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Description: Selective TRPV4 antagonist
Chemical Name: 2,4-Dichloro-N-isopropyl-N-(2-isopropylaminoethyl)benzenesulfonamide
Biological Activity for RN 1734
RN 1734 is a 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 for RN 1734
RN 1734 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for RN 1734
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for RN 1734
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 35.33 | 100 | |
| ethanol | 17.67 | 50 |
Preparing Stock Solutions for RN 1734
The following data is based on the product molecular weight 353.31. Batch specific molecular weights may vary from batch to batch due to the degree 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 for RN 1734
References for RN 1734
References are publications that support the biological activity of the product.
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, RN 1734 supplier, RN1734, selective, TRPV4, antagonists, transient, receptors, potential, channels, vanilloid, TRPV, 3746, Tocris Bioscience
11 Citations for RN 1734
Citations are publications that use Tocris products. Selected citations for RN 1734 include:
Tchieu et al (2017) A modular platform for differentiation of human PSCs into all major ectodermal lineages. Cell Stem Cell. 21 399 PMID: 28886367
Feetham et al (2015) The depressor response to intracerebroventricular hypotonic saline is sensitive to TRPV4 antagonist RN1734. Cephalalgia 6 83 PMID: 25954200
Albert et al (2012) TRPV4 channels mediate the infrared laser-evoked response in sensory neurons. J Neurophysiol 107 3227 PMID: 22442563
Butenko et al (2012) The increased activity of TRPV4 channel in the astrocytes of the adult rat hippocampus after cerebral hypoxia/ischemia. PLoS One 7 e39959 PMID: 22761937
Mundt et al (2018) TRPV4 is the temperature-sensitive ion channel of human sperm. Elife 7 PMID: 29963982
Mihara et al (2018) Involvement of VNUT-exocytosis in transient receptor potential vanilloid 4-dependent ATP release from gastrointestinal epithelium. PLoS One 13 e0206276 PMID: 30365528
Mueller-Tribbensee et al (2015) Differential Contribution of TRPA1, TRPV4 and TRPM8 to Colonic Nociception in Mice. PLoS One 10 e0128242 PMID: 26207981
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
Vizin et al (2015) TRPV4 activates autonomic and behavioural warmth-defence responses in Wistar rats. Acta Physiol 214 275 PMID: 25739906
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
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
Do you know of a great paper that uses RN 1734 from Tocris? Please let us know.
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Literature in this Area
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Pain Research Product Guide
A collection of over 280 products for pain research, the guide includes research tools for the study of:
- Nociception
- Ion Channels
- G-Protein-Coupled Receptors
- Intracellular Signaling
Pain Poster
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.