A TRPV4 antagonist (IC50s = 2.3

RN-1734 – 5 mg

Brand:
Cayman
CAS:
946387-07-1
Storage:
-20
UN-No:
Non-Hazardous - /

RN-1734 is a transient receptor potential vanilloid 4 (TRPV4) antagonist, blocking calcium influx induced by the TRPV4 agonist 4α-phorbol 12,13-didecanoate (Item No. 20446) with IC50 values of 2.3, 5.9, and 3.2 µM for human, mouse, and rat TRPV4, respectively.{41579} It is selective for TRPV4 over TRPV1, TRPV3, and TRPM8 (IC50s = >100, >30, and >30 µM, respectively). RN-1734 (10 µM) reduces GSK1016790A-induced increases in glycine-activated current (IGly) from 34.5 to 0.97% in mouse hippocampal neurons in vitro.{41580} It blocks arteriolar dilation induced by GSK1016790A (Item No. 17289) and increases myogenic tone in rat cremaster arterioles ex vivo when used at a concentration of 30 µM.{41581} RN-1734 (1 mg/kg, i.p.) reduces edema and MAPK signaling induced by traumatic brain injury in rats.{41582} It also inhibits breakdown of the blood-retinal barrier in streptozotocin-induced diabetic rats when administered at a dose of 100 µM.{41583}  

 

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SKU: 24205 - 5 mg Category:

Description

A TRPV4 antagonist (IC50s = 2.3, 5.9, and 3.2 µM for human, mouse, and rat, respectively), selective for TRPV4 over TRPV1, TRPV3, and TRPM8 (IC50s = >100, >30, and >30 µM, respectively), reduces GSK1016790A-induced increases in IGly from 34.5 to 0.97% in mouse hippocampal neurons in vitro (10 µM); blocks GSK1016790A-induced arteriolar dilation and increases myogenic tone in rat cremaster arterioles ex vivo (30 µM), reduces edema and MAPK signaling induced by traumatic brain injury in rats (1 mg/kg, i.p.), inhibits breakdown of the blood-retinal barrier in streptozotocin-induced diabetic rats (100 µM)

Formal name: 2,4-dichloro-N-(1-methylethyl)-N-[2-[(1-methylethyl)amino]ethyl]-benzenesulfonamide

Synonyms: 

Molecular weight: 353.3

CAS: 946387-07-1

Purity: ≥98%

Formulation: An oil

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Cardiovascular System|Vasculature|Vasoconstriction||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes||Research Area|Neuroscience

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