| Identification | Back Directory | [Name]
TY-52156 | [CAS]
934369-14-9 | [Synonyms]
TY-52156
TY52156;TY 52156
N'-(4-chloroanilino)-N-(4-chlorophenyl)-3,3-dimethyl-2-oxo-butanamidine
N-(4-chlorophenyl)-N'-(4-chlorophenylamino)-3,3-dimethyl-2-oxobutanamidine
N-(4-Chlorophenyl)-3,3-dimethyl-2-oxobutanimidic 2-(4-chlorophenyl) hydrazide
Butanimidic acid, N-(4-chlorophenyl)-3,3-dimethyl-2-oxo-, 2-(4-chlorophenyl)hydrazide | [Molecular Formula]
C18H19Cl2N3O | [MDL Number]
MFCD30182278 | [MOL File]
934369-14-9.mol | [Molecular Weight]
364.27 |
| Chemical Properties | Back Directory | [Melting point ]
90-91 °C | [Boiling point ]
62-69 °C(Press: 20 Torr) | [density ]
1.22±0.1 g/cm3(Predicted) | [storage temp. ]
Keep in dark place,Sealed in dry,2-8°C | [solubility ]
≥92.8 mg/mL in DMSO; ≥94.6 mg/mL in EtOH; insoluble in H2O | [form ]
crystalline solid | [pka]
0.99±0.50(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
TY 52156 is a sphingosine-1-phosphate receptor subtype 3 (S1PR3) antagonist, which is used for the treatment of lung cancer. | [Definition]
ChEBI: TY 52156 is an imidohydrazide resulting from the formal condensation of the hydrazide carbonyl group of N'-(p-chlorophenyl)-3,3-dimethyl-2-oxobutanehydrazide with the amino group of p-chloroaniline. A potent and selective antagonist of sphingosine-1-phosphate receptor 3 (S1PR3). It has a role as a sphingosine-1-phosphate receptor 3 antagonist. It is a member of monochlorobenzenes and an imidohydrazide. | [Biological Activity]
ty 52156 (1-(4-chlorophenylhydrazono)-1-(4-chlorophenylamino)-3,3-dimethyl-2-butanone) is a novel s1p3 receptor antagonist [1].sphingosine 1-phosphate (s1p) is a bioactive lysophospholipid mediator mainly released from activated platelets and implicated in many biological responses, such as angiogenesis, vascular development, and cardiovascular function [1]. | [in vitro]
ty-52156 preferentially inhibited the s1p-induced increase in [ca2+]i in s1p3-cho cells. ty-52156 competitively inhibited the dose-dependent [ca2+]i increase elicited by s1p in s1p3-cho with the ki value of ～110 nm for s1p3 receptor. ty-52156 showed submicromolar potency and a high degree of selectivity for s1p3 receptor. ty-52156 (10 μm) inhihbited 24 gpcrs and three ion channels by 〈 30%. s1p dose-dependently decreased cf (coronary flow) in perfused rat heart. s1p dose-dependently induced vasoconstriction in isolated canine cerebral arteries. in hcasmcs, ty-52156 inhibited s1p-induced rho activation. | [in vivo]
in sd rats, oral bioavailability of ty-52156 was ～70.9%. in rats, pretreatment with ty-52156 significantly attenuated fty-720-induced bradycardia, a broad agonist of s1p receptors. pretreatment with ty-52156 prevented the fty-720-p-induced increase in [ca2+]i in a dose-dependent manner. | [storage]
Store at -20°C | [References]
[1] murakami a, takasugi h, ohnuma s, et al. sphingosine 1-phosphate (s1p) regulates vascular contraction via s1p3 receptor: investigation based on a new s1p3 receptor antagonist[j]. molecular pharmacology, 2010, 77(4): 704-713. |
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| Company Name: |
Tcichem, Inc.
|
| Tel: |
13918644899 |
| Website: |
http://m.is0513.com/ShowSupplierProductsList19113/0.htm |
| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
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