MMV1557817
Based on 1 publication(s) in Google Scholar
MMV1557817 is an orally active dual aminopeptidase (Aminopeptidase) inhibitor. MMV1557817 targets multiple parasite life cycle stages by inhibiting M1 alanyl aminopeptidase and M17 leucyl aminopeptidase involved in terminal Hemoglobin (HY-P2995) digestion (PfA-M1 Ki = 269 nM; PfA-M17 Ki = 101 nM), exhibits broad cross-species antiplasmodial activity, and clears P. berghei infection in a mouse model. MMV1557817 can be used for research on malaria.
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- Pureté : 99.06%
- CAS No.: 2065197-82-0
- Formule: C20H21F3N2O3
- Masse moléculaire:394.39
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Stockage:
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) MMV1557817
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Activité biologique
Description
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PfA-M1 269 nM (Ki app) |
PfA-M17 101 nM (Ki app) |
Plasmodium |
In Vitro
MMV1557817 selects the A460S mutation of PfA-M17 during in vitro selection in P. falciparum, suggesting that PfA-M17 is involved in its mechanism of action[1].
MMV1557817 (4-8 μM; 10 min) is a dual nanomolar inhibitor of recombinant PfA-M1 and PfA-M17 (Ki (app) of 269 nM and 101 nM, respectively), and inhibits the M1/M17 homologs of P. vivax and P. berghei[2].
MMV1557817 (10 mM stock solution; 72 h) inhibits the in vitro growth of P. falciparum 3D7 with an EC50 of 94 nM in the LDH assay[2].
MMV1557817 (1.25 µM) exhibits limited low-µM cross-reactivity with human LTA4H, shows no ERAP1/2 activity, and has a Ki of 0.3 µM for human APN[3].
MMV1557817 (300-1200 nM) stabilizes PfA-M1 and PfA-M17 in Pf3D7 parasite lysates at 300 nM and 1200 nM[3].
MMV1557817 (72 h) inhibits early and late-stage PfNF54 gametocytes with IC50 values of 99 nM and 309 nM, respectively, and has an IC50 of 1474 nM against mature gametocytes[3].
MMV1557817 retains activity against drug-resistant P. falciparum isolates, with an NF54 IC50 of 22 nM and no IC50 shift among the tested resistant strains[3].
MMV1557817 (320 nM; 1 h) increases hemoglobin-derived peptides in Pf3D7 trophozoites, consistent with dual inhibition of PfA-M1 and PfA-M17[3].
In MMV1557817-resistant Dd2 parasites, PfA-M17 hexamer levels decrease after PfA-M1 inhibition, and residual PfA-M17 activity is reduced[3].
MMV1557817-resistant Dd2 parasites contain 1.5 times more hemozoin than parental Dd2 at the mid-to-late trophozoite stage[3].
MMV1557817-resistant parasites exhibit 22-fold resistance to PfA-M17 inhibition and 3.5-fold increased sensitivity to PfA-M1 inhibition[3].
The PfA-M17 A460S mutation associated with MMV1557817 resistance disrupts hexamerization and cannot be introduced into Pf3D7 alone[3].
MMV1557817 (1 μM; 15-20 min) identifies MMV1557817-dependent stabilization of the aminopeptidases PfA-M1 and PfA-M17 in one-pot SPP of P. falciparum 3D7 lysates under 23% AEA, confirming these as targets of MMV1557817[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | T1/2 |
|---|---|---|---|
| Mice[3] | 50 mg/kg | p.o. | 4.3 h |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c (female, 6 weeks of age)[3]
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Dosage:50 mg/kg
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Administration:p.o. (oral gavage); at 2 h and on days 1, 2, and 3 post-infection
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Result:Showed excellent efficacy, with mice exhibiting a 95.4% parasite reduction when compared to the vehicle control.
No significant difference was seen versus the artesunate control.
Chemical Information
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CAS No. 2065197-82-0
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Appearance Solid
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Masse moléculaire 394.39
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Formule C20H21F3N2O3
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Color White to off-white
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SMILES
CC(C)(CC(NC(C1=CC=C(C=C1)C2=CC(F)=C(C(F)=C2)F)C(NO)=O)=O)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (253.56 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
Pureté et documentation
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Fiche technique (293 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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Instruction de manipulation (2659 KB)
Références
[2]. Mansouri M, et al. Novel Scaffold Unlocks Potent Cross-Peptidase and Cross-Species Inhibitors as Promising Antimalarial Agents. Journal of medicinal chemistry. 2026 Jan 22;69(2):1358-1386. [Content Brief]
[3]. Edgar RCS, et al. On-target, dual aminopeptidase inhibition provides cross-species antimalarial activity. mBio. 2024 Jun 12;15(6):e0096624. [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 (sealed storage, away from moisture). 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 | 2.5356 mL | 12.6778 mL | 25.3556 mL | 63.3890 mL |
| 5 mM | 0.5071 mL | 2.5356 mL | 5.0711 mL | 12.6778 mL | |
| 10 mM | 0.2536 mL | 1.2678 mL | 2.5356 mL | 6.3389 mL | |
| 15 mM | 0.1690 mL | 0.8452 mL | 1.6904 mL | 4.2259 mL | |
| 20 mM | 0.1268 mL | 0.6339 mL | 1.2678 mL | 3.1695 mL | |
| 25 mM | 0.1014 mL | 0.5071 mL | 1.0142 mL | 2.5356 mL | |
| 30 mM | 0.0845 mL | 0.4226 mL | 0.8452 mL | 2.1130 mL | |
| 40 mM | 0.0634 mL | 0.3169 mL | 0.6339 mL | 1.5847 mL | |
| 50 mM | 0.0507 mL | 0.2536 mL | 0.5071 mL | 1.2678 mL | |
| 60 mM | 0.0423 mL | 0.2113 mL | 0.4226 mL | 1.0565 mL | |
| 80 mM | 0.0317 mL | 0.1585 mL | 0.3169 mL | 0.7924 mL | |
| 100 mM | 0.0254 mL | 0.1268 mL | 0.2536 mL | 0.6339 mL |
MMV1557817 Related Classifications
HY-163727 Related Classifications
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