2. Membrane Transporter/Ion Channel
  3. Urea Transporter
  4. M353-0039

M353-0039 is a selective UT-A2 inhibitor with a human IC50 of 0.35 μM. M353-0039 blocks urea transport mediated by UT-A2. M353-0039 can be used for the study of hyponatremia and edema associated with congestive heart failure, nephrotic syndrome, and cirrhosis.

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M353-0039

M353-0039 Chemical Structure

CAS No. : 1185074-29-6

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Description

M353-0039 is a selective UT-A2 inhibitor with a human IC50 of 0.35 μM. M353-0039 blocks urea transport mediated by UT-A2. M353-0039 can be used for the study of hyponatremia and edema associated with congestive heart failure, nephrotic syndrome, and cirrhosis[1].

In Vitro

M353-0039 (50 seconds) potently and selectively inhibits UT-A2 in human UT-A2-overexpressing HEK293F cells with an IC50 of 0.35 μM, showing no activity against UT-A3 or UT-B[1].
M353-0039 (10-100 μM; 30 minutes) does not inhibit rat UT-A1-mediated urea transport in stably expressing MDCK cells[1].
M353-0039 (10 nM-100 μM; 6 minutes) does not inhibit mouse UT-B-mediated urea transport in erythrocytes[1].
M353-0039 (10 μM; 5 minutes) inhibits urea transport in human HepG2 cells, confirming UT-A2-mediated urea efflux in these hepatic cells[1].
M353-0039 (50 μM) binds deeply to UT-A2, forming more interactions than prior inhibitors, including critical contacts in the unique "T-T" subpocket, which underpins its superior inhibitory potency[1].
M353-0039 (50 seconds) demonstrates that the C285 residue in UT-A2 is critical for its binding and inhibitory activity, as mutating it to alanine reduces potency and mutating it to tryptophan abolishes activity[1].
M353-0039 (100 μM; 24 hours) exhibits no cytotoxicity toward MDCK cells[1].

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

M353-0039 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: MDCK cells
Concentration: 100 μM
Incubation Time: 24 hours
Result: Did not reduce MDCK cell viability compared to vehicle controls.
In Vivo

M353-0039 (80 mg/kg; i.p.; single dose) selectively inhibits UT-A2-mediated renal urea transport in mice, producing significant reductions in kidney medulla and urine urea concentration and osmolarity under low-protein diet plus water deprivation conditions[1].

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

Animal Model: C57BL/6J (male, 8 weeks old)[1]
Dosage: 80 mg/kg
Administration: i.p.; single dose
Result: Significantly reduced kidney medulla urea concentration (P=0.0186) and osmolarity (P=0.0037).
Significantly reduced urine urea concentration (P<0.0001) and osmolarity (P<0.0001).
Caused only a minor decrease in kidney medulla urea concentration (P=0.0310) in mice on normal diet plus water deprivation.
Produced no significant changes in urine urea concentration or osmolarity in mice on normal diet plus water deprivation.
Molecular Weight

361.44

Formula

C16H15N3O3S2
CAS No.
SMILES

CC1=CSC(C2=CC(NC(CNC(C3=CC=CO3)=O)=O)=C(S2)C)=N1
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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M353-0039 Related Classifications

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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:

M353-00391185074-29-6Urea Transporterhepatic cellsC285UT-BG322MDCK cellsHEK293F cellsmouse modelsUT-A2HepG2 cellsUT-A3Inhibitorinhibitorinhibit

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