Linvencorvir
Based on 1 Customer Validation
Linvencorvir (RG7907) is an orally active Hepatitis B virus core protein allosteric modulator. Linvencorvir induces Apoptosis. Linvencorvir has antiviral activity against HBV.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.14%
- No. CAS: 1808248-05-6
- Fòrmula: C29H35FN6O5S
- Peso molecular:598.69
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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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Anti-Infection Compound Library
HY-L002
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Apoptosis Compound Library
HY-L003
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Immunology/Inflammation Compound Library
HY-L007
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Clinical Compound Library
HY-L026
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Antiviral Compound Library
HY-L027
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Drug Repurposing Compound Library
HY-L035
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Covalent Screening Library
HY-L036
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Orally Active Compound Library
HY-L061
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HY-L138
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Cell Death Library
HY-L162
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Allosteric Modulators (AMs) Compound Library
HY-L170
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MCE Bioactive Compound Library
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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High-Throughput Bioactive Compound Library
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 2.2.15 | EC50 |
0.006 μM
Compound: 39; RG7907
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Antiviral activity against HBV stably transfected in human HepG2.2.15 cells assessed as reduction of HBV DNA replication incubated for 5 days by q-PCR analysis
Antiviral activity against HBV stably transfected in human HepG2.2.15 cells assessed as reduction of HBV DNA replication incubated for 5 days by q-PCR analysis
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[PMID: 36896968] |
Linvencorvir (20 mg/kg; p.o.; once daily; 70 days) significantly reduces serum HBsAg, HBeAg, and liver AAV-HBV episome levels in the adeno-associated virus-hepatitis B virus (AAV-HBV) mouse model, while inducing hepatocyte apoptosis and proliferation, accompanied by a transient increase in ALT[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice (5-6 weeks old) injected with AAV-HBV to establish the AAV-HBV mouse model[4]
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Dosage:20 mg/kg
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Administration:Oral gavage (p.o.), once daily for 70 days
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Result:Rapidly reduced serum HBV DNA levels by ~3 log10 IU/mL by day 7.
Decreased serum HBsAg and HBeAg by 1.5 and 1.2 log10 IU/mL respectively, but with a delay compared to HBV DNA decline.
Significantly reduced the number of HBc-positive and HBsAg-positive hepatocytes on day 35, and further decreased them on day 70.
Significantly decreased intrahepatic HBV pgRNA on day 35 and further decreased it on day 70.
Reduced the amount of AAV-HBV DNA in the liver.
Increased apoptotic cells at days 14 and 35.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1808248-05-6
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Appearance Solid
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Peso molecular 598.69
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Fòrmula C29H35FN6O5S
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Color Light yellow to yellow
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SMILES
CCOC(C1=C(CN2C[C@]3([H])N(C(N(C3)CC(C)(C)C(O)=O)=O)CC2)N=C(C4=NC=CS4)N[C@@]1([H])C5=C(C(F)=CC=C5)C)=O
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Synonyms
RG7907; RO7049389
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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 : 62.5 mg/mL (104.39 mM; ultrasonic and warming and heat to 60°C; 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)
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Vanrusselt H, et al. Novel non-HAP class A HBV capsid assembly modulators have distinct in vitro and in vivo profiles. J Virol. 2023 Oct 31;97(10):e0072223. [Content Brief]
[2]. Zhang Y, et al. Evaluation of the drug disposition of RO7049389 with in vitro data and human mass balance supported by physiologically based pharmacokinetic modelling. Br J Clin Pharmacol. 2023 Oct;89(10):3079-3091. [Content Brief]
[3]. Zhang W, et al. Discovery of Linvencorvir (RG7907), a Hepatitis B Virus Core Protein Allosteric Modulator, for the Treatment of Chronic HBV Infection. J Med Chem. 2023 Mar 23;66(6):4253-4270. [Content Brief]
[4]. Kum DB, et al. Class A capsid assembly modulator RG7907 clears HBV-infected hepatocytes through core-dependent hepatocyte death and proliferation. Hepatology. 2023 Oct 1;78(4):1252-1265. [Content Brief]
[5]. Feng S, et al. A Five-in-One First-in-Human Study To Assess Safety, Tolerability, and Pharmacokinetics of RO7049389, an Inhibitor of Hepatitis B Virus Capsid Assembly, after Single and Multiple Ascending Doses in Healthy Participants. Antimicrob Agents Chemother. 2020 Oct 20;64(11):e01323-20. [Content Brief]
[6]. Yang L, et al. Treatment of Chronic Hepatitis B Virus Infection Using Small Molecule Modulators of Nucleocapsid Assembly: Recent Advances and Perspectives. ACS Infect Dis. 2019 May 10;5(5):713-724. [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 | 1.6703 mL | 8.3516 mL | 16.7031 mL | 41.7578 mL |
| 5 mM | 0.3341 mL | 1.6703 mL | 3.3406 mL | 8.3516 mL | |
| 10 mM | 0.1670 mL | 0.8352 mL | 1.6703 mL | 4.1758 mL | |
| 15 mM | 0.1114 mL | 0.5568 mL | 1.1135 mL | 2.7839 mL | |
| 20 mM | 0.0835 mL | 0.4176 mL | 0.8352 mL | 2.0879 mL | |
| 25 mM | 0.0668 mL | 0.3341 mL | 0.6681 mL | 1.6703 mL | |
| 30 mM | 0.0557 mL | 0.2784 mL | 0.5568 mL | 1.3919 mL | |
| 40 mM | 0.0418 mL | 0.2088 mL | 0.4176 mL | 1.0439 mL | |
| 50 mM | 0.0334 mL | 0.1670 mL | 0.3341 mL | 0.8352 mL | |
| 60 mM | 0.0278 mL | 0.1392 mL | 0.2784 mL | 0.6960 mL | |
| 80 mM | 0.0209 mL | 0.1044 mL | 0.2088 mL | 0.5220 mL | |
| 100 mM | 0.0167 mL | 0.0835 mL | 0.1670 mL | 0.4176 mL |
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