MLS8091
Based on 1 Customer Validation
MLS8091 is a highly selective inhibitor of the human cytomegalovirus (HCMV) helicase-primase complex with antiviral activity. MLS8091 inhibits HCMV replication during the early and late stages of the virus, and suppresses viral DNA replication as well as all HCMV viral proteins. MLS8091 inhibits guinea pig cytomegalovirus replication, and exerts an additive effect when combined with Letermovir (HY-15233). MLS8091 can be used in studies related to human cytomegalovirus infection.
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- Purity: 99.77%
- CAS No.: 848217-46-9
- 화학식: C21H16N4O2S2
- 분자량:420.51
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
MLS8091 (8-10 days) potently inhibits HCMV Towne strain, GCV-resistant HCMV Towne strain, and HCMV TB40 strain in human foreskin fibroblasts (HFFs), with EC50 values ranging from 0.26 to 0.39 μM, and shows no cytotoxicity at concentrations up to 250 μM[1].
MLS8091 exhibits specific anti-HCMV activity and does not inhibit the replication of HSV1, HSV2, MCMV or lytic EBV in relevant cell systems[1].
MLS8091 inhibits the replication of HCMV Towne in HFF from the early to late stages of the viral life cycle; in add-on assays, its timing of action overlaps with that of GCV, but it exhibits an earlier action effect in washout assays[1].
MLS8091 (0-10 μM; 72 h) reduces the expression of IE1, IE2, UL84, UL44 and pp65 proteins of HCMV Towne strain in human foreskin fibroblasts (HFFs)[1].
MLS8091 (1.5 μM; 0-120 hpi) significantly inhibits DNA replication of HCMV Towne strain in human foreskin fibroblasts (HFFs)[1].
MLS8091 (dose based on 2×EC50 value; 72 h, 8-10 days) exhibits additive to mild synergistic anti-human cytomegalovirus activity when combined with GCV or Letermovir (HY-15233) in human foreskin fibroblasts (HFFs), with a Bliss coefficient of 1.3 for both combinations[1].
MLS8091 potently inhibits the replication of HCMV Towne strain in human foreskin fibroblasts, with an EC50 of 0.4 µM; it moderately inhibits the replication of GPCMV in guinea pig lung fibroblasts, with EC50 values of 3.6 µM and 3.1 µM in plaque and PCR assays, respectively[2].
MLS8091 (72 h) induces MLS8091-resistant HCMV Towne mutants (SS-8091-R1, SS-8091-R2, SS-8091-R3) in human foreskin fibroblasts; compared with the EC50 value of 0.4 µM for wild-type HCMV, the EC50 values of these mutants range from 52.4 to 63.6 µM (with a resistance fold of 131 to 158.9). This resistance is mediated by the D487Y mutation in the UL70 gene (accompanied by the P165S mutation in the UL102 gene in SS-8091-R1)[2].
MLS8091 (Varying concentrations; 72 h) induces MLS8091-resistant HCMV Towne mutants (MS-8091-R1, MS-8091-R2, MS-8091-R3) in human foreskin fibroblasts; compared with the EC50 value of 0.4 µM for wild-type HCMV, these mutants have EC50 values ranging from 58.4 to 88.6 µM (with a resistance fold change of 145.9 to 221.6), and this resistance is mediated by UL102F275L or UL70D486H mutations[2].
MLS8091 (0.1-10 µM; 10 days) demonstrates that UL70D487Y and UL70D486H mutations both confer full resistance to MLS8091 in HCMV Towne strain. In human foreskin fibroblasts, neither mutant virus strain receives inhibitory effects under treatment with up to 10 µM MLS8091, while wild-type HCMV displays dose-dependent viral suppression[2].
MLS8091 (0.1-10 µM; 10 days) exhibits drastically weakened antiviral activity against tagged UL70D487Y mutant HCMVAD169 in human foreskin fibroblasts: the EC50 value reaches 40.84 µM with a 97.3-fold resistance shift, whereas wild-type HCMVAD169 has an EC50 of 0.42 µM[2].
MLS8091 (0.1–10 µM; 96 h) fails to suppress the expression of HCMVAD169 viral proteins (IE1/2, UL44, UL84, pp65) in human foreskin fibroblasts if the virus harbors the UL70D487Y mutation[2].
MLS8091 (0.1-10 µM; 4 days) loses strong inhibitory activity against HCMV AD169 viral load in human foreskin fibroblast supernatants when virus carries the UL70D487Y mutation[2].
MLS8091 (0.1-10 µM; 48 h) reveals that the UL70D487Y mutation abolishes the inhibitory activity of MLS8091 against HCMV AD169 viral DNA replication in human foreskin fibroblasts[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human foreskin fibroblasts (HFFs)
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Concentration:0, 0.1, 0.5, 1, 3, 10 μM
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Incubation Time:72 h post-infection
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Result:Inhibited expression of all tested viral proteins (IE1, IE2, UL84, UL44, pp65) at 72 hpi.
Reduced protein levels observed in a dose-dependent manner.
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Cell Line:human foreskin fibroblasts (HFFs)
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Concentration:1.5 μM
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Incubation Time:0, 24, 48, 72, 96, 120 hpi
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Result:Inhibited viral DNA replication more strongly than GCV, while effects on viral DNA yield in supernatants were not significantly different from GCV.
Viral DNA load in cells was significantly reduced at 72, 96, and 120 hpi compared to untreated infected controls.
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Cell Line:human foreskin fibroblasts (HFFs) infected with HCMV Towne strain
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Concentration:3 µM
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Incubation Time:Continuous exposure (Day 0-6)
Exposure (Day 0-1)
Exposure (Day 0-2)
Exposure (Day 0-3)
Exposure (Day 3-6) -
Result:Caused reversible inhibition of HCMV, as viral DNA yield recovered following compound removal on days 1, 2, or 3, similar to the pattern observed with Ganciclovir (HY-13637).
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Cell Line:human foreskin fibroblasts (HFFs) infected with UL70 D487Y recombinant HCMV AD169 mutant
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Concentration:0.1, 0.5, 3, 10 µM
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Incubation Time:96 h
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Result:Caused a dose-dependent inhibition of HCMV proteins IE1/2, UL44, UL84, and pp65 in wild-type AD169, but showed no decrease in these viral proteins in the UL70 D487Y mutant.
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Cell Line:human foreskin fibroblasts (HFFs) infected with UL70 D487Y recombinant HCMV AD169 mutant
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Concentration:0.1, 0.5, 3, 10 µM
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Incubation Time:4 days
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Result:Caused a dose-dependent reduction in viral load in supernatants from wild-type AD169-infected cells, while only a significantly attenuated inhibitory effect was observed in UL70 D487Y mutant-infected cells.
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Cell Line:human foreskin fibroblasts (HFFs) infected with UL70 D487Y recombinant HCMV AD169 mutant
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Concentration:0.1, 0.5, 3, 10 µM
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Incubation Time:48 h
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Result:Significantly inhibited viral DNA replication in wild-type AD169-infected cells, while the inhibitory effect on the UL70 D487Y mutant was not statistically significant.
Chemical Information
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CAS No. 848217-46-9
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Appearance Solid
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분자량 420.51
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화학식 C21H16N4O2S2
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Color Pink to orange
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SMILES
O=S(C1=CC=CS1)(C2=C(N)N(CC3=CC=CC=C3)C4=C2N=C5C=CC=CC5=N4)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 50 mg/mL (118.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (290 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Kapoor A, et al. Validation and Characterization of Five Distinct Novel Inhibitors of Human Cytomegalovirus. Journal of medicinal chemistry. 2020 Apr 23;63(8):3896-3907. [Content Brief]
[2]. Kapoor A, et al. A novel inhibitor of human cytomegalovirus acts through a specific antiviral mechanism that involves the helicase-primase complex. Antimicrobial agents and chemotherapy. 2026 Jul 13. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3781 mL | 11.8903 mL | 23.7806 mL | 59.4516 mL |
| 5 mM | 0.4756 mL | 2.3781 mL | 4.7561 mL | 11.8903 mL | |
| 10 mM | 0.2378 mL | 1.1890 mL | 2.3781 mL | 5.9452 mL | |
| 15 mM | 0.1585 mL | 0.7927 mL | 1.5854 mL | 3.9634 mL | |
| 20 mM | 0.1189 mL | 0.5945 mL | 1.1890 mL | 2.9726 mL | |
| 25 mM | 0.0951 mL | 0.4756 mL | 0.9512 mL | 2.3781 mL | |
| 30 mM | 0.0793 mL | 0.3963 mL | 0.7927 mL | 1.9817 mL | |
| 40 mM | 0.0595 mL | 0.2973 mL | 0.5945 mL | 1.4863 mL | |
| 50 mM | 0.0476 mL | 0.2378 mL | 0.4756 mL | 1.1890 mL | |
| 60 mM | 0.0396 mL | 0.1982 mL | 0.3963 mL | 0.9909 mL | |
| 80 mM | 0.0297 mL | 0.1486 mL | 0.2973 mL | 0.7431 mL | |
| 100 mM | 0.0238 mL | 0.1189 mL | 0.2378 mL | 0.5945 mL |
MLS8091 Related Classifications
HY-186273 Related Classifications
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