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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- Purity : 99.53%
- CAS No.: 1436920-57-8
- 화학식: C20H25Br2ClN2
- 분자량:488.69
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보관:
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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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Tapencarium
More
Biological Activity
제품 설명
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. Further protocols information, click here.
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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.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1436920-57-8
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Appearance Solid
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분자량 488.69
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
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
용액&용해도
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.
Protocol
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How to Select the Route of Administration for Mammals
Route-of-administration selection in mammals is a pharmacokinetic, pharmacodynamic, formulation, animal-welfare, and translational decision, not a default technical choice. The selected route should match the study goal: intravenous dosing is most useful when complete systemic exposure and rapid onset are required, oral dosing is most translational for orally intended medicines but is affected by absorption and first-pass metabolism, subcutaneous or intramuscular dosing can provide slower systemic exposure, and intraperitoneal dosing can be useful in rodent proof-of-concept studies but may have limited clinical translation. Published route-comparison studies show that the same compound can produce different exposure, onset, bioavailability, tissue distribution, and tolerability depending on route; therefore, route choice should be supported by pilot pharmacokinetic or pharmacodynamic evidence when the literature is insufficient. Unresolved questions include how to standardize route sel
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Mitochondrial membrane-potential fluorescent assay
Mitochondrial membrane potential fluorescent assays estimate ΔΨm in living cells using lipophilic cationic dyes such as TMRM, TMRE, rhodamine 123, and JC-1, which accumulate in mitochondria according to membrane polarization; loss of signal after FCCP or CCCP treatment is interpreted as mitochondrial depolarization. TMRM/TMRE and rhodamine 123 are commonly used for semi-quantitative live-cell microscopy or flow cytometry, while JC-1 can report a shift from red aggregate fluorescence to green monomer fluorescence during depolarization; interpretation requires controls because dye concentration, quenching mode, cell type, dye efflux, and mitochondrial mass can affect fluorescence independently of ΔΨm.
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Fluorescent plasma-membrane potential dye assay
Fluorescent plasma-membrane potential dye assays measure changes in cell membrane potential using voltage-sensitive dyes whose fluorescence changes when cells depolarize or hyperpolarize. Anionic bis-oxonol dyes such as DiBAC4(3) enter depolarized cells more readily and show increased fluorescence after intracellular binding, while hyperpolarization reduces dye accumulation and fluorescence. FMP/FLIPR membrane-potential dyes are used for faster, homogeneous microplate assays of ion-channel or receptor-mediated membrane-potential changes.
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Mitochondrial membrane-potential and mitochondrial mass staining
Mitochondrial membrane potential staining measures the electrochemical polarization across the mitochondrial inner membrane in live cells using lipophilic cationic fluorescent probes; early rhodamine-based work showed that selective mitochondrial dye accumulation is lost when the mitochondrial transmembrane potential is dissipated. JC-1 reports mitochondrial polarization by shifting from green monomer fluorescence to red J-aggregate fluorescence as dye concentration increases within energized mitochondria; therefore, the red/green fluorescence ratio is used as a relative readout of mitochondrial membrane potential. TMRE or TMRM staining provides a single-channel relative readout because these cationic rhodamine esters accumulate in polarized mitochondria, and lower fluorescence indicates reduced mitochondrial polarization when acquisition and dye-loading conditions are controlled. Mitochondrial mass staining is commonly performed with MitoTracker Green FM or related MitoTracker dyes as
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Transepithelial/transendothelial electrical resistance assay
TEER measures electrical resistance across epithelial or endothelial monolayers cultured on permeable supports, and the readout reflects ionic conductance through the cell barrier, especially the paracellular pathway regulated by junctional integrity. TEER can be measured without destroying the monolayer and is commonly used before or during transport, permeability, barrier-disruption, and barrier-maturation experiments. TEER values are influenced by biological maturation and technical conditions; reported factors include temperature, medium formulation, passage number, electrode geometry, membrane properties, and junctional length during early monolayer maturation. Therefore, TEER should be interpreted with blank-insert subtraction, area normalization, repeated readings, and, when possible, orthogonal barrier readouts such as FITC-dextran flux or tight-junction staining.
순도&문서
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Data Sheet (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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Handling Instructions (2659 KB)
References
[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