Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
IC50: 0.20 μM (PAN)[1] KD: 56.02 nM (PAN)[1]
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ln Vitro |
Influenza virus-IN-6 (Compound 35) exhibits anti-influenza virus activity after 48 hours, with EC50s of 1.28 ± 0.35, 1.12 ± 0.65, 0.76 ± 0.11, and Flu B against H1N1, H5N1, H3N2, and Flu B in MDCK cells, respectively. 0.43 ± 0.06 μM[1]. Influenza virus-IN-6 (5–20 μM; 24 h) impacts viral adsorption, but not viral particles, cells, or replication [1]. Influenza virus-IN-6 suppresses the activity of influenza virus polymerase at 2.5–10 μM for 24 hours [1]. In liver microsomes, intestine S9-UDPGA, and mouse plasma, influenza virus-IN-6 exhibits good stability [1].
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ln Vivo |
Compound 35 (7.5-30 mg/kg/d; intraperitoneally; twice daily for 7 days) effectively shields mice against influenza virus infection [1]. The influenza virus-IN-6 (Compound 35) pharmacokinetic (PK) profile in vivo after a single dose in rats (n = 5)a[1] parameter IV (2 mg/kg) PO (10 mg/kg) IP (15 mg/kg) T1/2 (h) 0.33 ± 0.07 0.82 ± 0.16 1.07 ± 0.25 Tmax (h) NA 0.52 0.45 Cmax (ng/mL) 1586.55 ± 366.48 92.20 ± 36.25 889.52 ± 233.17 AUC0-t (h · ng/mL) 536.45 ± 58.72 164.30 ± 26.37 790.62 ± 188.31 CL (mL/min/kg) 53.76 ± 13.18 NA NA F % NA 6.13% 29.50% aIV stands for intravenous injection, IP for intraperitoneal injection, and PO for the gastrointestinal route. The half-life of a compound exposure in plasma is known as T1/2. The time it takes to focus to its maximum is known as Tmax. Cmax is the greatest concentration that has been measured. The area under the curve is known as AUC (0–t). The clearance is CL (mL/min/kg). The percentage of bioavailability is F%.
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Cell Assay |
Western Blot Analysis[1]
Cell Types: MDCK cells Tested Concentrations: 5, 10 and 20 μM Incubation Duration: 24 h Experimental Results: diminished nucleoprotein (NP) and matrix protein 2 (M2). RT-PCR[1] Cell Types: MDCK cells Tested Concentrations: 2.5, 5, 10 and 20 μM Incubation Duration: 24 h Experimental Results: diminished the expression of viral NP mRNA in a well-defined dose-dependent manner. Inhibited cRNA synthesis in a dose-dependent fashion. |
Animal Protocol |
Animal/Disease Models: balb/c (Bagg ALBino) mouse:, H1N1 infection model[1]
Doses: 0, 7.5, 15, and 30 mg/kg/d Route of Administration: intraperitoneal (ip)injection, twice per day for 7 days Experimental Results: demonstrated excellent anti-IAV activity in vivo at a dose of 30 mg/kg/d. Still demonstrated potent antiviral activity in vivo , with a survival ratio of approximately 60% against lethal virus infection in mice at 15 mg/kg/d. Animal/Disease Models: SD rats[1] Doses: 2, 10 or 15 mg/kg Route of Administration: IV, IP, or PO ( pharmacokinetic/PK Analysis) Experimental Results: demonstrated good pharmacokinetic/PK profiles. |
References |
[1]. Liao Y, et al. Identification of N- and C-3-Modified Laudanosoline Derivatives as Novel Influenza PAN Endonuclease Inhibitors. J Med Chem. 2022 Dec 15.
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Molecular Formula |
C27H26CLNO7
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Molecular Weight |
511.95
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CAS # |
2919303-26-5
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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 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.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.9533 mL | 9.7666 mL | 19.5332 mL | |
5 mM | 0.3907 mL | 1.9533 mL | 3.9066 mL | |
10 mM | 0.1953 mL | 0.9767 mL | 1.9533 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.