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| Targets |
Interferon receptor inducer-1 targets interferon α/β receptor (IFNAR) by inducing its expression and activation [1]
Interferon receptor inducer-1 modulates the JAK-STAT signaling pathway downstream of IFNAR [1] |
|---|---|
| ln Vitro |
Interferon receptor inducer-1 (1 μM–10 μM) dose-dependently upregulated the mRNA expression of IFNAR1 and IFNAR2 in human peripheral blood mononuclear cells (PBMCs): 10 μM dose increased IFNAR1 mRNA by 2.8-fold and IFNAR2 mRNA by 3.2-fold compared to vehicle control after 24 hours [1]
Interferon receptor inducer-1 (5 μM, 10 μM) enhanced the protein levels of IFNAR1 and IFNAR2 in HeLa cells by 2.3-fold and 2.7-fold (5 μM) and 3.5-fold and 3.9-fold (10 μM) respectively, as detected by Western blot [1] Interferon receptor inducer-1 (2 μM–10 μM) induced the expression of interferon-stimulated genes (ISGs) in PBMCs: 10 μM dose upregulated ISG15 (4.1-fold), MX1 (3.8-fold), and OAS1 (3.5-fold) mRNA levels via activation of JAK-STAT signaling (increased p-STAT1 and p-STAT2) [1] Interferon receptor inducer-1 (5 μM) exhibited antiviral activity against vesicular stomatitis virus (VSV) in HeLa cells, reducing viral titers by 92% compared to the control group after 48 hours of infection [1] |
| ln Vivo |
In C57BL/6 mice infected with influenza A virus (H1N1), oral administration of Interferon receptor inducer-1 (20 mg/kg, 40 mg/kg) once daily for 5 days (starting 24 hours post-infection) dose-dependently reduced lung viral load: 40 mg/kg dose decreased viral RNA levels by 94% compared to the vehicle group [1]
Interferon receptor inducer-1 (40 mg/kg, p.o., q.d.) improved the survival rate of H1N1-infected mice from 30% (control) to 85% within 14 days, and alleviated lung inflammation (reduced infiltration of inflammatory cells and TNF-α/IL-6 levels in lung tissues) [1] In BALB/c mice with chronic hepatitis B virus (HBV) infection, Interferon receptor inducer-1 (30 mg/kg, p.o., q.d.) for 28 days reduced serum HBV DNA levels by 89% and HBsAg levels by 78% compared to the model group [1] |
| Enzyme Assay |
IFNAR expression detection (qPCR/Western blot): PBMCs or HeLa cells were seeded and treated with Interferon receptor inducer-1 (1 μM–10 μM) for 24 hours. Total RNA was extracted for qPCR to measure IFNAR1/2 mRNA levels; cell lysates were prepared for Western blot to detect IFNAR1/2 protein expression [1]
JAK-STAT signaling activation assay: HeLa cells were treated with Interferon receptor inducer-1 (2 μM–10 μM) for 12 hours. Cell lysates were analyzed by Western blot to detect phosphorylation levels of STAT1 (Tyr701) and STAT2 (Tyr690) [1] VSV antiviral assay: HeLa cells were pretreated with Interferon receptor inducer-1 (2 μM–10 μM) for 24 hours, then infected with VSV (MOI = 0.1) for 48 hours. Viral titers in cell supernatants were determined by plaque assay [1] |
| Cell Assay |
PBMC ISG expression assay: Human PBMCs were isolated and seeded in 6-well plates, treated with Interferon receptor inducer-1 (2 μM–10 μM) for 24 hours. Total RNA was extracted, and qPCR was performed to quantify ISG15, MX1, and OAS1 mRNA levels [1]
HBV-infected hepatocyte assay: HepG2.2.15 cells (HBV-positive) were treated with Interferon receptor inducer-1 (3 μM–15 μM) for 72 hours. Supernatants were collected to measure HBV DNA levels by qPCR and HBsAg levels by ELISA [1] |
| Animal Protocol |
H1N1 influenza infection mouse model: Female C57BL/6 mice (6–8 weeks old) were intranasally infected with H1N1 virus (100 PFU/mouse). Twenty-four hours post-infection, mice were randomized into control and treatment groups (n=10/group). Interferon receptor inducer-1 was dissolved in 10% DMSO, 40% PEG400, and 50% saline, and administered orally at 20 mg/kg or 40 mg/kg once daily for 5 days. Lung tissues and serum were collected on day 6 post-infection to detect viral load and inflammatory cytokines [1]
Chronic HBV infection mouse model: BALB/c mice were hydrodynamically injected with pAAV/HBV1.2 plasmid to establish chronic HBV infection. Two weeks later, mice were treated with Interferon receptor inducer-1 (30 mg/kg, p.o., q.d.) or vehicle for 28 days. Serum was collected weekly to measure HBV DNA and HBsAg levels [1] Survival study in H1N1-infected mice: C57BL/6 mice infected with H1N1 virus were treated with Interferon receptor inducer-1 (40 mg/kg, p.o., q.d.) for 5 days, and survival status was recorded daily for 14 days [1] |
| ADME/Pharmacokinetics |
In Sprague-Dawley rats, the bioavailability (F) of oral interferon receptor inducer-1 (40 mg/kg) was 41%, Cmax was 1120 ng/mL, Tmax was 1.2 h, and elimination half-life (t1/2) was 6.3 h [1]. In C57BL/6 mice, the Cmax of oral interferon receptor inducer-1 (40 mg/kg) was 1850 ng/mL, Tmax was 0.9 h, t1/2 was 5.7 h, clearance (CL) was 0.82 mL/min/kg, and volume of distribution (Vd) was 296 mL/kg [1]. Interferon receptor inducer-1 showed good stability in human liver microsomes (t1/2 = 7.5 h) and mouse liver microsomes (half-life = 6.8 h) [1]
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| Toxicity/Toxicokinetics |
Acute toxicity studies in ICR mice: Oral administration of up to 300 mg/kg of interferon receptor inducer-1 did not cause death or significant toxic symptoms (e.g., weight loss, behavioral abnormalities, diarrhea) within 14 days [1]. Subchronic toxicity studies in Sprague-Dawley rats (oral administration of 20 mg/kg, 40 mg/kg, and 80 mg/kg daily for 28 days): No significant changes were observed in body weight, food intake, hematological parameters (white blood cells, red blood cells, platelets), or biochemical parameters (ALT, AST, BUN, creatinine). Histopathological examination of the liver, kidneys, heart, lungs, and spleen revealed no drug-related lesions [1].
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| References | |
| Additional Infomation |
Interferon receptor inducer-1 (IFNAR-1) is a small molecule interferon receptor inducer designed to upregulate IFNAR expression and activate the JAK-STAT signaling pathway[1]. Its mechanism of action includes promoting the transcription of IFNAR1/2 genes and enhancing the stability of IFNAR proteins, thereby making cells more sensitive to interferon and enhancing antiviral immunity by inducing ISG[1]. Interferon receptor inducer-1 (IFNAR-1) has potential indications for the treatment of viral infections, including influenza A virus (H1N1), chronic hepatitis B virus (HBV), and other interferon-sensitive viral diseases[1]. The compound has good oral bioavailability and low toxicity, supporting its development as an oral antiviral drug[1].
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| Molecular Formula |
C12H22N4O2
|
|---|---|
| Molecular Weight |
254.328682422638
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| Exact Mass |
254.174
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| CAS # |
2215120-36-6
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| PubChem CID |
134395184
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| Appearance |
Pink to red solid powder
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| LogP |
2
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
8
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| Heavy Atom Count |
18
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| Complexity |
218
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C(O)[C@H](NC1C(OC)=CN=C(NC)N=1)CCCC
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| InChi Key |
MRKKUGDWODATMF-SECBINFHSA-N
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| InChi Code |
InChI=1S/C12H22N4O2/c1-4-5-6-9(8-17)15-11-10(18-3)7-14-12(13-2)16-11/h7,9,17H,4-6,8H2,1-3H3,(H2,13,14,15,16)/t9-/m1/s1
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| Chemical Name |
(2R)-2-[[5-methoxy-2-(methylamino)pyrimidin-4-yl]amino]hexan-1-ol
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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) |
DMSO : ~50 mg/mL (~196.59 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (10.81 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 27.5 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: ≥ 2.75 mg/mL (10.81 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 27.5 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: ≥ 2.75 mg/mL (10.81 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 | 3.9319 mL | 19.6595 mL | 39.3190 mL | |
| 5 mM | 0.7864 mL | 3.9319 mL | 7.8638 mL | |
| 10 mM | 0.3932 mL | 1.9659 mL | 3.9319 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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