YS-49 monohydrate

YS-49 is an anti-inflammatory agent and activator of PI3K/Akt signaling. YS-49 regulates angiotensin II-stimulated ROS production, JNK phosphorylation and vascular smooth muscle cell proliferation via the induction of heme oxygenase-1. YS 49 induced HO-1 protein production in a dose-and time-dependent manner in VSMCs. Treatment with YS 49 significantly and dose-dependently inhibited Ang II-induced VSMC proliferation, ROS production, and phosphorylation of JNK, but not P38 MAP kinase or ERK1/2. YS 49 has potential as a therapeutic strategy for the pathogenesis of Ang II-related vascular diseases such as hypertension and atherosclerosis, via the induction of HO-1 gene activity.

Product information

Molecular Weight: 404.30

Formula: C20H22BrNO3

Synonym:

YS49 monohydrate

YS 49 monohydrate

Related CAS Number:

132836-42-1 (YS-49 HBr)

626252-74-2 (YS-49(S) HBr)

626252-73-1 (YS-49(R) HBr)

Chemical Name: 1-[(naphthalen-1-yl)methyl]-1, 2, 3, 4-tetrahydroisoquinoline-6, 7-diol hydrate hydrobromide

Smiles: O.Br.OC1=CC2CCNC(CC3=CC=CC4=CC=CC=C34)C=2C=C1O

InChiKey: QHCUNMLYODPTIU-UHFFFAOYSA-N

InChi: InChI=1S/C20H19NO2.BrH.H2O/c22-19-11-15-8-9-21-18(17(15)12-20(19)23)10-14-6-3-5-13-4-1-2-7-16(13)14;;/h1-7,11-12,18,21-23H,8-10H2;1H;1H2

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

YS-49 (1-100 μM; 18 hours; RAVSMC and RAW 264.7 cells) concentration-dependently inhibits the accumulation of nitrite in both RAVSMC and RAW 264.7 exposed to lipopolysaccharide (LPS) plus INF-γ, with IC50 values of 22 μM and 30 μM, respectively. YS-49 (10-100 μM; 18 hours; RAVSMC and RAW 264.7 cells) suppresses iNOS gene expression induced by LPS and/or cytokines in RAVSMC and RAW 264.7 cells at the transcriptional level.

In Vivo:

YS-49 (5 mg/kg; intraperitoneal injection; 8 hours; male Sprague Dawley rats) treatment significantly reduces serum NOx levels in LPS-treated rats, the NOx levels reduce from 86 μM to 34 μM.

References:

1. Sun JJ, et al. YS 49, 1-(alpha-naphtylmethyl)-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline, regulates angiotensin II-stimulated ROS production, JNK phosphorylation and vascular smooth muscle cell proliferation via the induction of heme oxygenase-1. Life Sci. 2008 Mar 12;82(11-12):600-7.
2. Kang YJ, et al. Prevention of the expression of inducible nitric oxide synthase by a novel positive inotropic agent, YS 49, in rat vascular smooth muscle and RAW 264.7 macrophages. Br J Pharmacol. 1999 Sep;128(2):357-64.
3. Hsu YH, et al. RhoA-mediated inhibition of vascular endothelial cell mobility: positive feedback through reduced cytosolic p21 and p27. J Cell Physiol. 2014 Oct;229(10):1455-65.

Products are for research use only. Not for human use.