Tenidap
Based on 1 Customer Validation
Tenidap (CP-66248) is an orally active cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) inhibitor. Tenidap exerts anti-inflammatory and chondroprotective effects by downregulating IL-1 receptor expression, reducing the release of pro-inflammatory cytokines, and inhibiting metalloproteinase and acute-phase protein production, while also inhibiting SLC26A3-mediated chloride transport and the pH and membrane potential changes associated with sperm capacitation. Tenidap attenuates carrageenan-induced paw edema and acetic acid-induced writhing, and induces gastric ulcers in a dose-dependent manner, and can be used for research on rheumatoid arthritis.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.93%
- No. CAS: 120210-48-2
- Fòrmula: C14H9ClN2O3S
- Peso molecular:320.75
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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HY-105028R
Tenidap (Standard)Reference Standard -
HY-13568
BenoxaprofenNonsteroidal Anti-inflammatory Agent -
HY-B0253
PiroxicamCOX Inhibitor -
HY-B0138
Ketorolac tromethamine saltCOX Inhibitor -
HY-111140
YS121mPGES-1/5-LOX Inhibitor -
HY-B0634
AceclofenacNSAID -
HY-B0578A
Loxoprofen sodiumAnti-Inflammatory Agent -
HY-B0138R
Ketorolac tromethamine salt (Standard)COX Inhibitor -
HY-115866
COX-2-IN-6COX Inhibitor -
HY-13568R
Benoxaprofen (Standard)Anti-inflammatory/Antipyretic Compound -
HY-B0253R
Piroxicam (Standard)COX Inhibitor -
HY-126898
5-LO/mPGES1-IN-15-LO/mPGES-1 Inhibitor
Actividad biológica
Descripciòn
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COX-1 2.56 μM (IC50) |
COX-2 8.4 μM (IC50) |
5-LOX 36.70 μM (IC50) |
IL-1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| CHO | EC50 |
402 nM
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Potentiation of 86Rb+ efflux in Chinese hamster ovary CHO cells stably expressing hKir2.3 incubated with tenidap for 50 min by 86Rb+ efflux assay.
Potentiation of 86Rb+ efflux in Chinese hamster ovary CHO cells stably expressing hKir2.3 incubated with tenidap for 50 min by 86Rb+ efflux assay.
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S0014-2999(01)01590-4 |
| CHO | EC50 |
1.3 μM
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Potentiation of whole-cell hKir2.3 currents in Chinese hamster ovary CHO cells stably expressing hKir2.3 by whole-cell patch-clamp electrophysiology.
Potentiation of whole-cell hKir2.3 currents in Chinese hamster ovary CHO cells stably expressing hKir2.3 by whole-cell patch-clamp electrophysiology.
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S0014-2999(01)01590-4 |
In Vitro
Tenidap (5-10 μg/mL) protects bovine and porcine cartilage from IL-1-induced catabolic effects and GAG loss and promotes cartilage repair[2].
Tenidap (20 μg/mL) reduces IL-1 receptor number and suppresses collagenase and stromelysin synthesis in human chondrocytes[2].
Tenidap (0.5-100 µM; 60 min) partially blocks capacitation-associated Em hyperpolarization in mouse sperm with an estimated IC50 of 2.6 µM[3].
Tenidap (0.5-100 µM; 10 min) blocks ~50% of the HCO3−-induced Em hyperpolarization in noncapacitated mouse sperm[3].
Tenidap (0.5-100 µM; 60 min) reduces the capacitation-associated pHi increase in mouse sperm with an estimated IC50 of 3.5 µM[3].
Tenidap (10 µM; 50 min) is a potent opener of hKir2.3 stably expressed in CHO cells, increasing 86Rb+ efflux with an EC50 of 402 nM[4].
Tenidap (10 µM; within seconds) reversibly potentiates whole-cell hKir2.3 currents in CHO cells with an EC50 of 1.3 µM[4].
Tenidap (1-10 µM) hyperpolarizes hKir2.3-expressing CHO cells and reduces input resistance at 10 µM[4].
Tenidap (10-30 µM) increases hKir2.3 currents in outside-out patches, and intracellular bovine serum albumin does not prevent potentiation, consistent with an extracellular site of action[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Tenidap reduces paw swelling and serum CRP in rat adjuvant arthritis when administered before or after disease onset[2].
Tenidap (10.38 mg/kg; p.o.; single administration; 1 h before carrageenan) sodium attenuates carrageenan-induced paw edema in male Wistar rats, with inhibition rates of 23.81%, 38.89%, and 19.61% at 1, 3, and 6 h, respectively[5].
Tenidap (20.76 mg/kg; p.o.) sodium reduces acetic acid-induced writhing in mice with an inhibition rate of 70.4%[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar (male)[5]
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Dosage:10.38 mg/kg
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Administration:p.o.; once; 1 h before carrageenan
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Result:Increase in paw volume was 0.16 mL at 1 h, 0.22 mL at 3 h, and 0.41 mL at 6 h.
Inhibition rates were 23.81% at 1 h, 38.89% at 3 h, and 19.61% at 6 h.
Chemical Information
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No. CAS 120210-48-2
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Appearance Solid
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Peso molecular 320.75
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Fòrmula C14H9ClN2O3S
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Color White to yellow
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SMILES
O/C(C1=CC=CS1)=C2C3=C(C=CC(Cl)=C3)N(C(N)=O)C/2=O
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Synonyms
CP-66248
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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
In Vitro:
DMSO : 25 mg/mL (77.94 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)
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: 2.5 mg/mL (7.79 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
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 (298 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[2]. Breedveld F, et al. Tenidap: a novel cytokine-modulating antirheumatic drug for the treatment of rheumatoid arthritis. Scandinavian journal of rheumatology. Supplement. 1994;100:31-44. [Content Brief]
[5]. Lai Y, et al. Synthesis and biological evaluation of 3-[4-(amino/methylsulfonyl)phenyl]methylene-indolin-2-one derivatives as novel COX-1/2 and 5-LOX inhibitors. Bioorganic & medicinal chemistry letters. 2010 Dec 15;20(24):7349-53. [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 | 3.1177 mL | 15.5885 mL | 31.1769 mL | 77.9423 mL |
| 5 mM | 0.6235 mL | 3.1177 mL | 6.2354 mL | 15.5885 mL | |
| 10 mM | 0.3118 mL | 1.5588 mL | 3.1177 mL | 7.7942 mL | |
| 15 mM | 0.2078 mL | 1.0392 mL | 2.0785 mL | 5.1962 mL | |
| 20 mM | 0.1559 mL | 0.7794 mL | 1.5588 mL | 3.8971 mL | |
| 25 mM | 0.1247 mL | 0.6235 mL | 1.2471 mL | 3.1177 mL | |
| 30 mM | 0.1039 mL | 0.5196 mL | 1.0392 mL | 2.5981 mL | |
| 40 mM | 0.0779 mL | 0.3897 mL | 0.7794 mL | 1.9486 mL | |
| 50 mM | 0.0624 mL | 0.3118 mL | 0.6235 mL | 1.5588 mL | |
| 60 mM | 0.0520 mL | 0.2598 mL | 0.5196 mL | 1.2990 mL |
Tenidap Related Classifications
HY-105028 Related Classifications
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Keywords
- Tenidap
- 120210-48-2
- CP-66248
- CP66248
- CP 66248
- COX
- Lipoxygenase
- Chloride Channel
- Interleukin Related
- 5-lipoxygenase
- IL-1 receptor
- bone resorption
- cartilage degradation
- cyclooxygenase
- glycosaminoglycan synthesis
- leucocyte-endothelial adhesion
- metalloprotease
- monocyte differentiation
- proinflammatory cytokine
- Inhibitor
- inhibitor
- inhibit