Home >> Research Area >>GPCR/G protein>>Sphingosine>> CYM 5442 hydrochloride

CYM 5442 hydrochloride

Selective S1P1 receptor agonist CAS# 1094042-01-9

CYM 5442 hydrochloride

Catalog No. BCC7722----Order now to get a substantial discount!

Product Name & Size Price Stock
CYM 5442 hydrochloride: 5mg $127 In Stock
CYM 5442 hydrochloride: 10mg Please Inquire In Stock
CYM 5442 hydrochloride: 20mg Please Inquire Please Inquire
CYM 5442 hydrochloride: 50mg Please Inquire Please Inquire
CYM 5442 hydrochloride: 100mg Please Inquire Please Inquire
CYM 5442 hydrochloride: 200mg Please Inquire Please Inquire
CYM 5442 hydrochloride: 500mg Please Inquire Please Inquire
CYM 5442 hydrochloride: 1000mg Please Inquire Please Inquire
Related Products

Quality Control of CYM 5442 hydrochloride

Number of papers citing our products

Chemical structure

CYM 5442 hydrochloride

3D structure

Chemical Properties of CYM 5442 hydrochloride

Cas No. 1094042-01-9 SDF Download SDF
PubChem ID 25110406 Appearance Powder
Formula C23H27N3O4 M.Wt 409.5
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 10 mM in water and to 100 mM in DMSO
Chemical Name 2-[[4-[5-(3,4-diethoxyphenyl)-1,2,4-oxadiazol-3-yl]-2,3-dihydro-1H-inden-1-yl]amino]ethanol
SMILES CCOC1=C(C=C(C=C1)C2=NC(=NO2)C3=C4CCC(C4=CC=C3)NCCO)OCC
Standard InChIKey NUIKTBLZSPQGCP-UHFFFAOYSA-N
Standard InChI InChI=1S/C23H27N3O4/c1-3-28-20-11-8-15(14-21(20)29-4-2)23-25-22(26-30-23)18-7-5-6-17-16(18)9-10-19(17)24-12-13-27/h5-8,11,14,19,24,27H,3-4,9-10,12-13H2,1-2H3
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of CYM 5442 hydrochloride

DescriptionPotent and selective S1P1 agonist in vitro (EC50 = 1.35 nM). Activates S1P1-mediated p42/p44 MAPK phosphorylation in CHO-K1 cells transfected with S1P1. Induces acute lymphopenia in mice. Brain penetrant.

CYM 5442 hydrochloride Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

CYM 5442 hydrochloride Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Preparing Stock Solutions of CYM 5442 hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.442 mL 12.21 mL 24.42 mL 48.84 mL 61.0501 mL
5 mM 0.4884 mL 2.442 mL 4.884 mL 9.768 mL 12.21 mL
10 mM 0.2442 mL 1.221 mL 2.442 mL 4.884 mL 6.105 mL
50 mM 0.0488 mL 0.2442 mL 0.4884 mL 0.9768 mL 1.221 mL
100 mM 0.0244 mL 0.1221 mL 0.2442 mL 0.4884 mL 0.6105 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
Deemed University
Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University
Featured Products
New Products
 

References on CYM 5442 hydrochloride

Full pharmacological efficacy of a novel S1P1 agonist that does not require S1P-like headgroup interactions.[Pubmed:18708635]

Mol Pharmacol. 2008 Nov;74(5):1308-18.

Strong evidence exists for interactions of zwitterionic phosphate and amine groups in sphingosine-1 phosphate (S1P) to conserved Arg and Glu residues present at the extracellular face of the third transmembrane domain of S1P receptors. The contribution of Arg(120) and Glu(121) for high-affinity ligand-receptor interactions is essential, because single-point R(120)A or E(121)A S1P(1) mutants neither bind S1P nor transduce S1P function. Because S1P receptors are therapeutically interesting, identifying potent selective agonists with different binding modes and in vivo efficacy is of pharmacological importance. Here we describe a modestly water-soluble highly selective S1P(1) agonist [2-(4-(5-(3,4-diethoxyphenyl)-1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-inden-1-yl amino) ethanol (CYM-5442)] that does not require Arg(120) or Glu(121) residues for activating S1P(1)-dependent p42/p44 mitogen-activated protein kinase phosphorylation, which defines a new hydrophobic pocket in S1P(1). CYM-5442 is a full agonist in vitro for S1P(1) internalization, phosphorylation, and ubiquitination. It is noteworthy that CYM-5442 was a full agonist for induction and maintenance of S1P(1)-dependent blood lymphopenia, decreasing B lymphocytes by 65% and T lymphocytes by 85% of vehicle. Induction of CYM-5442 lymphopenia was dose- and time-dependent, requiring serum concentrations in the 50 nM range. In vitro measures of S1P(1) activation by CYM-5442 were noncompetitively inhibited by a specific S1P(1) antagonist [(R)-3-amino-(3-hexylphenylamino)-4-oxobutylphosphonic acid (W146)], competitive for S1P, 2-amino-2-(4-octylphenethyl)propane-1,3-diol (FTY720-P), and 5-[4-phenyl-5-(trifluoromethyl)-2-thienyl]-3-[3-(trifluoromethyl)phenyl]-1,2, 4-oxadiazole (SEW2871). In addition, lymphopenia induced by CYM-5442 was reversed by W146 administration or upon pharmacokinetic agonist clearance. Pharmacokinetics in mice also indicated that CYM-5442 partitions significantly in central nervous tissue. These data show that CYM-5442 activates S1P(1)-dependent pathways in vitro and to levels of full efficacy in vivo through a hydrophobic pocket separate from the orthosteric site of S1P binding that is headgroup-dependent.

Description

CYM5442 is a potent, highly-selective and orally active sphingosine 1-phosphate (S1P1) receptor agonist with an EC50 of 1.35 nM. CYM5442 is inactive against S1P2, S1P3, S1P4, and S1P5. CYM5442 activates S1P1-dependent p42/p44-MAPK phosphorylation. CYM5442 exerts retinal neuroprotection. CYM5442 can easily penetrate the central nervous system (CNS).

Keywords:

CYM 5442 hydrochloride,1094042-01-9,Natural Products,Sphingosine, buy CYM 5442 hydrochloride , CYM 5442 hydrochloride supplier , purchase CYM 5442 hydrochloride , CYM 5442 hydrochloride cost , CYM 5442 hydrochloride manufacturer , order CYM 5442 hydrochloride , high purity CYM 5442 hydrochloride

Online Inquiry for:

      Fill out the information below

      • Size:Qty: - +

      * Required Fields

                                      Result: