RN 1734
Chemical Name: 2,4-Dichloro-N-isopropyl-N-(2-isopropylaminoethyl)benzenesulfonamide
Biological Activity
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.Technical Data
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.
Background References
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Low intravascular pressure activates endothelial cell TRPV4 channels, local Ca2+ events, and IKCa channels, reducing arteriolar tone.
Bagher et al.
Proc.Natl.Acad.Sci.U.S.A., 2012;109:18174 -
Identification and characterization of novel TRPV4 modulators.
Vincent et al.
Biochem.Biophys.Res.Comms., 2009;389:490 -
Androgen Signaling Regulates SARS-CoV-2 Receptor Levels and Is Associated with Severe COVID-19 Symptoms in Men
RM Samuel, H Majd, MN Richter, Z Ghazizadeh, SM Zekavat, A Navickas, JT Ramirez, H Asgharian, CR Simoneau, LR Bonser, KD Koh, M Garcia-Kni, M Tassetto, S Sunshine, S Farahvashi, A Kalantari, W Liu, R Andino, H Zhao, P Natarajan, DJ Erle, M Ott, H Goodarzi, F Fattahi
Cell Stem Cell, 2020;27(6):876-889.e12.
Product Datasheets
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Citations for RN 1734
The citations listed below are publications that use Tocris products. Selected citations for RN 1734 include:
14 Citations: Showing 1 - 10
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TRPV4 antagonists ameliorate ventriculomegaly in a rat model of hydrocephalus.
Authors: Joon W Et al.
JCI Insight 2020;5
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TRPV4 channel opening mediates pressure-induced pancreatitis initiated by Piezo1 activation.
Authors: Stephen J Et al.
J Clin Invest 2020;130:2527-2541
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TRPV4 is the temperature-sensitive ion channel of human sperm.
Authors: Mundt Et al.
Elife 2018;7
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Involvement of VNUT-exocytosis in transient receptor potential vanilloid 4-dependent ATP release from gastrointestinal epithelium.
Authors: Mihara Et al.
PLoS One 2018;13:e0206276
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A modular platform for differentiation of human PSCs into all major ectodermal lineages.
Authors: Tchieu Et al.
Cell Stem Cell. 2017;21:399
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The depressor response to intracerebroventricular hypotonic saline is sensitive to TRPV4 antagonist RN1734.
Authors: Feetham Et al.
Cephalalgia 2015;6:83
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TRPV4 activates autonomic and behavioural warmth-defence responses in Wistar rats.
Authors: Vizin Et al.
Acta Physiol 2015;214:275
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Co-administration of transient receptor potential vanilloid 4 (TRPV4) and TRPV1 antagonists potentiate the effect of each drug in a rat model of cystitis.
Authors: Francisco Et al.
BJU Int 2015;115:452-60
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Differential Contribution of TRPA1, TRPV4 and TRPM8 to Colonic Nociception in Mice.
Authors: Mueller-Tribbensee Et al.
PLoS One 2015;10:e0128242
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Functional expression of purinergic P2 receptors and transient receptor potential channels by the human urothelium.
Authors: Shabir Et al.
Front Pharmacol 2013;305:F396
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The increased activity of TRPV4 channel in the astrocytes of the adult rat hippocampus after cerebral hypoxia/ischemia.
Authors: Butenko Et al.
PLoS One 2012;7:e39959
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TRPV4 in porcine lens epithelium regulates hemichannel-mediated ATP release and Na-K-ATPase activity.
Authors: Shahidullah Et al.
Am J Physiol Cell Physiol 2012;302:C1751
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TRPV4 channels mediate the infrared laser-evoked response in sensory neurons.
Authors: Albert Et al.
J Neurophysiol 2012;107:3227
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Activation of TRPV4 on dural afferents produces headache-related behavior in a preclinical rat model.
Authors: Wei Et al.
PLoS One 2011;31:1595
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