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Purity: ≥98%
RG7834 S-isomer, also known as RO 7020322 is the S-enantiomer of RG7834 (RO-7020322) which is a novel, potent and orally bioavailable inhibitor of HBV viral gene expression which blocks viral antigen and virion production. RG7834 is highly selective for HBV, and has a unique antiviral profile that is clearly differentiated from nucleos(t)ide analogues. RG7834 (also known as RO 7020322) is a novel, potent, highly selective and orally bioavailable HBV inhibitor which potently inhibits HBV antigens (both HBsAg and HBeAg) and HBV DNA, with IC50s of 2.8, 2.6, and 3.2 nM, respectively in dHepaRG Cells. RG7834 is a novel oral HBV viral gene expression inhibitor that blocks viral antigen and virion production. RG7834 has a unique antiviral profile that is clearly differentiated from nucleos(t)ide analogues.
Targets |
HBsAg(IC50: 2.8 nM);HBeAg(IC50: 2.6 nM);HBV DNA(IC50: 3.2 nM)
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ln Vitro |
With IC50s of 2.8, 2.6, and 3.2 nM, respectively, RG7834 ((S)-(+)-64) is a potent and highly selective oral bioavailable HBV inhibitor that potently inhibits HBV DNA and antigens (HBsAg and HBeAg) in dHepaRG Cells[1].
CYP3A4, CYP2D6, CYP2C9 (IC50s >50 μM), and the hERG channel are not inhibited by RG7834[1]. |
ln Vivo |
HBV-infected human liver chimeric uPA-SCID mice demonstrate anti-HBV efficacy in response to RG7834 (4 mg/kg, twice daily for 21 days)[1].
In mice, RG7834 (2, 14.5 mg/kg, p.o.) has a half-life of 4.9 hours and demonstrates good oral bioavailability[1]. |
Animal Protocol |
Animal Model: HBV-infected human liver chimeric uPA-SCID mice[1]
Dosage: 4 mg/kg Administration: Twice daily for 21 days Result:demonstrates good oral bioavailability[1]. reduced serum HBV DNA in mice by 0.6 log10 and lowered both HBsAg and HBeAg. |
References |
Molecular Formula |
C22H27NO6
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Molecular Weight |
401.452886819839
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Exact Mass |
401.18
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Elemental Analysis |
C, 65.82; H, 6.78; N, 3.49; O, 23.91
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CAS # |
2072057-17-9
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Related CAS # |
199482-36-3 (S-isomer hydrate);2072057-17-9 (S-isomer);2072057-18-0 (R-isomer);1802407-46-0 (racemic);
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Appearance |
White to off-white solid powder.
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SMILES |
O=C(C1=CN2[C@H](C(C)C)CC3=CC(OCCCOC)=C(OC)C=C3C2=CC1=O)O
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InChi Key |
KBXLMOYQNDMHQT-KRWDZBQOSA-N
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InChi Code |
InChI=1S/C22H27NO6/c1-13(2)17-8-14-9-21(29-7-5-6-27-3)20(28-4)10-15(14)18-11-19(24)16(22(25)26)12-23(17)18/h9-13,17H,5-8H2,1-4H3,(H,25,26)/t17-/m0/s1
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Chemical Name |
(6S)-6-Isopropyl-10-methoxy-9-(3-methoxypropoxy)-2-oxo-6,7-dihydrobenzo[a]quinolizine-3-carboxylic acid
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Synonyms |
RG7834; RG 7834; RG-7834; RO7020322; RO 7020322; RO-7020322
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~125 mg/mL (~311.37 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.87 mg/mL (7.15 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.18 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.18 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.08 mg/mL (5.18 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly. Solubility in Formulation 5: 5% DMSO+95% (20% SBE-β-CD in Saline): ≥ 2.87 mg/mL (7.15 mM) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4910 mL | 12.4549 mL | 24.9097 mL | |
5 mM | 0.4982 mL | 2.4910 mL | 4.9819 mL | |
10 mM | 0.2491 mL | 1.2455 mL | 2.4910 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.