| Chemical Properties | Back Directory | [Boiling point ]
667.3±55.0 °C(Predicted) | [density ]
1.17±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
13.72±0.70(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Description]
IHVR-19029 is a lead endoplasmic reticulum α-glucosidases I and II inhibitor, which efficiently protected mice from lethal Ebola and Marburg virus infections via injection route. IHVR-19029 has been demonstrated to significantly protect mice from lethal infections of the Marburg and Ebola viruses when administrated via intraperitoneal injections. | [Uses]
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[1][2][3][4]. | [in vivo]
IHVR-19029 (25-75 mg/kg; I.p.; twice daily for 10 days) inhibits EBOV and MARV infection in mice[2].
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]. | Animal Model: | BALB/c mice (12 week 233 of age) (MARV infection)[2] | | Dosage: | 25, 75 mg/kg | | Administration: | I.p.; twice daily, until 10 days | | 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] | | Dosage: | 25, 75 mg/kg | | Administration: | I.p.; twice daily for 10 days | | Result: | Significant survival were observed.
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| [References]
[1] Bray M, et al. Meeting report: 31st International Conference on Antiviral Research. Antiviral Res. 2018 Oct;158:88-102. DOI:10.1016/j.antiviral.2018.08.002
[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. DOI:10.1016/j.antiviral.2013.03.023
[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. DOI:10.1021/acsmedchemlett.6b00332
[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. DOI:10.1016/j.antiviral.2017.12.008 |
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