2. Membrane Transporter/Ion Channel
  3. Amino acid Transporter
  4. SLC6A19-IN-4

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.

SLC6A19-IN-4

SLC6A19-IN-4 Chemical Structure

CAS No. : 2962069-39-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

SLC6A19-IN-4 Related Antibodies

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Description

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[1].

In Vitro

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.

SLC6A19-IN-4 Related Antibodies
In Vivo

SLC6A19-IN-4 (30 mg/kg, p.o., once) reduces intestinal Phe absorption promotes urinary excretion and lowers systemic Phe levels in male Pahenu2 mice carry a homozygous F263[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Pahenu2 mice (12 weeks) carry a homozygous F263[1]
Dosage: 30 mg/kg
Administration: p.o., once
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.
Molecular Weight

355.31

Formula

C16H16F3N3O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NCC(N1CC(NCC1)=O)=O)/C=C/C2=CC=C(C=C2)C(F)(F)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8144 mL 14.0722 mL 28.1444 mL
5 mM 0.5629 mL 2.8144 mL 5.6289 mL
View the 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.

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Purity & Documentation
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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SLC6A19-IN-4 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SLC6A19-IN-42962069-39-0Amino acid Transporter氨基酸转运蛋白B?AT1orally activeintestinekidneyphenylketonuriaSLC6-familyInhibitorinhibitorinhibit

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