Tapencarium
Based on 1 publication(s) in Google Scholar
Tapencarium (RZL-012; Utenpanium chloride) is an injectable fat volume-reducing agent. Tapencarium irreversibly impairs cell membrane integrity, increases membrane permeability, induces elevated cytoplasmic calcium, alters mitochondrial membrane potential, and triggers necrosis. Tapencarium induces fat necrosis, inflammatory responses and fibrous tissue formation at the injection site. Tapencarium can be used in research related to submental fat excess and Dercum's disease.
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- Pureza : 99.53%
- No. CAS: 1436920-57-8
- Fòrmula: C20H25Br2ClN2
- Peso molecular:488.69
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Tapencarium
More
Actividad biológica
Descripciòn
In Vitro
Tapencarium (RZL-012) (0.01-300 μM; 2-24 h) reduces the viability of Wi38 human lung fibroblasts and differentiated human visceral adipocytes in a time-dependent manner[2].
Tapencarium (12.5-400 μM; 2 h) directly disrupts the integrity of human bone marrow mesenchymal stem cell-derived nanoghost membranes in a dose-dependent manner, causing increased permeability, reduced nanoghost counts, and full membrane destruction at high concentrations[2].
Tapencarium (0.03-100 μM; 2-24 h) induces dose- and time-dependent membrane disruption in differentiated human adipocytes, with early increases in intracellular calcium and membrane permeability preceding mitochondrial dysfunction and cell death[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Wi38 human lung fibroblasts
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Concentration:0.01, 0.03, 0.1, 1, 3, 10, 30, 100, 300 μM
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Incubation Time:2 h, 6 h, 24 h
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Result:Reduced Wi38 human lung fibroblast viability with IC50 values ranging from 30.8 μM (2 h incubation) to 25.5 μM (24 h incubation).
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Cell Line:differentiated human visceral adipocytes
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Concentration:0.01, 0.03, 0.1, 1, 3, 10, 30, 100, 300 μM
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Incubation Time:2 h, 6 h, 24 h
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Result:Reduced differentiated human visceral adipocyte viability with IC50 values ranging from 106.1 μM (2 h incubation) to 52.0 μM (24 h incubation).
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Domestic Yorkshire crossbred (male and female, initial weight 73.5-86.5 kg (males) and 74.0-84.5 kg (females), subcutaneous abdominal fat injection model)[2]
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Dosage:25 mg per injection site; 500 mg per pig
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Administration:s.c.; single multiinjection session
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Result:Induced marked liponecrosis and slight inflammation with no detectable fibrosis at 24 hours postdosing.
Decreased liponecrosis and inflammation scores to ~1.2 and ~0.4, respectively, while increasing fibrosis to a mean score ~1.0 at 14 days postdosing.
Reduced liponecrosis and inflammation scores to 0, and increased fibrosis to a mean score ~1.7 at 84 days postdosing.
Achieved a mean 18% reduction in fat thickness at injected sites compared to noninjected sites at 84 days postdosing.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1436920-57-8
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Appearance Solid
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Peso molecular 488.69
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Fòrmula C20H25Br2ClN2
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Color White to off-white
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SMILES
BrC1=CC=C2C(C3=C(N2CCCCC[N+](C)(C)C)C=CC(Br)=C3)=C1.[Cl-]
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Synonyms
RZL-012; Utenpanium chloride
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Eur J Pharmacol
Phosphorylated HAND1 contributes to trophoblast cell migration during placentation by activating the Vav2-Rac1-PAK signaling. [Abstract]2026 Jun 26:1030:179096. PMID: 42361881
Solvente y solubilidad
In Vitro:
DMSO : 50 mg/mL (102.31 mM; ultrasonic and warming and heat to 60°C; 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (10.23 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (10.23 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Shridharani SM, et al. Efficacy and Safety of Tapencarium (RZL-012) in Submental Fat Reduction. Aesthetic surgery journal. 2023 Sep 14;43(10):NP797-NP806. [Content Brief]
[2]. Blaugrund E, et al. Mode of Action of RZL-012, a New Fat-Reducing Molecule. Dermatologic surgery : official publication for American Society for Dermatologic Surgery [et al.]. 2021 Dec 01;47(12):1601-1605. [Content Brief]
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 (sealed storage, away from moisture). 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 |
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| DMSO | 1 mM | 2.0463 mL | 10.2314 mL | 20.4629 mL | 51.1572 mL |
| 5 mM | 0.4093 mL | 2.0463 mL | 4.0926 mL | 10.2314 mL | |
| 10 mM | 0.2046 mL | 1.0231 mL | 2.0463 mL | 5.1157 mL | |
| 15 mM | 0.1364 mL | 0.6821 mL | 1.3642 mL | 3.4105 mL | |
| 20 mM | 0.1023 mL | 0.5116 mL | 1.0231 mL | 2.5579 mL | |
| 25 mM | 0.0819 mL | 0.4093 mL | 0.8185 mL | 2.0463 mL | |
| 30 mM | 0.0682 mL | 0.3410 mL | 0.6821 mL | 1.7052 mL | |
| 40 mM | 0.0512 mL | 0.2558 mL | 0.5116 mL | 1.2789 mL | |
| 50 mM | 0.0409 mL | 0.2046 mL | 0.4093 mL | 1.0231 mL | |
| 60 mM | 0.0341 mL | 0.1705 mL | 0.3410 mL | 0.8526 mL | |
| 80 mM | 0.0256 mL | 0.1279 mL | 0.2558 mL | 0.6395 mL | |
| 100 mM | 0.0205 mL | 0.1023 mL | 0.2046 mL | 0.5116 mL |
Tapencarium Related Classifications
HY-172241 Related Classifications
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Keywords
- Tapencarium
- 1436920-57-8
- RZL-012
- Utenpanium
- RZL012
- RZL 012
- Biochemical Assay Reagents
- subcutaneous abdominal fat
- pigs
- differentiated human adipocytes
- Dercum disease
- adipocytes
- Wi38 human lung fibroblast
- excess submental fat
- differentiated human visceral adipocyte
- fibroblasts
- human bone marrow mesenchymal stem cell-derived nanoghost membranes
- Inhibitor
- inhibitor
- inhibit