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).
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 98.83%
- CAS No.: 2495324-66-6
- 화학식: C22H19FN4O4
- 분자량:422.41
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보관: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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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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.
| 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 % |
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.
| 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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분자량 422.41
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
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)
순도&문서
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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
HY-177022 Related Classifications
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