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TY 52156

 
Catalog No.
C4797
鞘氨醇-1-磷酸受体3(SIP3)拮抗剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,069.00
现货
5mg
¥ 973.00
现货
10mg
¥ 1,603.00
现货
25mg
¥ 3,608.00
现货
50mg
¥ 6,414.00
现货
100mg
¥ 10,881.00
Ship with 10-15 days

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A

背景

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.

化学属性

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt364.3
Cas No.934369-14-9
FormulaC18H19Cl2N3O
Solubility≥92.8 mg/mL in DMSO; ≥94.6 mg/mL in EtOH; insoluble in H2O
Chemical NameN-(4-chlorophenyl)-3,3-dimethyl-2-oxobutanimidic acid, 2-(4-chlorophenyl)hydrazide
SDFDownload SDF
Canonical SMILESCC(C)(C)C(/C(NNC1=CC=C(Cl)C=C1)=N/C2=CC=C(Cl)C=C2)=O
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