WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H319769
CAS#: 940908-79-2
Description: Mericitabine, also known as RG7128 and R-7128, is a HCV polymerase inhibitor. RG7128 is also a prodrug of PSI-6130, which shows potent antiviral efficacy in patients infected with hepatitis C virus (HCV) genotypes 1, 2, or 3.
Hodoodo Cat#: H319769
Name: Mericitabine
CAS#: 940908-79-2
Chemical Formula: C18H26FN3O6
Exact Mass: 399.18
Molecular Weight: 399.419
Elemental Analysis: C, 54.13; H, 6.56; F, 4.76; N, 10.52; O, 24.03
Synonym: RG7128; RG-7128; RG 7128; R-7128; R7128; R 7128; PSI 6130 diisobutyrate; 3',5'-Diisobutyryl PSI 6130; Mericitabine.
IUPAC/Chemical Name: (2R,3R,4R,5R)-5-(4-amino-2-oxopyrimidin-1(2H)-yl)-4-fluoro-2-((isobutyryloxy)methyl)-4-methyltetrahydrofuran-3-yl isobutyrate
InChi Key: MLESJYFEMSJZLZ-MAAOGQSESA-N
InChi Code: InChI=1S/C18H26FN3O6/c1-9(2)14(23)26-8-11-13(28-15(24)10(3)4)18(5,19)16(27-11)22-7-6-12(20)21-17(22)25/h6-7,9-11,13,16H,8H2,1-5H3,(H2,20,21,25)/t11-,13-,16-,18-/m1/s1
SMILES Code: O=C(N=C(C=C1)N)N1[C@H](O2)[C@](C)(F)[C@H](OC(C(C)C)=O)[C@H]2COC(C(C)C)=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: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
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: | HCV NS5B polymerase. |
| In vitro activity: | TBD |
| In vivo activity: | In Arm A, the SVR24 rate in patients receiving 24 weeks of therapy was 37.9% (25/66); 63.6% (14/22) in G1b and 25.0% (11/44) in G1a patients. Virologic breakthrough and relapse were associated with danoprevir-resistant virus in most cases. The mericitabine-resistance mutation (NS5BS282T) was detected in two patients bearing dual resistant virus NS3 R155K/NS5B S282T and dual resistance mutation L159F/L320F in one patient. Treatment was safe and well tolerated. Mericitabine, danoprevir/r plus ribavirin for 24 weeks were safe and well tolerated. However, SVR rates were poor, achieving rates of only 25.0% in G1a and 63.6% in G1b patients. Reference: Gane EJ, Pockros PJ, Zeuzem S, Marcellin P, Shikhman A, Bernaards C, Zhou J, Yetzer ES, Ballester R, Dwyer C, Tong X, Nájera I, Bertasso A, Hammond J, Kindrick A, Morcos PN, Smith P, Stancic S, Shulman NS. Mericitabine and ritonavir-boosted danoprevir with or without ribavirin in treatment-naive HCV genotype 1 patients: INFORM-SVR study. Liver Int. 2015 Jan;35(1):79-89. doi: 10.1111/liv.12588. Epub 2014 Jun 19. PMID: 24814388. |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 100.0 | 250.36 |
The following data is based on the product molecular weight 399.42 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: | Gane EJ, Pockros PJ, Zeuzem S, Marcellin P, Shikhman A, Bernaards C, Zhou J, Yetzer ES, Ballester R, Dwyer C, Tong X, Nájera I, Bertasso A, Hammond J, Kindrick A, Morcos PN, Smith P, Stancic S, Shulman NS. Mericitabine and ritonavir-boosted danoprevir with or without ribavirin in treatment-naive HCV genotype 1 patients: INFORM-SVR study. Liver Int. 2015 Jan;35(1):79-89. doi: 10.1111/liv.12588. Epub 2014 Jun 19. PMID: 24814388. |
| In vitro protocol: | N/A |
| In vivo protocol: | Gane EJ, Pockros PJ, Zeuzem S, Marcellin P, Shikhman A, Bernaards C, Zhou J, Yetzer ES, Ballester R, Dwyer C, Tong X, Nájera I, Bertasso A, Hammond J, Kindrick A, Morcos PN, Smith P, Stancic S, Shulman NS. Mericitabine and ritonavir-boosted danoprevir with or without ribavirin in treatment-naive HCV genotype 1 patients: INFORM-SVR study. Liver Int. 2015 Jan;35(1):79-89. doi: 10.1111/liv.12588. Epub 2014 Jun 19. PMID: 24814388. |
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3: Canini L, Guedj J, Chatterjee A, Lemenuel-Diot A, Smith PF, Perelson AS. Modelling the interaction between danoprevir and mericitabine in the treatment of chronic HCV infection. Antivir Ther. 2015 Nov 10. doi: 10.3851/IMP3006. [Epub ahead of print] PubMed PMID: 26555159.
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