RN 1734

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Cat.No. 3746 - RN 1734 | C14H22Cl2N2O2S | CAS No. 946387-07-1
Description: Selective TRPV4 antagonist
Chemical Name: 2,4-Dichloro-N-isopropyl-N-(2-isopropylaminoethyl)benzenesulfonamide
Datasheet
Citations (7)
Reviews
Literature

Biological Activity

Selective TRPV4 antagonist (IC50 values are 2.3, 3.2 and 5.9 μM for hTRPV4, rTRPV4 and mTRPV4 receptors respectively). Displays selectivity for TRPV4 over other TRP channels (IC50 values are 2.3, >30, >30 and >100 μM for TRPV4, TRPV3, TRPM8 and TRPV1 respectively). Blocks TRPV4-mediated arteriole vasodilation and increases myogenic tone ex vivo.

Compound Libraries

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Technical Data

M. Wt 353.31
Formula C14H22Cl2N2O2S
Storage Store at +4°C
CAS Number 946387-07-1
PubChem ID 3601086
InChI Key IHYZMEAZAIFMTN-UHFFFAOYSA-N
Smiles CC(C)NCCN(C(C)C)S(C1=C(Cl)C=C(Cl)C=C1)(=O)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 35.33 100
ethanol 17.67 50

Preparing Stock Solutions

The following data is based on the product molecular weight 353.31. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.83 mL 14.15 mL 28.3 mL
5 mM 0.57 mL 2.83 mL 5.66 mL
10 mM 0.28 mL 1.42 mL 2.83 mL
50 mM 0.06 mL 0.28 mL 0.57 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Vincent et al (2009) Identification and characterization of novel TRPV4 modulators. Biochem.Biophys.Res.Comms. 389 490 PMID: 19737537

Bagher et al (2012) Low intravascular pressure activates endothelial cell TRPV4 channels, local Ca2+ events, and IKCa channels, reducing arteriolar tone. Proc.Natl.Acad.Sci.U.S.A. 109 18174 PMID: 23071308


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Keywords: RN 1734, supplier, RN1734, selective, TRPV4, antagonists, transient, receptors, potential, channels, vanilloid, TRPV, TRPV, Tocris Bioscience

7 Citations for RN 1734

Citations are publications that use Tocris products. Selected citations for RN 1734 include:

Wei et al (2011) Activation of TRPV4 on dural afferents produces headache-related behavior in a preclinical rat model. PLoS One 31 1595 PMID: 22049072

Feetham et al (2015) The depressor response to intracerebroventricular hypotonic saline is sensitive to TRPV4 antagonist RN1734. Cephalalgia 6 83 PMID: 25954200

Tchieu et al (2017) A modular platform for differentiation of human PSCs into all major ectodermal lineages. Cell Stem Cell. 21 399 PMID: 28886367

Shahidullah et al (2012) TRPV4 in porcine lens epithelium regulates hemichannel-mediated ATP release and Na-K-ATPase activity. Am J Physiol Cell Physiol 302 C1751 PMID: 22492652

Mueller-Tribbensee et al (2015) Differential Contribution of TRPA1, TRPV4 and TRPM8 to Colonic Nociception in Mice. PLoS One 10 e0128242 PMID: 26207981

Shabir et al (2013) Functional expression of purinergic P2 receptors and transient receptor potential channels by the human urothelium. Front Pharmacol 305 F396 PMID: 23720349

Albert et al (2012) TRPV4 channels mediate the infrared laser-evoked response in sensory neurons. J Neurophysiol 107 3227 PMID: 22442563


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Literature in this Area

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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.