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Submit ReviewRN 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.
RN 1734 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 353.31 |
公式 | C14H22Cl2N2O2S |
储存 | 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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 35.33 | 100 | |
ethanol | 17.67 | 50 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for RN 1734, please let us know.
关键词: RN 1734, RN 1734 supplier, RN1734, selective, TRPV4, antagonists, transient, receptors, potential, channels, vanilloid, TRPV, 3746, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 RN 1734 的部分引用包括:
Joon W et al (2020) TRPV4 antagonists ameliorate ventriculomegaly in a rat model of hydrocephalus. JCI Insight 5 PMID: 32938829
Stephen J et al (2020) TRPV4 channel opening mediates pressure-induced pancreatitis initiated by Piezo1 activation. J Clin Invest 130 2527-2541 PMID: 31999644
Feetham et al (2015) The depressor response to intracerebroventricular hypotonic saline is sensitive to TRPV4 antagonist RN1734. Cephalalgia 6 83 PMID: 25954200
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
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
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
Tchieu et al (2017) A modular platform for differentiation of human PSCs into all major ectodermal lineages. Cell Stem Cell. 21 399 PMID: 28886367
Francisco et al (2015) Co-administration of transient receptor potential vanilloid 4 (TRPV4) and TRPV1 antagonists potentiate the effect of each drug in a rat model of cystitis. BJU Int 115 452-60 PMID: 25041193
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
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
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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