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| | TY-52156 Basic information |
| Product Name: | TY-52156 | | Synonyms: | TY-52156;N-(4-chlorophenyl)-N'-(4-chlorophenylamino)-3,3-dimethyl-2-oxobutanamidine;TY52156;TY 52156;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;N'-(4-chloroanilino)-N-(4-chlorophenyl)-3,3-dimethyl-2-oxo-butanamidine;N,N'-bis(4-Chlorophenyl)-3,3-dimethyl-2-oxobutanimidhydrazide;Inhibitor,LPL Receptor,TY-52156,inhibit,Lysophospholipid Receptor,TY 52156,TY52156 | | CAS: | 934369-14-9 | | MF: | C18H19Cl2N3O | | MW: | 364.27 | | EINECS: | | | Product Categories: | | | Mol File: | 934369-14-9.mol |  |
| | TY-52156 Chemical Properties |
| Melting point | 90-91 °C | | Boiling point | 62-69 °C(Press: 20 Torr) | | density | 1.22±0.1 g/cm3(Predicted) | | storage temp. | 2-8°C(protect from light) | | 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 |
| | TY-52156 Usage And Synthesis |
| 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. |
| | TY-52156 Preparation Products And Raw materials |
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