| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg | |||
| Other Sizes |
| Targets |
IHVR-19029 targets ER α-glucosidases I and II, host enzymes essential for the proper folding and maturation of viral envelope glycoproteins. By inhibiting these enzymes, it disrupts the N-linked glycosylation process, leading to misfolded viral glycoproteins and impaired viral entry and replication.
|
|---|---|
| ln Vitro |
With EC50 values of 0.25, 0.74, and 1.25 μM, respectively, IHVR-19029 may efficiently suppress the dengue virus (DENV), Takarib virus (TCRV), and bovine viral diarrhea virus (BVDV) [2]. IHVR-19029 and Favipiravir work in concert to suppress the replication of Ebola and yellow fever viruses in cultured cells [4].
In vitro, IHVR-19029 potently inhibits ER α-glucosidase I with an IC50 of 0.48 μM. It effectively blocks the replication of several hemorrhagic fever viruses, including DENV, EBOV, and Rift Valley fever virus. |
| ln Vivo |
IHVR-19029 (25-75 mg/kg; i.p.; twice daily for 10 days) suppresses EBOV and MARV infection in mice [2]. The AUC, C0, T1/2, CL and Vd values of IHVR-19029 (5 mg/kg; iv) are 1383 μg*h/mL, 1.79 μg/mL, 1.2 hours, 3.49 L/h/kg and 3.0 L/ kg, respectively[2]. The AUC value of IHVR-19029 (75/5/5 mg/kg; po/im/ip) is 945/1839/983 μg*h/mL, the Cmax value is 0.26/1.23/1.33 μg/ml, and the Tmax value is 2.1 /0.1/0.17 hours, the F values are 4.6/71/133% respectively[2].
In vivo, IHVR-19029 is being studied as a host-targeted antiviral agent for the treatment of hemorrhagic fever viruses. It has been shown to enhance the antiviral effect when combined with Favipiravir, suggesting potential for combination therapy. |
| Enzyme Assay |
ER α-glucosidase inhibition is assessed using an in vitro enzyme activity assay. The enzyme is incubated with a fluorogenic substrate and varying concentrations of IHVR-19029. The inhibition of substrate cleavage is measured to determine the IC50.
|
| Cell Assay |
The antiviral activity of IHVR-19029 is assessed in cell-based assays using virus-infected cells. Cells are infected with a virus (e.g., EBOV) and treated with varying concentrations of the compound. Viral replication is measured, and the EC50 is calculated.
|
| Animal Protocol |
Animal/Disease Models: balb/c (Bagg ALBino) mouse (12 weeks 233 years old) (MARV infection) [2]
Doses: 25, 75 mg/kg Route of Administration: intraperitoneal (ip) injection; twice (two times) daily until day 10 Experimental Results: Observed effects on Marburg Virus (MARV)-induced death was Dramatically protective. Animal/Disease Models: C57B1/6 mice (8-12 weeks old) (EBOV infection) [2] Doses: 25, 75 mg/kg Route of Administration: intraperitoneal (ip) injection; twice (two times) daily for 10 days Experimental Results: Significant effects were observed survival rate. In vivo efficacy is evaluated in animal models of viral infection, such as mice infected with EBOV or DENV. IHVR-19029 is administered alone or in combination with Favipiravir. Viral load, clinical signs, and survival are measured. |
| ADME/Pharmacokinetics |
As a small molecule, IHVR-19029 is expected to have favorable drug-like properties. It may have good oral bioavailability and tissue distribution, making it suitable for systemic antiviral therapy.
|
| Toxicity/Toxicokinetics |
As a host-targeted antiviral, IHVR-19029 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.
|
| References |
|
| Additional Infomation |
IHVR-19029 is a research compound being developed as a host-targeted antiviral agent for hemorrhagic fever viruses. It is a potent inhibitor of ER α-glucosidases I and II and has shown synergistic effects with Favipiravir. It is not approved for clinical use.
|
| Molecular Formula |
C23H43N3O5
|
|---|---|
| Molecular Weight |
441.604626893997
|
| Exact Mass |
443.335
|
| CAS # |
1447464-73-4
|
| PubChem CID |
71713800
|
| Appearance |
Off-white to light yellow solid powder
|
| LogP |
1.7
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
10
|
| Heavy Atom Count |
31
|
| Complexity |
536
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
O=C(NC(C)(C)C)N(CCCCCCN1[C](CO)[C@H]([C]([C@H](C1)O)O)O)C1CCCCC1 |^1:15,19|
|
| InChi Key |
GFBNIASMQRMEDU-PLACYPQZSA-N
|
| InChi Code |
InChI=1S/C23H45N3O5/c1-23(2,3)24-22(31)26(17-11-7-6-8-12-17)14-10-5-4-9-13-25-15-19(28)21(30)20(29)18(25)16-27/h17-21,27-30H,4-16H2,1-3H3,(H,24,31)/t18-,19+,20-,21-/m1/s1
|
| Chemical Name |
3-tert-butyl-1-cyclohexyl-1-[6-[(2R,3R,4R,5S)-3,4,5-trihydroxy-2-(hydroxymethyl)piperidin-1-yl]hexyl]urea
|
| Synonyms |
IHVR19029; IHVR 19029; IHVR-19029
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~225.42 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.64 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.64 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.64 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2645 mL | 11.3225 mL | 22.6449 mL | |
| 5 mM | 0.4529 mL | 2.2645 mL | 4.5290 mL | |
| 10 mM | 0.2264 mL | 1.1322 mL | 2.2645 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.