| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
IHVR-17028 targets ER α-glucosidase I, a host enzyme critical for the proper folding and maturation of viral envelope glycoproteins. By inhibiting this enzyme, it disrupts the N-linked glycosylation process, leading to the production of misfolded viral glycoproteins and impaired viral infectivity.
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|---|---|
| ln Vitro |
IHVR-17028 suppresses viral activity in virus yield reduction experiments, with EC50 values of 0.4 μM, 0.26 μM, and 0.3 μM for DENV (serotype 2, New Guinea C), bovine viral diarrhea virus (BVDV) (NADL strain), and tacaribe virus (TCRV) (11573 strain), respectively. Furthermore, IHVR-17028 shows IC50 values in MDBK, Huh7.5, or BHK cells that are all >500 μM in MTT assays[1].
In vitro, IHVR-17028 potently inhibits ER α-glucosidase I with an IC50 of 0.24 μM. It exhibits broad-spectrum antiviral activity, with EC50 values of 0.4 μM against BVDV, 0.26 μM against TCRV, and 0.3 μM against DENV. |
| ln Vivo |
In rats, IHVR17028 (oral gavage; 75 mg/kg) demonstrates a Cmax in pharmacokinetic study.T1/2 value is 0.88 hours after IV; value of 0.18 μg/ml; Tmax value is 1.56 hours; and the F% value is 12% following PO delivery. administration [1]. In a mouse model of deadly MARV infection, IHVR-17028 (oral gavage; 25–50 mg/kg; therapy 1 day prior to virus challenge) shows substantial protection[1].
In vivo, IHVR-17028 has antiviral activity. Its inhibition of ER α-glucosidase I disrupts viral replication in animal models of viral infection. It is being studied for the treatment of infectious diseases caused by enveloped viruses. |
| Enzyme Assay |
ER α-glucosidase I inhibition is assessed using an in vitro enzyme activity assay. The enzyme is incubated with a fluorogenic substrate and varying concentrations of IHVR-17028. The inhibition of substrate cleavage is measured to determine the IC50.
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| Cell Assay |
The antiviral activity of IHVR-17028 is assessed in cell-based assays using virus-infected cells. Cells are infected with a virus (e.g., DENV) and treated with varying concentrations of the compound. Viral replication is measured by quantifying viral RNA or infectious virus particles, and the EC50 is calculated.
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| Animal Protocol |
Animal/Disease Models: balb/c (Bagg ALBino) mouse: are challenged with 1,000 PFU mouse adapted MARV via IP injection[1]
Doses: 50 mg/kg Route of Administration: Treatment 1 day prior to virus challenging Experimental Results: demonstrated protection in mouse when the treatment is initiated 1 day prior to virus challenging. Animal/Disease Models: C57B1/6 mice challenged with 1,000 PFU mouse adapted EBOV[1] Doses: 25 mg/kg Route of Administration: twice (two times) daily at 12 h interval ; starting 4 h post infection for 10 days Experimental Results: Inhibited EBOV infection in mice. In vivo efficacy is evaluated in animal models of viral infection, such as mice infected with DENV. IHVR-17028 is administered, and viral load, clinical signs, and survival are measured. The compound's ability to reduce viral replication and improve outcomes is assessed. |
| ADME/Pharmacokinetics |
As a small molecule with an IC50 of 0.24 μM, IHVR-17028 is expected to have favorable drug-like properties. It may have good oral bioavailability and tissue distribution, making it suitable for systemic antiviral therapy.
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| Toxicity/Toxicokinetics |
As an antiviral agent targeting a host enzyme, IHVR-17028 may have a higher barrier to resistance development. Potential toxicities may include effects on host glycoprotein processing, but these are expected to be minimal at therapeutic doses.
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| References | |
| Additional Infomation |
IHVR-17028 is a research compound being developed as a broad-spectrum antiviral agent. It is a potent inhibitor of ER α-glucosidase I with activity against several viruses. It is not approved for clinical use.
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| Molecular Formula |
C23H44N2O5
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|---|---|
| Molecular Weight |
428.61
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| Exact Mass |
428.325
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| CAS # |
1428247-78-2
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| PubChem CID |
71580338
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| Appearance |
Colorless to light yellow ointment
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| LogP |
2.3
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
30
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| Complexity |
518
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CC(C)(C)C(=O)N(CCCCCCN1C[C@@H]([C@H]([C@@H]([C@H]1CO)O)O)O)C2CCCCC2
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| InChi Key |
DWMQGQSPNDGKJC-PLACYPQZSA-N
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| InChi Code |
InChI=1S/C23H44N2O5/c1-23(2,3)22(30)25(17-11-7-6-8-12-17)14-10-5-4-9-13-24-15-19(27)21(29)20(28)18(24)16-26/h17-21,26-29H,4-16H2,1-3H3/t18-,19+,20-,21-/m1/s1
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| Chemical Name |
N-cyclohexyl-2,2-dimethyl-N-[6-[(2R,3R,4R,5S)-3,4,5-trihydroxy-2-(hydroxymethyl)piperidin-1-yl]hexyl]propanamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3331 mL | 11.6656 mL | 23.3312 mL | |
| 5 mM | 0.4666 mL | 2.3331 mL | 4.6662 mL | |
| 10 mM | 0.2333 mL | 1.1666 mL | 2.3331 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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