Rovafovir etalafenamide
Based on 1 Customer Validation
Rovafovir etalafenamide (GS-9131), a proagent of the adenosine nucleotide analogue GS-9148, is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Rovafovir etalafenamide is potent and active against a variety of NRTI mutants, and shows potent anti-HIV-1 activity.
For research use only. We do not sell to patients.
- Purity: 99.85%
- CAS No.: 912809-27-9
- Formula: C21H24FN6O6P
- Molecular Weight:506.42
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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HIV-2 |
HIV-1 |
reverse transcriptase |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MT2 | CC50 |
74000 nM
Compound: 18v
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Cytotoxicity against human MT2 cells after 5 days by XTT assay
Cytotoxicity against human MT2 cells after 5 days by XTT assay
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[PMID: 20409721] |
| MT2 | EC50 |
96 nM
Compound: 18v
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Antiviral activity against HIV1 3B infected in human MT2 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by XTT assay
Antiviral activity against HIV1 3B infected in human MT2 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by XTT assay
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[PMID: 20409721] |
Rovafovir etalafenamide (GS-9131) shows anti-HIV-1 activity in PBMCs (EC50=3.7 nM) and MT-2 cells (EC50=150 nM). Rovafovir etalafenamide is also a potent HIV-1 inhibitor in a single-cycle infection assay with primary CD4+ T lymphocytes (EC50=24 nM). Rovafovir etalafenamide inhibits different subtypes of HIV-1 (UG-92-031 subtype A, B940374 subtype B, LJM subtype B, BR-92-025 subtype C, and UG-92-024 subtype D) clinical isolates in PBMCs with EC50s ranging from 23 to 68 nM. Rovafovir etalafenamide inhibits HIV-2 isolated in MT-2 cells (CDD77618 subtype A, CDD310248 subtype A, and CDD310319 subtype B) with EC50s ranging from 39 to 650 nM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 912809-27-9
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Appearance Solid
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Molecular Weight 506.42
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Formula C21H24FN6O6P
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Color White to off-white
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SMILES
FC([C@](O1)([H])N2C3=NC=NC(N)=C3N=C2)=C[C@H]1OC[P@](OC4=CC=CC=C4)(N[C@@H](C)C(OCC)=O)=O
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Synonyms
GS-9131
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Purity & Documentation
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Data Sheet (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Mackman RL, et al. Discovery of GS-9131: Design, synthesis and optimization of amidate prodrugs of the novel nucleoside phosphonate HIV reverse transcriptase (RT) inhibitor GS-9148. Bioorg Med Chem. 2010;18(10):3606‐3617. [Content Brief]
[2]. Rai MA, Pannek S, Fichtenbaum CJ. Emerging reverse transcriptase inhibitors for HIV-1 infection. Expert Opin Emerg Drugs. 2018;23(2):149‐157. [Content Brief]
[3]. Cihlar T, et al. Design and profiling of GS-9148, a novel nucleotide analog active against nucleoside-resistant variants of human immunodeficiency virus type 1, and its orally bioavailable phosphonoamidate prodrug, GS-9131. Antimicrob Agents Chemother. 2008;52(2):655‐665. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Rovafovir etalafenamide Related Classifications
HY-19851 Related Classifications
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