2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. TRPC4/5-IN-2

TRPC4/5-IN-2 (Compound 12) is an orally effective transient receptor potential (TRPC5) inhibitor with a IC50 value of 81 nM. TRPC4/5-IN-2 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).

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TRPC4/5-IN-2 Chemical Structure

TRPC4/5-IN-2 Chemical Structure

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TRPC4/5-IN-2 Related Antibodies

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Description

TRPC4/5-IN-2 (Compound 12) is an orally effective transient receptor potential (TRPC5) inhibitor with a IC50 value of 81 nM. TRPC4/5-IN-2 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)[1].
IC50 & Target

TRPC5

 

In Vitro

TRPC4/5-IN-2 (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.

TRPC4/5-IN-2 Related Antibodies

Cell Viability Assay[1].

Cell Line: Hepatocyte, HK-2 cell
Concentration: 3, 10, 30 μM
Incubation Time: 24 h
Result: Didn’t affect cell growth on both primary cultured hepatocytes and HK-2 cells
In Vivo

TRPC4/5-IN-2 (Compound 12) (10 mL/kg, p.o.,) exhibits good pharmacokinetics in male ICR mice, and its low blood-brain barrier penetration rate avoids unnecessary inhibition of TRPC5 activity in the central nervous system [1].
TRPC4/5-IN-2 (Compound 12) (500 mg/kg, p.o.,) exhibits good biosafety in C57 mice[1].
TRPC4/5-IN-2 (Compound 12) (10 mg/kg, p.o., twice daily for 3 weeks) is effective in treating hypotensive renal injury in rats[1].

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

Animal Model: male ICR mice[1].
Dosage: 10 mL/kg
Administration: oral gavage (p.o.)
Result: Was well and rapidly absorbed and mainly distributed in the colon, kidney, and liver[1].
Animal Model: hypertensive renal injury rat model[1].
Dosage: 5, 10 mg/kg
Administration: oral gavage (p.o.)
Result: Suppressed levels of urinary protein and urinary albumin to creatinine ratio (UACR) and attenuated the degree of podocyte injury [1].
Animal Model: C57 mice[1].
Dosage: 10 mL/kg, the final dose is 500 mg/kg
Administration: oral gavage (p.o.)
Result: Didn't cause death or abnormal behavior in mice[1].
Molecular Weight

424.26

Formula

C18H16Cl2FN5O2
SMILES

O=C1C(Cl)=C(N2CCN3C(C2)=NC=C3C(C4=C(Cl)C=C(F)C=C4)OC)C=NN1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TRPC4/5-IN-2 Related Classifications

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

TRPC4/5-IN-2TRP ChannelTransient receptor potential channelsHepatocyteHK-2 cellHEK-293 cellhypertensive renal injury rat modelInhibitorinhibitorinhibit

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