SLC6A19-IN-4
Based on 1 Customer Validation
SLC6A19-IN-4 is an allosteric-competitive and orally active B0AT1 inhibitor. SLC6A19-IN-4 inhibits both human and mouse B0AT1 with IC50 values of 513 nM and 295 nM, respectively. SLC6A19-IN-4 exhibits excellent metabolic stability. SLC6A19-IN-4 significantly increases urinary phenylalanine (Phe) excretion and reduces plasma Phe levels through dual inhibition of B0AT1 in both the intestine (reducing absorption) and kidney (promoting excretion) in vivo. SLC6A19-IN-4 can be used for phenylketonuria (PKU) and other disorders involving SLC6-family transporters research.
For research use only. We do not sell to patients.
- Purity: 99.55%
- CAS No.: 2962069-39-0
- Formula: C16H16F3N3O3
- Molecular Weight:355.31
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
SLC6A19-IN-4 (1500-4000 nM) increases the Km for d5-Phe without affecting Vmax, indicating competitive inhibition (Km = 0.866, 5.19, 12.1 mM Vmax = 337, 351, 380 μmol/min/mg-protein) in the Jump-In TI platform cells expressing human SLC6A19 and human Collectrin[1].
SLC6A19-IN-4 revealed Kd = 123.1 nM for mock cell and mB0AT1 and ACE2-expressing cell and Kd = 46.98 nM in mock cell and hB0AT1 and ACE2-expressing cell[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Pahenu2 mice (12 weeks) carry a homozygous F263[1]
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Dosage:30 mg/kg
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Administration:p.o., once
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Result:Had a plasma concentration of 915 ng/ml and 1590 ng/ml at 4 and 8 hours post-dose.
Showed low membrane permeability 24.2 × 10-7 cm/s.
Increased urinary Phe excretion and concomitantly reduced plasma Phe concentrations 4 hours after dosing.
Chemical Information
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CAS No. 2962069-39-0
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Appearance Solid
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Molecular Weight 355.31
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Formula C16H16F3N3O3
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Color White to off-white
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SMILES
O=C(NCC(N1CC(NCC1)=O)=O)/C=C/C2=CC=C(C=C2)C(F)(F)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 50 mg/mL (140.72 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)
Purity & Documentation
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Data Sheet (271 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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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 | 2.8144 mL | 14.0722 mL | 28.1444 mL | 70.3611 mL |
| 5 mM | 0.5629 mL | 2.8144 mL | 5.6289 mL | 14.0722 mL | |
| 10 mM | 0.2814 mL | 1.4072 mL | 2.8144 mL | 7.0361 mL | |
| 15 mM | 0.1876 mL | 0.9381 mL | 1.8763 mL | 4.6907 mL | |
| 20 mM | 0.1407 mL | 0.7036 mL | 1.4072 mL | 3.5181 mL | |
| 25 mM | 0.1126 mL | 0.5629 mL | 1.1258 mL | 2.8144 mL | |
| 30 mM | 0.0938 mL | 0.4691 mL | 0.9381 mL | 2.3454 mL | |
| 40 mM | 0.0704 mL | 0.3518 mL | 0.7036 mL | 1.7590 mL | |
| 50 mM | 0.0563 mL | 0.2814 mL | 0.5629 mL | 1.4072 mL | |
| 60 mM | 0.0469 mL | 0.2345 mL | 0.4691 mL | 1.1727 mL | |
| 80 mM | 0.0352 mL | 0.1759 mL | 0.3518 mL | 0.8795 mL | |
| 100 mM | 0.0281 mL | 0.1407 mL | 0.2814 mL | 0.7036 mL |
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