C4797-50mg | TY 52156 [934369-14-9] Biotrend

Background

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.

Reference:
[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.

Chemical Properties

Physical Appearance	A crystalline solid
Storage	Store at -20°C
M.Wt	364.3
Cas No.	934369-14-9
Formula	C₁₈H₁₉Cl₂N₃O
Solubility	≥92.8 mg/mL in DMSO; ≥94.6 mg/mL in EtOH; insoluble in H2O
Chemical Name	N-(4-chlorophenyl)-3,3-dimethyl-2-oxobutanimidic acid, 2-(4-chlorophenyl)hydrazide
SDF	Download SDF
Canonical SMILES	CC(C)(C)C(/C(NNC1=CC=C(Cl)C=C1)=N/C2=CC=C(Cl)C=C2)=O
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Purity = 99.89%

Chemical structure

TY 52156 [934369-14-9]

Katalog-Nummer C4797-50mg

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Marke : ApexBio Technology

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Background

Chemical Properties

Quality Control

Chemical structure