ALG-001075
Based on 1 Customer Validation
ALG-001075, a capsid assembly modulator (CAM), is an orally active HBV inhibitor. ALG-001075 effectively blocks not only HBV DNA production but also extracellular HBsAg/HBeAg and intracellular HBV RNA in primary human hepatocytes. ALG-001075 shows pronounced reductions of circulating HBV DNA in the AAV-HBV mouse model. ALG-001075 can be used for the study of Chronic hepatitis B (CHB).
For research use only. We do not sell to patients.
- Purity : 98.83%
- CAS No.: 2495324-66-6
- Formula: C22H19FN4O4
- Molecular Weight:422.41
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Storage:Powder -20°C, 3 years , 4°C, 2 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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
ALG-001075 (Compound 10) (0.01-1000 nM) inhibits HBV DNA production in HepG2.117cells with an EC50 of 0.63 nM and an EC90 of 3.17 nM[1]. ALG-001075 (0.01-1000 nM) effectively blocks not only HBV DNA production (EC50 = 1.98 nM) but also extracellular HBsAg (EC50 = 70 nM), HBeAg (EC50 = 10.5 nM) and intracellular HBV RNA (EC50 = 54.7 nM) in primary human hepatocytes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
| Species | Dose | Route | CL | Vss | T1/2 | AUCinf | Tmax | Cmax | F |
|---|---|---|---|---|---|---|---|---|---|
| Cynomolgus Monkey[1] | 1 mg/kg | i.v. | 7.89 mL/min/kg | 0.89 L/kg | 1.85 h | 2235 ng·h/mL | / | / | / |
| Cynomolgus Monkey[1] | 5 mg/kg | p.o. | / | / | 14.4 h | 2189 ng·h/mL | 1.17 h | 490 ng/mL | 19.6 % |
| Dog[1] | 1 mg/kg | i.v. | 1.97 mL/min/kg | 1.03 L/kg | 6.38 h | 8519 ng·h/mL | / | / | / |
| Dog[1] | 5 mg/kg | p.o. | / | / | 7.83 h | 24494 ng·h/mL | 2.17 h | 1903 ng/mL | 57.5 % |
| Mice[1] | 1 mg/kg | i.v. | 12.0 mL/min/kg | 1.00 L/kg | 1.37 h | 1394 ng·h/mL | / | / | / |
| Mice[1] | 5 mg/kg | p.o. | / | / | 1.55 h | 7987 ng·h/mL | 1.00 h | 2287 ng/mL | 115 % |
| Rat[1] | 1 mg/kg | i.v. | 6.09 mL/min/kg | 0.50 L/kg | 1.64 h | 2778 ng·h/mL | / | / | / |
| Rat[1] | 5 mg/kg | p.o. | / | / | 2.17 h | 8723 ng·h/mL | 1.67 h | 1833 ng/mL | 62.8 % |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male 5-6 weeks old C57BL/6 mice adeno-associated virus (AAV) HBV[1]
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Dosage:15, 50 mg/kg
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Administration:p.o. twice daily for 56 days
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Result:Showed pronounced reductions of circulating HBV DNA in the AAV-HBV mouse model.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2495324-66-6
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Appearance Solid
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Molecular Weight 422.41
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Formula C22H19FN4O4
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SMILES
N#CC1=CC(NC(C2=C(C)C(C(C(NC3(COC3)C#C)=O)=O)=C(C)N2C)=O)=CC=C1F
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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 : 70 mg/mL (165.72 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)
Protocols
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How to Choose the Right Model Animal
Choosing the right model animal is a validity-driven decision in which the species, strain, sex, age, genetic background, disease-induction method, outcome measures, and welfare burden must match the scientific question rather than laboratory tradition or convenience. A model should be selected by judging face validity, construct validity, and predictive validity: whether it resembles the human phenotype, whether it reproduces relevant mechanisms, and whether results are likely to predict human biology or treatment response. Animal studies often fail to translate because of species differences, weak disease resemblance, poor experimental design, inadequate reporting, publication bias, and underuse of randomization, blinding, and sample-size justification. Unresolved questions include how to rank competing models objectively, how much human-disease complexity must be reproduced for a given objective, and when non-animal systems such as organoids, ex vivo tissue, or computational models
Purity & Documentation
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Data Sheet (274 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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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 | 2.3674 mL | 11.8368 mL | 23.6737 mL | 59.1842 mL |
| 5 mM | 0.4735 mL | 2.3674 mL | 4.7347 mL | 11.8368 mL | |
| 10 mM | 0.2367 mL | 1.1837 mL | 2.3674 mL | 5.9184 mL | |
| 15 mM | 0.1578 mL | 0.7891 mL | 1.5782 mL | 3.9456 mL | |
| 20 mM | 0.1184 mL | 0.5918 mL | 1.1837 mL | 2.9592 mL | |
| 25 mM | 0.0947 mL | 0.4735 mL | 0.9469 mL | 2.3674 mL | |
| 30 mM | 0.0789 mL | 0.3946 mL | 0.7891 mL | 1.9728 mL | |
| 40 mM | 0.0592 mL | 0.2959 mL | 0.5918 mL | 1.4796 mL | |
| 50 mM | 0.0473 mL | 0.2367 mL | 0.4735 mL | 1.1837 mL | |
| 60 mM | 0.0395 mL | 0.1973 mL | 0.3946 mL | 0.9864 mL | |
| 80 mM | 0.0296 mL | 0.1480 mL | 0.2959 mL | 0.7398 mL | |
| 100 mM | 0.0237 mL | 0.1184 mL | 0.2367 mL | 0.5918 mL |
ALG-001075 Related Classifications
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