Laroprovstat
Based on 1 publication(s) in Google Scholar
Laroprovstat (AZD0780) is an orall active PCSK9 inhibitor. PCSK9-IN-12 has bind affinity for PCSK9 with a Kd value of <200 nM. Laroprovstat binds to a pocket in the PCSK9 C-terminal domain and does not affect the PCSK9-LDL receptor (LDLR) interaction. Laroprovstat inhibits lysosomal trafficking of PSCK9-LDLR complexes and prevents PCSK9-induced LDLR degradation. Laroprovstat can be used for the research of hypercholesterolemia.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.93%
- CAS. Nr.: 2455427-91-3
- Formel: C20H20F2N6O2
- Molecular Weight:414.41
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Speicherung:Powder -20°C, 3 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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
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Publications Citing Use of MedChemExpress (MCE) Laroprovstat
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Biologische Aktivität
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 2455427-91-3
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Appearance Solid
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Molecular Weight 414.41
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Formel C20H20F2N6O2
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Color Off-white to light yellow
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SMILES
O=C1N(C=CC=C1)C2=CN=C(N[C@@H]3C[C@H](CC3)NC4=NC=C(OC(F)F)C=N4)C=C2
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Synonyms
AZD0780; PCSK9-IN-12
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 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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Metabolism
CADD-engineered peptide protacs efficiently target PCSK9 for hypercholesterolemia in vivo. [Abstract]2025 Dec 23:176:156485. PMID: 41448485
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (241.31 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (6.03 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 (6.03 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.
Reinheit & Dokumentation
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Data Sheet (272 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)
Verweise
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 |
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| DMSO | 1 mM | 2.4131 mL | 12.0653 mL | 24.1307 mL | 60.3267 mL |
| 5 mM | 0.4826 mL | 2.4131 mL | 4.8261 mL | 12.0653 mL | |
| 10 mM | 0.2413 mL | 1.2065 mL | 2.4131 mL | 6.0327 mL | |
| 15 mM | 0.1609 mL | 0.8044 mL | 1.6087 mL | 4.0218 mL | |
| 20 mM | 0.1207 mL | 0.6033 mL | 1.2065 mL | 3.0163 mL | |
| 25 mM | 0.0965 mL | 0.4826 mL | 0.9652 mL | 2.4131 mL | |
| 30 mM | 0.0804 mL | 0.4022 mL | 0.8044 mL | 2.0109 mL | |
| 40 mM | 0.0603 mL | 0.3016 mL | 0.6033 mL | 1.5082 mL | |
| 50 mM | 0.0483 mL | 0.2413 mL | 0.4826 mL | 1.2065 mL | |
| 60 mM | 0.0402 mL | 0.2011 mL | 0.4022 mL | 1.0054 mL | |
| 80 mM | 0.0302 mL | 0.1508 mL | 0.3016 mL | 0.7541 mL | |
| 100 mM | 0.0241 mL | 0.1207 mL | 0.2413 mL | 0.6033 mL |
Laroprovstat Related Classifications
HY-148673 Related Classifications
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