Org 43553
Based on 1 Customer Validation
Org 43553 is an orally active and low molecular weight (LMW) luteinizing hormone receptor (LH-R) agonist. Org 43553 shows agonistic activity to human LH and FSH receptors with EC50 values of 3.7 and 110 nM, respectively. Org 43553 can be used for the research of endocrine.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.30%
- No. CAS: 501444-88-8
- Fòrmula: C24H30N6O3S2
- Peso molecular:514.66
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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
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Org 43553 (0-3 μM; 4 h) shows agonistic activity to human LH, FSH and TSH receptors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CHO and HEK293 cell lines
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Concentration:0-3 μM
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Incubation Time:4 hours
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Result:Exhibited agonistic activity to human LH, FSH and TSH receptors with EC50 values of 3.7 nM, 110 nM and ＞3 μM, respectively. Showed no CRF1-R agonistic effect in CHO-CRF1 cell line.
| Rats IV 5 mg/kg |
Rats PO 50 mg/kg |
Dogs IV 12.5 mg/kg |
Dogs PO 50 mg/kg |
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| AUC (h mg/L) | 6.9±0.4 | 55.1±2.0 | 9.1±3.1 | 16.1±1.2 |
| Tmax (h) | 3.3±3.3 | 0.9±1.0 | ||
| Cmax (mg/L) | 5.1±2.3 | 3.8±0.9 | 8.7±2.2 | 4.1±1.7 |
| t1/2 (h) | 3.4±1.3 | 4.5±1.8 | 1.5±1.3 | 3.5±2.5 |
| CL (L/h) | 0.7±0.1 | 0.9±0.1 | 1.5±0.6 | 3.1±0.2 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Immature Humegon primed mice and GnRH-antagonist-treated female Orga rats [1]
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Dosage:5-50 mg/kg
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Administration:Oral gavage; 50 mg/kg once
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Result:Triggered ovulation in 80% of the animals, with a mean number of 9.3 ova per ovulating animals. Dose-dependently increased the number of ovulated oocytes in the ampulla, and showed a similar ovulation number at a dose of 25 mg/kg compared with hCG group.
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Animal Model:Adult male rats[1]
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Dosage:10, 50 and 250 mg/kg
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Administration:Oral gavage; 10-250 mg/kg once
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Result:Significantly increased testosterone production in male rats and at a dose of 250 mg/kg the testosterone levels were very similar to those induced by hCG.
Chemical Information
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No. CAS 501444-88-8
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Appearance Solid
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Peso molecular 514.66
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Fòrmula C24H30N6O3S2
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Color Light yellow to yellow
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SMILES
O=C(C1=C(N)C2=C(C3=CC=CC(NC(CN4CCOCC4)=O)=C3)N=C(SC)N=C2S1)NC(C)(C)C
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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 (194.30 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)
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 (4.86 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.86 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 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 (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 1.9430 mL | 9.7152 mL | 19.4303 mL | 48.5758 mL |
| 5 mM | 0.3886 mL | 1.9430 mL | 3.8861 mL | 9.7152 mL | |
| 10 mM | 0.1943 mL | 0.9715 mL | 1.9430 mL | 4.8576 mL | |
| 15 mM | 0.1295 mL | 0.6477 mL | 1.2954 mL | 3.2384 mL | |
| 20 mM | 0.0972 mL | 0.4858 mL | 0.9715 mL | 2.4288 mL | |
| 25 mM | 0.0777 mL | 0.3886 mL | 0.7772 mL | 1.9430 mL | |
| 30 mM | 0.0648 mL | 0.3238 mL | 0.6477 mL | 1.6192 mL | |
| 40 mM | 0.0486 mL | 0.2429 mL | 0.4858 mL | 1.2144 mL | |
| 50 mM | 0.0389 mL | 0.1943 mL | 0.3886 mL | 0.9715 mL | |
| 60 mM | 0.0324 mL | 0.1619 mL | 0.3238 mL | 0.8096 mL | |
| 80 mM | 0.0243 mL | 0.1214 mL | 0.2429 mL | 0.6072 mL | |
| 100 mM | 0.0194 mL | 0.0972 mL | 0.1943 mL | 0.4858 mL |
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