[CAS NO. 1450929-77-7] LHF-535
PRODUCTS SPECIFICATIONS [1450929-77-7]
DESCRIPTION [1450929-77-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 412.52 |
| Molecular Formula | C27H28N2O2 |
| SMILES | OC(C)(C)C1=CC=C(/C=C\C2=CC=C3C(N=CN3C4=CC=C(OC(C)C)C=C4)=C2)C=C1 |
Summary
LHF-535 is an antiviral agent extracted from patent WO2013123215A2, Compound 38, has EC 50 s of <1 μM, <1 μM, <1 μM, and 1-10 μM for Lassa, Machupo, Junin, and VSVg virus, respectively [1] .
In Vitro
LHF-535 is a small-molecule viral entry inhibitor that targets the arenavirus envelope glycoprotein (GP). LHF-535 exhibits potent antiviral activity against a broad array of hemorrhagic fever arenaviruses. LHF-535 inhibits Lassa GP-pseudotyped lentivirus with an IC 50 of 0.1-0.3 nM [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
LHF-535 (3, 10 or 30 mg/kg; orally; daily; 14 days) protectes mice from a lethal challenge with Tacaribe virus and dramatically reduces viral titers in plasma, spleen, and liver
[2]
.
An increase in survival is also observed when the first dose of LHF-535 (10 mg/kg) is delayed by 1, 2, or 3 days after infection, demonstrating that LHF-535 is efficacious as a post-exposure therapeutic in mice
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | IFN-α/β and-γ receptor-deficient AG129 mice [2] |
| Dosage: | 3, 10, or 30 mg/kg/day |
| Administration: | Orally; daily; 14 days |
| Result: | Effective as a post-exposure therapeutic. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT03993704 | Kineta Inc.|Wellcome Trust |
Healthy
|
September 16, 2019 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 96.67 mg/mL ( 234.34 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.4241 mL | 12.1206 mL | 24.2412 mL |
| 5 mM | 0.4848 mL | 2.4241 mL | 4.8482 mL |
| 10 mM | 0.2424 mL | 1.2121 mL | 2.4241 mL |
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1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.42 mg/mL (5.87 mM); Clear solution
References