TY-52156
- Product Name
- TY-52156
- CAS No.
- 934369-14-9
- Chemical Name
- TY-52156
- Synonyms
- TY-52156;TY52156;TY 52156;N,N'-bis(4-Chlorophenyl)-3,3-dimethyl-2-oxobutanimidhydrazide;N,N'-bis(4-Chlorophenyl)-3,3-dimethyl-2-oxobutanimidhydrazide;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;N'-(4-chlorophenyl)-N-[(4-chlorophenyl)amino]-3,3-dimethyl-2-oxobutanimidamide;Inhibitor,LPL Receptor,TY-52156,inhibit,Lysophospholipid Receptor,TY 52156,TY52156;Butanimidic acid, N-(4-chlorophenyl)-3,3-dimethyl-2-oxo-, 2-(4-chlorophenyl)hydrazide
- CBNumber
- CB73122351
- Molecular Formula
- C18H19Cl2N3O
- Formula Weight
- 364.27
- MOL File
- 934369-14-9.mol
TY-52156 Property
- 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
N-Bromosuccinimide Price
- Product number
- SML2499
- Product name
- TY-52156
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $115
- Updated
- 2024/03/01
- Product number
- SML2499
- Product name
- TY-52156
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $462
- Updated
- 2024/03/01
- Product number
- 19119
- Product name
- TY 52156
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 19119
- Product name
- TY 52156
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $139
- Updated
- 2024/03/01
- Product number
- 19119
- Product name
- TY 52156
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $184
- Updated
- 2024/03/01
TY-52156 Chemical Properties,Usage,Production
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
Raw materials
Preparation Products
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