RG7834 R-isomer | RO0321 | CAS#2072057-18-0 | HBV expression inhibitor

RG7834 R-isomer
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 555327

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

Description: 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

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

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 555327
Name: RG7834 R-isomer
CAS#: 2072057-18-0 (R-isomer)
Chemical Formula: C22H27NO6
Exact Mass: 401.18
Molecular Weight: 401.459
Elemental Analysis: C, 65.82; H, 6.78; N, 3.49; O, 23.91

Price and Availability

Size	Price	Availability
10mg	USD 150	Ready to ship
25mg	USD 330	Ready to ship
50mg	USD 550	Ready to ship
100mg	USD 950	Ready to ship
200mg	USD 1850	Ready to ship
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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:

Product Data:

Product Data

Certificate of Analysis:

View CoA: current batch, Lot#YXM81227

QC Data:

View QC data: current batch, Lot#YXM81227

Safety Data Sheet (SDS):

View Safety Data Sheet (SDS)

Instruction:

View handling instruction

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.

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.

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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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RG7834 R-isomer new featured