated.
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| Cell Assay |
SR 140333 is evaluated in U373MG cells or other cells expressing NK1 receptors. Receptor binding and functional assays are performed. Calcium flux or other signaling readouts are measured in response to substance P stimulation in the presence of the compound. IC50 values are determined.
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| Animal Protocol |
SR 140333 is evaluated in animal models of pain and neurogenic inflammation. The compound is administered via appropriate routes. Nociceptive responses are measured. Thalamic neuron activation is assessed. Pharmacokinetic studies determine bioavailability and half-life.
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| References | |
| Additional Infomation |
SR 140333 is a tachykinin antagonist with potential for treating diarrhea caused by food allergies or inflammatory bowel disease. See also: Nopistane besylate (note moved here). Drug indications: Has been investigated for the treatment of asthma and inflammatory bowel disease.
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| Molecular Formula |
C37H45CL3N2O2
|
|---|---|
| Molecular Weight |
656.129
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| Exact Mass |
654.254
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| CAS # |
153050-21-6
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| Related CAS # |
(R)-Nolpitantium; 154728-59-3
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| PubChem CID |
108166
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
44
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| Complexity |
913
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| Defined Atom Stereocenter Count |
1
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| SMILES |
[Cl-].CC(OC1C=CC=C(CC(N2CCCC(C3=CC=C(Cl)C(Cl)=C3)(CC[N+]34CCC(C5=CC=CC=C5)(CC3)CC4)C2)=O)C=1)C
|
| InChi Key |
NQHFSECYQAQZBN-LSYPWIJNSA-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,7,14-23,25,27H2,1-2H31H/q+1/p-1/t36?,37-,41?/m1./s1
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| Chemical Name |
1-Azoniabicyclo(2.2.2)octane, 1-(2-(3-(3,4-dichlorophenyl)-1-((3-(1-methylethoxy)phenyl)acetyl)-3-piperidinyl)ethyl)-4-phenyl-, chloride, (S)-
|
| Synonyms |
SR 140,333 SR 140333ASR 140333
|
| 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 | 1.5241 mL | 7.6204 mL | 15.2409 mL | |
| 5 mM | 0.3048 mL | 1.5241 mL | 3.0482 mL | |
| 10 mM | 0.1524 mL | 0.7620 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00232258 | COMPLETED | Drug: Nolpitantium besylate | Inflammatory Bowel Disease Ulcerative Colitis |
Sanofi | 2005-04 | Phase 2 |
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