LP-922056
Based on 1 publication(s) in Google Scholar
LP-922056 is an orally active, highly potent Notum Pectinacetylesterase inhibitor with EC50s of 21 nM, 55 nM in human and mouse cellular assay, respectively. LP-922056 significantly increases midshaft femur cortical bone thickness in mice and rats.
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- Pureza: 99.63%
- No. CAS: 1365060-22-5
- Fòrmula: C11H9ClN2O2S2
- Peso molecular:300.78
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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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) LP-922056
More
Actividad biológica
EC50: 21 nM (human Notum Pectinacetylesterase) and 55 nM (mouse Notum Pectinacetylesterase)[1]
? LP-922056 (10 mg/kg; orally) achieves high Cmax (129 μM) and AUC (1533 μM?h)[1].
? LP-922056 (10?mg/kg; daily diet; for 4 weeks) increases cortical bone thickness and strength in midshaft femur, bone mass in the femoral neck and vertebral body cortical shell in Twelve-week-old male mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:F1 male hybrid (129xC57) mice at 8.7 weeks of age[1]
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Dosage:3, 10, 30 mg/kg
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Administration:Oral gavage; daily; for 25 days
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Result:Caused an increase in cortical bone thickness at all doses.
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Animal Model:Mouse[1]
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Dosage:10 mg/kg (Pharmacokinetic Analysis)
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Administration:Orally
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Result:Achieved high Cmax (129 μM) and AUC (1533 μM•h) while has low clearance (0.49 mL/min•kg) and volume of distribution (0.13 L/kg).
Chemical Information
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No. CAS 1365060-22-5
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Appearance Solid
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Peso molecular 300.78
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Fòrmula C11H9ClN2O2S2
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Color White to light yellow
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SMILES
O=C(O)CSC1=C2C(C(C3CC3)=C(Cl)S2)=NC=N1
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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
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Stem Cell
VIPR1 acts as an enteric neural checkpoint that suppresses intestinal stem cell-driven epithelial regeneration and exacerbates colitis. [Abstract]2026 Mar 5;33(3):502-516.e7. PMID: 41734764
Solvente y solubilidad
DMSO : 100 mg/mL (332.47 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: ≥ 2.08 mg/mL (6.92 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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 (277 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
[1]. James E Tarver Jr, et al. Stimulation of cortical bone formation with thienopyrimidine based inhibitors of Notum Pectinacetylesterase. Bioorg Med Chem Lett. 2016 Mar 15;26(6):1525-1528. [Content Brief]
[2]. Robert Brommage, et al. NOTUM inhibition increases endocortical bone formation and bone strength. Bone Res. 2019 Jan 8;7:2. [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 | 3.3247 mL | 16.6234 mL | 33.2469 mL | 83.1172 mL |
| 5 mM | 0.6649 mL | 3.3247 mL | 6.6494 mL | 16.6234 mL | |
| 10 mM | 0.3325 mL | 1.6623 mL | 3.3247 mL | 8.3117 mL | |
| 15 mM | 0.2216 mL | 1.1082 mL | 2.2165 mL | 5.5411 mL | |
| 20 mM | 0.1662 mL | 0.8312 mL | 1.6623 mL | 4.1559 mL | |
| 25 mM | 0.1330 mL | 0.6649 mL | 1.3299 mL | 3.3247 mL | |
| 30 mM | 0.1108 mL | 0.5541 mL | 1.1082 mL | 2.7706 mL | |
| 40 mM | 0.0831 mL | 0.4156 mL | 0.8312 mL | 2.0779 mL | |
| 50 mM | 0.0665 mL | 0.3325 mL | 0.6649 mL | 1.6623 mL | |
| 60 mM | 0.0554 mL | 0.2771 mL | 0.5541 mL | 1.3853 mL | |
| 80 mM | 0.0416 mL | 0.2078 mL | 0.4156 mL | 1.0390 mL | |
| 100 mM | 0.0332 mL | 0.1662 mL | 0.3325 mL | 0.8312 mL |
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