I1421
Based on 1 Customer Validation
I1421 is an activator of the cystic fibrosis transmembrane conductance regulator (CFTR) with an EC50 of 64 nM for WT CFTR currents. I1421 also allosterically activates multiple mutants causing cystic fibrosis (CF) with good in vivo potency, with an oral bioavailability of 60% in mice corresponding to a half-life of 75 min. I1421 synergizes with Elexacaftor (HY-111772) to enhance CFTR currents.
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- Purity: 99.15%
- CAS No.: 3054995-92-2
- 화학식: C18H18FN3O3
- 분자량:343.35
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보관: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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Immunology/Inflammation Compound Library
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Membrane Transporter/Ion Channel Compound Library
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Membrane Protein-targeted Compound Library
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Membrane Receptor-targeted Compound Library
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
EC50: 64 nM (WT CFTR)[1]
I1421 (3 mg/kg; iv, po; single dose) has a bioavailability of 60% in mice after oral and intravenous injection, but the oral T1/2 is shorter (75 min)[1].
Pharmacokinetic Analysis in C57BL/6 Mice[1]
| Route | Dose (mg/kg) | Tmax (h) | Cmax (ng/mL) | AUClast (ng·h/mL) | T1/2 (h) | CL (mL/min/kg) | Vss (1/kg) | F (%) |
| IP | 10 | 0.25 | 2617 | 2145 | 2.16 | - | - | - |
| PO | 10 | 0.25 | 1181 | 1211 | 1.24 | - | - | 60 |
| SC | 10 | 0.50 | 625 | 1512 | 1.36 | - | - | - |
| IV | 3 | - | 2354 | 610 | 1.78 | 81.51 | 2.49 | - |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3054995-92-2
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Appearance Solid
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분자량 343.35
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화학식 C18H18FN3O3
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Color White to off-white
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SMILES
O=C(N1N=C(N)C2=C1C=C(CO)C=C2)[C@@H](C)COC3=CC=C(F)C=C3
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 100 mg/mL (291.25 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)
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 (7.28 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 (7.28 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.
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.
순도&문서
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9125 mL | 14.5624 mL | 29.1248 mL | 72.8120 mL |
| 5 mM | 0.5825 mL | 2.9125 mL | 5.8250 mL | 14.5624 mL | |
| 10 mM | 0.2912 mL | 1.4562 mL | 2.9125 mL | 7.2812 mL | |
| 15 mM | 0.1942 mL | 0.9708 mL | 1.9417 mL | 4.8541 mL | |
| 20 mM | 0.1456 mL | 0.7281 mL | 1.4562 mL | 3.6406 mL | |
| 25 mM | 0.1165 mL | 0.5825 mL | 1.1650 mL | 2.9125 mL | |
| 30 mM | 0.0971 mL | 0.4854 mL | 0.9708 mL | 2.4271 mL | |
| 40 mM | 0.0728 mL | 0.3641 mL | 0.7281 mL | 1.8203 mL | |
| 50 mM | 0.0582 mL | 0.2912 mL | 0.5825 mL | 1.4562 mL | |
| 60 mM | 0.0485 mL | 0.2427 mL | 0.4854 mL | 1.2135 mL | |
| 80 mM | 0.0364 mL | 0.1820 mL | 0.3641 mL | 0.9101 mL | |
| 100 mM | 0.0291 mL | 0.1456 mL | 0.2912 mL | 0.7281 mL |
I1421 Related Classifications
HY-158991 Related Classifications
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