trans-Ned 19
Based on 1 Customer Validation
trans-Ned 19 is a NAADP antagonist and TPC blocker. trans-Ned 19 suppresses the calcium signal and the rat aorta relaxation in response to low histamine concentrations. trans-Ned 19 increases the spontaneous acrosome reaction rate, alleviates anti-CD3 mAb-induced intestinal inflammation, and improves kidney damage in mice with nephrotoxic serum nephritis.
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- Pureza: 99.33%
- No. CAS: 1354235-96-3
- Fòrmula: C30H31FN4O3
- Peso molecular:514.59
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Help & FAQs
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Ver todos los productos específicos de isoformas Calcium Channel
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Actividad biológica
NAADP, TPC, Calcium Channel[1]
trans-Ned 19 (25-100 μM; 1 h) inhibits T cell receptor (TCR)-stimulated Ca2+ signaling, cell activation and proliferation in primary naive CD4+ T cells from C57BL/6N mice[1].
trans-Ned 19 (25-50 µM; 10 min) inhibits Norepinephrine (HY-13715)-induced Ca2+ elevation in rat aortic smooth muscle cells in a concentration-dependent manner[2].
trans-Ned 19 (10 µM) causes lysosomal cholesterol accumulation in human umbilical vein endothelial cells, inhibits CD63 transport from late endosomes/lysosomes to Weibel-Palade bodies, and reduces the amount of CD63 associated with Weibel-Palade bodies[3].
trans-Ned 19 (100 μM; 30 min) significantly increases the spontaneous acrosome reaction rate in acrosome reaction assay performed on permeabilized mouse sperm[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
trans-Ned 19 (20 mg/kg; i.p.; once administered 2 h before the first injection of anti-CD3 antibody and then once daily for 3 days or once administered 2 h before the injection of nephrotoxic serum and then once daily for 10 days) improves disease progression and reduces weight loss in a mouse model of transient intestinal inflammation induced by CD3-specific antibody, and improves renal damage in mice with nephrotoxic serum nephritis[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice + CD3-specific antibody-induced transient intestinal inflammation mouse model or nephrotoxic serum nephritis mouse model[4]
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Dosage:20 mg/kg
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Administration:intraperitoneal injection, once 2 h before the first injection of anti-CD3 antibody, then once a day for 3 days; once 2 hours before the injection of nephrotoxic serum, then once a day for 10 days
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Result:Improved disease progression, reduced weight loss, and reduced the percentage of IFN-γ-producing cells and IFN-γ, IL-17A dual-producing cells in the small intestinal mucosa (transient intestinal inflammation mice).
Improved kidney damage, tended to reduce IL-17A+IFN-γ+ cells and IL-17A+IFN-γ dual-producing cells, increased the percentage of Th1 cells, and reduced the percentage of Foxp3⁺ Tregs (nephrotoxic serum nephritis mice).
Chemical Information
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No. CAS 1354235-96-3
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Appearance Solid
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Peso molecular 514.59
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Fòrmula C30H31FN4O3
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Color Light yellow to yellow
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SMILES
O=C([C@@H]1CC2=C([C@@H](C3=CC=C(OC)C(CN4CCN(C5=CC=CC=C5F)CC4)=C3)N1)NC6=C2C=CC=C6)O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (194.33 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. 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)
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: ≥ 6.25 mg/mL (12.15 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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: ≥ 6.25 mg/mL (12.15 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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.
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.
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 (283 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]. Nawrocki M, et al. Trans-Ned 19-Mediated Antagonism of Nicotinic Acid Adenine Nucleotide-Mediated Calcium Signaling Regulates Th17 Cell Plasticity in Mice. Cells. 2021 Nov 5;10(11):3039. [Content Brief]
[2]. Trufanov SK, et al. The Role of Two-Pore Channels in Norepinephrine-Induced [Ca2+]i Rise in Rat Aortic Smooth Muscle Cells and Aorta Contraction. Cells. 2019 Sep 25;8(10):1144. [Content Brief]
[5]. Arndt L, et al. NAADP and the two-pore channel protein 1 participate in the acrosome reaction in mammalian spermatozoa. Mol Biol Cell. 2014 Mar;25(6):948-64. [Content Brief]
[6]. Zharkich IL, et al. Suppression of Histamine-Induced Relaxation of Rat Aorta and Calcium Signaling in Endothelial Cells by Two-Pore Channel Blocker trans-NED19 and Hydrogen Peroxide. Izv Akad Nauk Ser Biol. 2016 Jul;(4):430-438. [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. 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 | 1.9433 mL | 9.7165 mL | 19.4329 mL | 48.5824 mL |
| 5 mM | 0.3887 mL | 1.9433 mL | 3.8866 mL | 9.7165 mL | |
| 10 mM | 0.1943 mL | 0.9716 mL | 1.9433 mL | 4.8582 mL | |
| 15 mM | 0.1296 mL | 0.6478 mL | 1.2955 mL | 3.2388 mL | |
| 20 mM | 0.0972 mL | 0.4858 mL | 0.9716 mL | 2.4291 mL | |
| 25 mM | 0.0777 mL | 0.3887 mL | 0.7773 mL | 1.9433 mL | |
| 30 mM | 0.0648 mL | 0.3239 mL | 0.6478 mL | 1.6194 mL | |
| 40 mM | 0.0486 mL | 0.2429 mL | 0.4858 mL | 1.2146 mL | |
| 50 mM | 0.0389 mL | 0.1943 mL | 0.3887 mL | 0.9716 mL | |
| 60 mM | 0.0324 mL | 0.1619 mL | 0.3239 mL | 0.8097 mL | |
| 80 mM | 0.0243 mL | 0.1215 mL | 0.2429 mL | 0.6073 mL | |
| 100 mM | 0.0194 mL | 0.0972 mL | 0.1943 mL | 0.4858 mL |
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