RN-1734

RN-1734 is a transient receptor potential vanilloid 4 (TRPV4) antagonist, blocking calcium influx induced by the TRPV4 agonist 4alpha-phorbol 12,13-didecanoate (Cay-20446) with IC50 values of 2.3, 5.9, and 3.2 µM for human, mouse, and rat TRPV4, respectively. 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. It blocks arteriolar dilation induced by GSK1016790A (Cay-17289) and increases myogenic tone in rat cremaster arterioles ex vivo when used at a concentration of 30 µM. RN-1734 (1 mg/kg, i.p.) reduces edema and MAPK signaling induced by traumatic brain injury in rats. It also inhibits breakdown of the blood-retinal barrier in streptozotocin-induced diabetic rats when administered at a dose of 100 µM.Formal Name: 2,4-dichloro-N-(1-methylethyl)-N-[2-[(1-methylethyl)amino]ethyl]-benzenesulfonamide. CAS Number: 946387-07-1. Molecular Formula: C14H22Cl2N2O2S. Formula Weight: 353.3. Purity: >98%. Formulation: (Request formulation change), An oil. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml, Ethanol: 2 mg/ml. lambdamax: 207, 238 nm. SMILES: ClC1=CC(Cl)=C(S(N(C(C)C)CCNC(C)C)(=O)=O)C=C1. InChi Code: InChI=1S/C14H22Cl2N2O2S/c1-10(2)17-7-8-18(11(3)4)21(19,20)14-6-5-12(15)9-13(14)16/h5-6,9-11,17H,7-8H2,1-4H3. InChi Key: IHYZMEAZAIFMTN-UHFFFAOYSA-N.