TRPC4/5-IN-2

Name: TRPC4/5-IN-2
Brand: TargetMol
SKU: T210278
Rating: 4.5 (1 reviews)

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Catalog No. T210278

TRPC4/5-IN-2 (Compound 12) is an orally active transient receptor potential (TRPC5) inhibitor with an IC50 value of 81 nM. This compound exhibits good biosafety and low hepatic and renal toxicity, making it a promising candidate for the treatment of chronic kidney disease (CKD).

TRPC4/5-IN-2

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Catalog No. T210278

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Product Introduction

Bioactivity

Description	TRPC4/5-IN-2 (Compound 12) is an orally active transient receptor potential (TRPC5) inhibitor with an IC50 value of 81 nM. This compound exhibits good biosafety and low hepatic and renal toxicity, making it a promising candidate for the treatment of chronic kidney disease (CKD).
In vitro	TRPC4/5-IN-2 (Compound 12) exhibits low cytotoxicity towards liver cells and HK-2 renal cells at a concentration of 30 μM over a 24-hour period.
In vivo	TRPC4/5-IN-2 (Compound 12) demonstrates favorable pharmacokinetics in male ICR mice at a dosage of 10 mL/kg administered orally, with a low blood-brain barrier penetration rate that minimizes the risk of unnecessary TRPC5 inhibition in the central nervous system. In C57 mice, TRPC4/5-IN-2 (Compound 12) shows good biosafety when given orally at 500 mg/kg. Additionally, TRPC4/5-IN-2 (Compound 12) administered orally at 10 mg/kg twice daily for three weeks effectively treats hypotensive-induced kidney injury in rats.

Chemical Properties

Formula

C₁₈H₁₆Cl₂FN₅O₂

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

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