Org 274179-0
Based on 1 Customer Validation
Org 274179-0 is a low-molecular-weight allosteric thyrotropin receptor (TSH Receptor) antagonist with equipotent follicle-stimulating hormone receptor antagonistic activity and selectivity for the luteinizing hormone receptor. Org 274179-0 binds to the transmembrane domain of the thyrotropin receptor, stabilizes the receptor's inactive state, and blocks agonist-induced and constitutive signaling through the adenylyl cyclase/cAMP and phospholipase C pathways. Org 274179-0 can be used for research on Graves' disease and Graves' ophthalmopathy.
For research use only. We do not sell to patients.
- Purity: 98.63%
- CAS No.: 1421683-12-6
- Formula: C28H27F3N2O2
- Molecular Weight:480.52
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Storage: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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
In Vitro
Org 274179-0 (4 h) acts as a full antagonist of bTSH-, hTSH-, and M22-stimulated CRE-luciferase activity in CHO.hTSH receptor cells with nanomolar potencies[1].
Org 274179-0 (1 h) is a potent full antagonist of bTSH-, hTSH-, and M22-induced cAMP synthesis in CHO.hTSH receptor cells, with IC50 values in the low nanomolar range[1].
Org 274179-0 (60 min) fully antagonizes bTSH- and M22-stimulated cAMP production in rat FRTL-5 thyroid cells with low nanomolar potencies[1].
Org 274179-0 (4 h) is a full antagonist at the human FSH receptor with an IC50 of 17 nM, and acts as a partial agonist at the human LH receptor with micromolar potency[1].
Org 274179-0 (60 min) is a potent full antagonist of TSH- and M22-stimulated PLC activation in CHO.hTSH receptor cells with low nanomolar IC50 values[1].
Org 274179-0 (60 min) potently inhibits rhTSH- and M22-induced cAMP production in CHO.hTSHR cells, with IC50 values of 11 nM and 4 nM respectively, and achieves complete blockade at 1 μM[2].
Org 274179-0 (0.1 nM-1 μM; 6 h) potently inhibits rhTSH-, GD-IgG-, and M22-induced cAMP production in differentiated GO patient orbital fibroblasts with IC50 values of 2.6 nM, 0.9 nM, and 0.5 nM respectively, with complete blockade at 1 μM, and does not affect Forskolin (HY-15371)-stimulated cAMP production[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1421683-12-6
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Appearance Solid
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Molecular Weight 480.52
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Formula C28H27F3N2O2
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Color Light yellow to yellow
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SMILES
C[C@]1(C2=CC=CC=C2)C3=CC(NC(CCC4=CC(C(F)(F)F)=CC=C4)=O)=CC=C3N(CC1)C(C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (208.11 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 (5.20 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
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 | 2.0811 mL | 10.4054 mL | 20.8108 mL | 52.0270 mL |
| 5 mM | 0.4162 mL | 2.0811 mL | 4.1622 mL | 10.4054 mL | |
| 10 mM | 0.2081 mL | 1.0405 mL | 2.0811 mL | 5.2027 mL | |
| 15 mM | 0.1387 mL | 0.6937 mL | 1.3874 mL | 3.4685 mL | |
| 20 mM | 0.1041 mL | 0.5203 mL | 1.0405 mL | 2.6013 mL | |
| 25 mM | 0.0832 mL | 0.4162 mL | 0.8324 mL | 2.0811 mL | |
| 30 mM | 0.0694 mL | 0.3468 mL | 0.6937 mL | 1.7342 mL | |
| 40 mM | 0.0520 mL | 0.2601 mL | 0.5203 mL | 1.3007 mL | |
| 50 mM | 0.0416 mL | 0.2081 mL | 0.4162 mL | 1.0405 mL | |
| 60 mM | 0.0347 mL | 0.1734 mL | 0.3468 mL | 0.8671 mL | |
| 80 mM | 0.0260 mL | 0.1301 mL | 0.2601 mL | 0.6503 mL | |
| 100 mM | 0.0208 mL | 0.1041 mL | 0.2081 mL | 0.5203 mL |
Org 274179-0 Related Classifications
HY-153213 Related Classifications
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Keywords
- Org 274179-0
- 1421683-12-6
- TSH Receptor
- GnRH Receptor
- Phospholipase
- phospholipase C pathways
- follicle-stimulating hormone receptor
- luteinizing hormone receptor
- rat FRTL-5 thyroid cells
- Graves’ ophthalmopathy
- adenylyl cyclase/cAMP
- CHO.hTSH receptor cells
- thyroid-stimulating hormone receptor
- Graves’ disease
- differentiated orbital fibroblasts
- Inhibitor
- inhibitor
- inhibit