TY 52156
目录号 : GC13720
A S1P3 receptor antagonist
Cas No.:934369-14-9
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 934369-14-9 | SDF | |
| 化学名 | N-(4-chlorophenyl)-3,3-dimethyl-2-oxobutanimidic acid, 2-(4-chlorophenyl)hydrazide | ||
| Canonical SMILES | CC(C)(C)C(/C(NNC1=CC=C(Cl)C=C1)=N/C2=CC=C(Cl)C=C2)=O | ||
| 分子式 | C18H19Cl2N3O | 分子量 | 364.3 |
| 溶解度 | ≤15mg/ml in ethanol;25mg/ml in DMSO;30mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.745 mL | 13.725 mL | 27.4499 mL |
| 5 mM | 0.549 mL | 2.745 mL | 5.49 mL |
| 10 mM | 0.2745 mL | 1.3725 mL | 2.745 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet