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MedKoo Cat#: 555327 | Name: RG7834 R-isomer
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

RG7834 R-isomer, also known as RO0321, is an enantiomer of RG7834 and a negative control for RG7834. RG7834 R-isomer has R-configuration with CAS#2072057-18-0. RG7834 is a novel oral HBV viral gene expression inhibitor that 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.

Chemical Structure

RG7834 R-isomer
RG7834 R-isomer
CAS#2072057-18-0 (R-isomer)

Theoretical Analysis

MedKoo Cat#: 555327

Name: RG7834 R-isomer

CAS#: 2072057-18-0 (R-isomer)

Chemical Formula: C22H27NO6

Exact Mass: 401.1838

Molecular Weight: 401.46

Elemental Analysis: C, 65.82; H, 6.78; N, 3.49; O, 23.91

Price and Availability

Size Price Availability Quantity
10mg USD 150.00 Ready to ship
25mg USD 330.00 Ready to ship
50mg USD 550.00 Ready to ship
100mg USD 950.00 Ready to ship
200mg USD 1,850.00 Ready to ship
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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)
Synonym
RG7834 R-isomer; RG 7834 R-isomer; RG-7834 R-isomer; RO7020322 R-isomer; RO 7020322 R-isomer; RO-7020322 R-isomer; RO0321; RO-0321; RO 0321;
IUPAC/Chemical Name
(6R)-6-Isopropyl-10-methoxy-9-(3-methoxypropoxy)-2-oxo-6,7-dihydrobenzo[a]quinolizine-3-carboxylic acid
InChi Key
KBXLMOYQNDMHQT-QGZVFWFLSA-N
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-/m1/s1
SMILES Code
O=C(C1=CN2[C@@H](C(C)C)CC3=CC(OCCCOC)=C(OC)C=C3C2=CC1=O)O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>3 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Biological target:
RG7834 is a highly selective and orally bioavailable HBV inhibitor, 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.
In vitro activity:
In cells expressing HBV mRNA, both PAPD5/7 were found to be physically associated with the viral RNA, and the polyadenylating activities of PAPD5/7 were susceptible to RG7834 repression in a biochemical assay. Reference: Antimicrob Agents Chemother. 2020 Dec 16;65(1):e00640-20. https://pubmed.ncbi.nlm.nih.gov/33046485/
In vivo activity:
When human blood stem cells engineered to carry dyskeratosis congenita (DC)-causing PARN mutations were xenotransplanted into immunodeficient mice, oral treatment with RG7834 rescued TERC 3' end maturation and telomere length. These findings could help develop systemic telomere therapeutics to counteract stem cell exhaustion in DC, pulmonary fibrosis, and possibly other aging-related diseases. Reference: Cell Stem Cell. 2020 Jun 4;26(6):896-909.e8. https://pubmed.ncbi.nlm.nih.gov/32320679/

Preparing Stock Solutions

The following data is based on the product molecular weight 401.46 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Sun L, Zhang F, Guo F, Liu F, Kulsuptrakul J, Puschnik A, Gao M, Rijnbrand R, Sofia M, Block T, Zhou T. The Dihydroquinolizinone Compound RG7834 Inhibits the Polyadenylase Function of PAPD5 and PAPD7 and Accelerates the Degradation of Matured Hepatitis B Virus Surface Protein mRNA. Antimicrob Agents Chemother. 2020 Dec 16;65(1):e00640-20. doi: 10.1128/AAC.00640-20. PMID: 33046485; PMCID: PMC7927841. 2. Mueller H, Wildum S, Luangsay S, Walther J, Lopez A, Tropberger P, Ottaviani G, Lu W, Parrott NJ, Zhang JD, Schmucki R, Racek T, Hoflack JC, Kueng E, Point F, Zhou X, Steiner G, Lütgehetmann M, Rapp G, Volz T, Dandri M, Yang S, Young JAT, Javanbakht H. A novel orally available small molecule that inhibits hepatitis B virus expression. J Hepatol. 2018 Mar;68(3):412-420. doi: 10.1016/j.jhep.2017.10.014. Epub 2017 Oct 25. PMID: 29079285. 3. Bopst M, Dinklo T, Funk J, Greiter-Wilke A, Lenz B, Kustermann S, Jiang T, Xie J. Unexpected neurotoxicity in chronic toxicity studies with a HBV viral expression inhibitor. Regul Toxicol Pharmacol. 2023 Jun;141:105407. doi: 10.1016/j.yrtph.2023.105407. Epub 2023 May 2. PMID: 37141985. 4. Nagpal N, Wang J, Zeng J, Lo E, Moon DH, Luk K, Braun RO, Burroughs LM, Keel SB, Reilly C, Lindsley RC, Wolfe SA, Tai AK, Cahan P, Bauer DE, Fong YW, Agarwal S. Small-Molecule PAPD5 Inhibitors Restore Telomerase Activity in Patient Stem Cells. Cell Stem Cell. 2020 Jun 4;26(6):896-909.e8. doi: 10.1016/j.stem.2020.03.016. Epub 2020 Apr 21. PMID: 32320679; PMCID: PMC7275922.
In vitro protocol:
1. Sun L, Zhang F, Guo F, Liu F, Kulsuptrakul J, Puschnik A, Gao M, Rijnbrand R, Sofia M, Block T, Zhou T. The Dihydroquinolizinone Compound RG7834 Inhibits the Polyadenylase Function of PAPD5 and PAPD7 and Accelerates the Degradation of Matured Hepatitis B Virus Surface Protein mRNA. Antimicrob Agents Chemother. 2020 Dec 16;65(1):e00640-20. doi: 10.1128/AAC.00640-20. PMID: 33046485; PMCID: PMC7927841. 2. Mueller H, Wildum S, Luangsay S, Walther J, Lopez A, Tropberger P, Ottaviani G, Lu W, Parrott NJ, Zhang JD, Schmucki R, Racek T, Hoflack JC, Kueng E, Point F, Zhou X, Steiner G, Lütgehetmann M, Rapp G, Volz T, Dandri M, Yang S, Young JAT, Javanbakht H. A novel orally available small molecule that inhibits hepatitis B virus expression. J Hepatol. 2018 Mar;68(3):412-420. doi: 10.1016/j.jhep.2017.10.014. Epub 2017 Oct 25. PMID: 29079285.
In vivo protocol:
1. Bopst M, Dinklo T, Funk J, Greiter-Wilke A, Lenz B, Kustermann S, Jiang T, Xie J. Unexpected neurotoxicity in chronic toxicity studies with a HBV viral expression inhibitor. Regul Toxicol Pharmacol. 2023 Jun;141:105407. doi: 10.1016/j.yrtph.2023.105407. Epub 2023 May 2. PMID: 37141985. 2. Nagpal N, Wang J, Zeng J, Lo E, Moon DH, Luk K, Braun RO, Burroughs LM, Keel SB, Reilly C, Lindsley RC, Wolfe SA, Tai AK, Cahan P, Bauer DE, Fong YW, Agarwal S. Small-Molecule PAPD5 Inhibitors Restore Telomerase Activity in Patient Stem Cells. Cell Stem Cell. 2020 Jun 4;26(6):896-909.e8. doi: 10.1016/j.stem.2020.03.016. Epub 2020 Apr 21. PMID: 32320679; PMCID: PMC7275922.
1: Mueller H, Lopez A, Tropberger P, Wildum S, Schmaler J, Pedersen L, Han X, Wang Y, Ottosen S, Yang S, Young JAT, Javanbakht H. PAPD5/7 Are Host Factors That Are Required for Hepatitis B Virus RNA Stabilization. Hepatology. 2019 Apr;69(4):1398-1411. doi: 10.1002/hep.30329. Epub 2019 Mar 1. PubMed PMID: 30365161. 2: Han X, Zhou C, Jiang M, Wang Y, Wang J, Cheng Z, Wang M, Liu Y, Liang C, Wang J, Wang Z, Weikert R, Lv W, Xie J, Yu X, Zhou X, Luangsay S, Shen HC, Mayweg AV, Javanbakht H, Yang S. Discovery of RG7834: The First-in-Class Selective and Orally Available Small Molecule Hepatitis B Virus Expression Inhibitor with Novel Mechanism of Action. J Med Chem. 2018 Dec 13;61(23):10619-10634. doi: 10.1021/acs.jmedchem.8b01245. Epub 2018 Oct 17. PubMed PMID: 30286292. 3: Mueller H, Wildum S, Luangsay S, Walther J, Lopez A, Tropberger P, Ottaviani G, Lu W, Parrott NJ, Zhang JD, Schmucki R, Racek T, Hoflack JC, Kueng E, Point F, Zhou X, Steiner G, Lütgehetmann M, Rapp G, Volz T, Dandri M, Yang S, Young JAT, Javanbakht H. A novel orally available small molecule that inhibits hepatitis B virus expression. J Hepatol. 2018 Mar;68(3):412-420. doi: 10.1016/j.jhep.2017.10.014. Epub 2017 Oct 25. PubMed PMID: 29079285.

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