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Art. -Nr.: HY-162584

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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).

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CAS. Nr.: 3047956-65-7
Formel: C₁₈H₁₆Cl₂FN₅O₂
Molecular Weight:424.26

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

TRPC5-IN-6 Chemical Structure

CAS. Nr.: 3047956-65-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

TRPC5

Alle TRP Channel Isoform-spezifische Produkte anzeigen :

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.

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

TRPC5-IN-6 (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].
TRPC5-IN-6 (Compound 12) (500 mg/kg, p.o.,) exhibits good biosafety in C57 mice^[1].
TRPC5-IN-6 (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].

Chemical Information

CAS. Nr. 3047956-65-7
Molecular Weight 424.26
Formel C₁₈H₁₆Cl₂FN₅O₂
SMILES

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

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Xu Yuanyuan, et al. Discovery of pyridazinone derivatives bearing tetrahydroimidazo[1,2-a] pyrazine scaffold as potent inhibitors of transient receptor potential canonical 5 to ameliorate hypertension-induced renal injury in rats. Eur.J.Med.Chem. 2024, 275:116565.

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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TRPC5-IN-6

Alle TRP Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

TRPC5-IN-6 Related Classifications

HY-162584 Related Classifications