BMS 182874 hydrochloride
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Ki值:对VSM-A10细胞中的ETA为61 nM;对CHO细胞中的ETA为48 nM.
内皮素(ET)最初被鉴定为内皮细胞分泌的有效的血管活性物质,在分离的猪冠状动脉中可刺激力量发育.ET-1属于高度保守的21氨基酸多肽家族,在多个组织中分泌,包括肺\肾\眼\肠和中枢神经系统.BMS-182874是一种小分子量的非肽内皮素(El)受体拮抗剂.
体外实验:BMS-182874可竞争性抑制[125I]ET-1与大鼠血管平滑肌A10(VSM-A10)细胞膜上和稳定表达人类ETA受体的CHO细胞中ETA受体的结合,Ki值分别为61 nM和48 nM,但对ETB受体(Ki > 50 μM)和非ET受体是弱抑制剂.在VSM-A10细胞中,BMS-l 82874抑制ET-l刺激的肌醇磷酸积累(KB 75 nM)和钙动员(Ki = 140 nM),但不影响最大反应[1].
体内实验:有意识的血压正常的大鼠口服(ED50 = 30 μmol/kg)或静脉注射(ED50 = 24 μmol/kg),BMS-182874可钝化对外源ET-l的压力响应.这些数据证明BMS-l 82874是一种具有竞争性\选择性的和口服活性的ETA受体拮抗剂[1].
临床试验:迄今为止,BMS 182874 hydrochloride仍处于临床前开发阶段.
参考文献:
[1] MARIA L WEBB, J. EILEEN BIRD, EDDIE C. K. LIU, PATRICIA M. ROSE, RANDY SERAFINO, PHILIP D. STEIN and SUZANNE MORELAND. BMS-182874 is a selective, nonpeptide endothelin ETA receptor antagonist. JPET 272:1124-1134, 1995.
Physical Appearance | White crystalline solid |
Storage | Store at RT |
M.Wt | 381.88 |
Cas No. | 1215703-04-0 |
Formula | C17H19N3O3S·HCl |
Solubility | Soluble to 100 mM in DMSO |
Chemical Name | 5-(dimethylamino)-N-(3,4-dimethylisoxazol-5-yl)naphthalene-1-sulfonamide hydrochloride |
SDF | Download SDF |
Canonical SMILES | CC(C(C)=NO1)=C1NS(C2=CC=CC3=C2C=CC=C3N(C)C)(=O)=O.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |