★【medlife】1-(4-Chlorophenylamino)-1-(4-chlorophenylhydrazono)-3,3-dimethyl-2-butanone 生物.医药.天然产物

★【medlife】1-(4-Chlorophenylamino)-1-(4-chlorophenylhydrazono)-3,3-dimethyl-2-butanone

2024年04月11日 17:29 生物.医药.天然产物

关键词： 1-(4-Chlorophenylamino)-1-(4-chlorophenylhydrazono)-3,3-dimethyl-2-butanone

鞘氨醇-1-磷酸受体3（SIP3）拮抗剂,TY-52156是一种有效的S1P3受体拮抗剂，作用于S1P3受体Ki值为110 nM。
中文名称
TY 52156
中文别名
TY-52156
英文名称
TY 52156
英文别名
TY 52156;TY-52156;1-(4-Chlorophenylamino)-1-(4-chlorophenylhydrazono)-3,3-dimethyl-2-butanone;1-(4-Chlorophenylhydrazono)-1-(4-chlorophenylamino)-3,3-dimethyl-2-butanone;N-(4-Chloroanilino)-N′-(4-chlorophenyl)-3,3-dimethyl-2-oxobutanimidamide;TY52156
Cas No.
934369-14-9
分子式
C18N3OCl2H19
分子量
364.27
包装储存
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

生物活性

TY-52156 is a potent and selective S1P₃ receptor antagonist with a K_i value of 110 nM.

性状

Solid

IC50 & Target[1][2]

Ki: 110 nM (S1P₃)

体外研究(In Vitro)

TY-52156 inhibits the S1P₃ receptor-dependent increase in [Ca]_i.
TY-52156 shows submicromolar potency and a high degree of selectivity for S1P₃ receptor.
TY-52156 (10 μM; 10 min) inhibits S1P-induced p44/p42 MAPK phosphorylation.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell Line:

Chinese hamster ovary K1 cells

Concentration:

10 μM

Incubation Time:

10 min

Result:

Inhibited S1P-induced p44/p42 MAPK phosphorylation.

体内研究(In Vivo)

TY-52156 (10 mg/kg, 30 mg/kg; p.o.) suppresses S1P₃ receptor-induced bradycardia after oral administration in vivo.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male SD rats (290–340 g)

Dosage:

10 mg/kg, 30 mg/kg

Administration:

Oral administration

Result:

Inhibited S1P₃ receptor-induced bradycardia after oral administration in vivo.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder

-20°C

3 years

4°C

2 years

In solvent

-80°C

6 months

-20°C

1 month

参考文献

[1]. Murakami A, et al. Sphingosine 1-phosphate (S1P) regulates vascular contraction via S1P3 receptor: investigation based on a new S1P3 receptor antagonist. Mol Pharmacol. 2010 Apr;77(4):704-13. [Information]

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