RP 67580
Based on 1 Customer Validation
RP 67580 is a non-peptide antagonist of substance P (SP), competitively inhibits the binding of [3H]SP to neurokinin receptor 1 (NK1 receptor) in rat brain membranes with a Ki value of 4.16 nM. RP 67580 is a specific antagonist of NK1 receptors and can be used in the research of pain and neurogenic inflammation.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 97.4%
- CAS No.: 135911-02-3
- Formule: C29H30N2O2
- Masse moléculaire:438.56
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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NolpitantiumNK1 Receptor Antagonist
Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| IM-9 | IC50 |
30 nM
Compound: 2
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Inhibitory activity against Tachykinin receptor 1 in human IM-9 cells using [125I]-labeled Boltan-Hunter substance P as radioligand
Inhibitory activity against Tachykinin receptor 1 in human IM-9 cells using [125I]-labeled Boltan-Hunter substance P as radioligand
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[PMID: 8576917] |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male albino Sprague-Dawley rats
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Dosage:0.03, 0.1, 0.3, 1 mg/kg
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Administration:i.v.; single dose
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Result:Potently and dose-dependently inhibited the strong plasma extravasation caused by electrical stimulation of the saphenous nerve for 15 minutes with an ED50 value of 0.15 mg/kg.
Chemical Information
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CAS No. 135911-02-3
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Appearance Solid
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Masse moléculaire 438.56
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Formule C29H30N2O2
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Color White to off-white
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SMILES
O=C1[C@@]2([H])CN(C(CC3=CC=CC=C3OC)=N)C[C@@]2([H])C(C4=CC=CC=C4)(C5=CC=CC=C5)CC1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 15 mg/mL (34.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocole
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Pureté et documentation
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Fiche technique (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2802 mL | 11.4009 mL | 22.8019 mL | 57.0047 mL |
| 5 mM | 0.4560 mL | 2.2802 mL | 4.5604 mL | 11.4009 mL | |
| 10 mM | 0.2280 mL | 1.1401 mL | 2.2802 mL | 5.7005 mL | |
| 15 mM | 0.1520 mL | 0.7601 mL | 1.5201 mL | 3.8003 mL | |
| 20 mM | 0.1140 mL | 0.5700 mL | 1.1401 mL | 2.8502 mL | |
| 25 mM | 0.0912 mL | 0.4560 mL | 0.9121 mL | 2.2802 mL | |
| 30 mM | 0.0760 mL | 0.3800 mL | 0.7601 mL | 1.9002 mL |
RP 67580 Related Classifications
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