IHVR-19029
Based on 1 Customer Validation
IHVR-19029 is a potent endoplasmic reticulum (ER) α-glucosidases I and II inhibitor, with an IC50 of 0.48 μM for ER a-glucosidase I. IHVR-19029 efficiently blocks the replication of several hemorrhagic fever viruses, such as Dengue virus (DENV), Ebola virus (EBOV) and Rift Valley fever virus. The combination of IHVR-19029 with Favipiravir (HY-14768) improves the antiviral efficacy.
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- Pureté: 96.0%
- CAS No.: 1447464-73-4
- Formule: C23H45N3O5
- Masse moléculaire:443.62
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7 | CC50 |
>500 μM
Compound: 8c
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Cytotoxicity against human Huh7.5 cells by MTT assay
Cytotoxicity against human Huh7.5 cells by MTT assay
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[PMID: 23747225] |
| Huh-7 | EC50 |
0.74 μM
Compound: 8c
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Antiviral activity against Tacaribe virus infected in human Huh7.5 cells assessed as reduction in viral yield after 3 days by neutral-red staining-based microscopic analysis
Antiviral activity against Tacaribe virus infected in human Huh7.5 cells assessed as reduction in viral yield after 3 days by neutral-red staining-based microscopic analysis
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[PMID: 23747225] |
In Vitro
IHVR-19029 efficiently inhibits Bovine viral diarrhea virus (BVDV), Tacaribe virus (TCRV) and Dengue virus (DENV) with EC50s of 0.25, 0.74, and 1.25 μM, respectively[2]. The combination of IHVR-19029 and Favipiravir (HY-14768) synergistically inhibits the replication of Yellow fever and Ebola viruses in cultured cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
IHVR-19029 (5 mg/kg; i.v.) has AUC, C0, T1/2, CL and Vd values of 1383 μg*h/mL, 1.79 μg/mL, 1.2 hours, 3.49 L/h/kg, and 3.0 L/kg, respectively[2].
IHVR-19029 (75/5/5 mg/kg; p.o./i.m./i.p.) has AUC values of 945/1839/983 μg*h/mL, Cmax values of 0.26/1.23/1.33 μg/ml, Tmax values of 2.1/0.1/0.17 hours, and F values of 4.6/71/133%, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice (12 week 233 of age) (MARV infection)[2]
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Dosage:25, 75 mg/kg
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Administration:I.p.; twice daily, until 10 days
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Result:Significant protection of Marburg virus (MARV) induced death were observed.
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Animal Model:C57B1/6 mice (8–12 week of age) (EBOV infection)[2]
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Dosage:25, 75 mg/kg
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Administration:I.p.; twice daily for 10 days
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Result:Significant survival were observed.
Chemical Information
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CAS No. 1447464-73-4
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Appearance Solid
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Masse moléculaire 443.62
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Formule C23H45N3O5
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Color Off-white to light yellow
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SMILES
O=C(NC(C)(C)C)N(C1CCCCC1)CCCCCCN2[C@H](CO)[C@@H](O)[C@H](O)[C@@H](O)C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (225.42 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)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.64 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.64 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (274 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
[1]. Bray M, et al. Meeting report: 31st International Conference on Antiviral Research. Antiviral Res. 2018 Oct;158:88-102. [Content Brief]
[2]. Chang J, et al. Small molecule inhibitors of ER α-glucosidases are active against multiple hemorrhagic fever viruses. Antiviral Res. 2013;98(3):432‐440. [Content Brief]
[3]. Ester Prodrugs of IHVR-19029 with Enhanced Oral Exposure and Prevention of Gastrointestinal Glucosidase Interaction.ACS Med Chem Lett. 2017 Jan 17;8(2):157-162. [Content Brief]
[4]. Ma J, et al. Enhancing the antiviral potency of ER α-glucosidase inhibitor IHVR-19029 against hemorrhagic fever viruses in vitro and in vivo. Antiviral Res. 2018 Feb;150:112-122. [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 |
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| DMSO | 1 mM | 2.2542 mL | 11.2709 mL | 22.5418 mL | 56.3545 mL |
| 5 mM | 0.4508 mL | 2.2542 mL | 4.5084 mL | 11.2709 mL | |
| 10 mM | 0.2254 mL | 1.1271 mL | 2.2542 mL | 5.6355 mL | |
| 15 mM | 0.1503 mL | 0.7514 mL | 1.5028 mL | 3.7570 mL | |
| 20 mM | 0.1127 mL | 0.5635 mL | 1.1271 mL | 2.8177 mL | |
| 25 mM | 0.0902 mL | 0.4508 mL | 0.9017 mL | 2.2542 mL | |
| 30 mM | 0.0751 mL | 0.3757 mL | 0.7514 mL | 1.8785 mL | |
| 40 mM | 0.0564 mL | 0.2818 mL | 0.5635 mL | 1.4089 mL | |
| 50 mM | 0.0451 mL | 0.2254 mL | 0.4508 mL | 1.1271 mL | |
| 60 mM | 0.0376 mL | 0.1878 mL | 0.3757 mL | 0.9392 mL | |
| 80 mM | 0.0282 mL | 0.1409 mL | 0.2818 mL | 0.7044 mL | |
| 100 mM | 0.0225 mL | 0.1127 mL | 0.2254 mL | 0.5635 mL |
IHVR-19029 Related Classifications
HY-124662 Related Classifications
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