TRPC5-IN-6
TRPC5-IN-6 (Compound 12) is an orally effective transient receptor potential (TRPC5) inhibitor with a IC50 value of 81 nM. TRPC5-IN-6 has good biosafety and low liver and kidney toxicity, and is expected to play an important role in the treatment of chronic kidney disease (CKD).
For research use only. We do not sell to patients.
- CAS No.: 3047956-65-7
- Formula: C18H16Cl2FN5O2
- Molecular Weight:424.26
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
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TRPC5 |
In Vitro
TRPC5-IN-6 (Compound 12) (30 μM, 24 h) shows low toxicity on liver cells and HK-2 kidney cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Hepatocyte, HK-2 cell
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Concentration:3, 10, 30 μM
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Incubation Time:24 h
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Result:Didn’t affect cell growth on both primary cultured hepatocytes and HK-2 cells
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:male ICR mice[1].
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Dosage:10 mL/kg
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Administration:oral gavage (p.o.)
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Result:Was well and rapidly absorbed and mainly distributed in the colon, kidney, and liver[1].
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Animal Model:hypertensive renal injury rat model[1].
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Dosage:5, 10 mg/kg
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Administration:oral gavage (p.o.)
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Result:Suppressed levels of urinary protein and urinary albumin to creatinine ratio (UACR) and attenuated the degree of podocyte injury [1].
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Animal Model:C57 mice[1].
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Dosage:10 mL/kg, the final dose is 500 mg/kg
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Administration:oral gavage (p.o.)
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Result:Didn't cause death or abnormal behavior in mice[1].
Chemical Information
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CAS No. 3047956-65-7
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Molecular Weight 424.26
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Formula C18H16Cl2FN5O2
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SMILES
O=C1C(Cl)=C(N2CCN3C(C2)=NC=C3C(C4=C(Cl)C=C(F)C=C4)OC)C=NN1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Nephrotoxicity Study
This protocol assesses nephrotoxicity by combining functional kidney injury readouts, urinary/tissue injury biomarkers, and renal histopathology. Serum creatinine and BUN reflect impaired kidney function, while KIM-1, NGAL, clusterin, osteopontin, IL-18, cystatin C, nephrin, Oat5, urinary protein, glucose, and alkaline phosphatase have been used to detect tubular injury in cisplatin-, gentamicin-, and acetaminophen-induced nephrotoxicity models.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)