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Chemical Structure| 946387-07-1 Chemical Structure| 946387-07-1
Chemical Structure| 946387-07-1

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CAS No.: 946387-07-1

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RN-1734 is selective antagonist of the TRPV4 channel, completely antagonizes 4αPDD-mediated activation of TRPV4 with comparable, low micromolar IC50 values for all three species (hTRPV4: IC50 = 2.3 μM, mTRPV4: IC50 = 5.9 μM, rTRPV4: IC50 = 3.2 μM).

Synonyms: TRPV4 Antagonist I

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Product Details of RN-1734

CAS No. :946387-07-1
Formula : C14H22Cl2N2O2S
M.W : 353.31
SMILES Code : O=S(C1=CC=C(Cl)C=C1Cl)(N(C(C)C)CCNC(C)C)=O
Synonyms :
TRPV4 Antagonist I
MDL No. :MFCD00129453
InChI Key :IHYZMEAZAIFMTN-UHFFFAOYSA-N
Pubchem ID :3601086

Safety of RN-1734

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description Reference
Oligodendrocytes 10 μM 24 h RN-1734 alleviated apoptosis of oligodendrocyte induced by LPS-activated microglia. PMC6230558
Microglial cells 10 μM 3 h RN-1734 clearly inhibited the influx of calcium and decreased the levels of IL-1β and TNF-α in LPS-activated microglial cells by suppressing NF-κB P65 phosphorylation. PMC6230558
M1 macrophages 10 μM 24 h To investigate the effect of RN-1734 on the polarization of M1 macrophages within 3D collagen matrices, results showed that TRPV4 inhibition partially mitigated inflammation, particularly under 6% mechanical strain, significantly reducing pro-inflammatory gene expression and increasing anti-inflammatory markers such as CD206. PMC11756524
Human coronary artery endothelial cells (HCAECs) 3 μM 5 min To investigate whether AA increases intracellular Ca2+ concentration in endothelial cells through TRPV4 channels. The results showed that AA significantly increased Ca2+ concentration in HCAECs via TRPV4-dependent Ca2+ entry. PMC3698766
U937-differentiated macrophages 10 μM 48 h To validate the effectiveness of RN-1734 as a TRPV4 antagonist, results showed that 10 μM concentration did not affect cell viability PMC10813551

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
C57BL/6 mice Cuprizone-induced demyelination model Lateral ventricle injection 10 mM Daily for 5 weeks RN-1734 clearly alleviated demyelination, inhibited glial activation and the production of TNF-α and IL-1β without altering the number of olig2-positive cells. PMC6230558

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.83mL

0.57mL

0.28mL

14.15mL

2.83mL

1.42mL

28.30mL

5.66mL

2.83mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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