BU 239 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.
靶点:I1咪唑啉受体,I2咪唑啉受体
IC50:35 nM,47 nM
BU 239 hydrochloride是咪唑啉受体的选择性拮抗剂。在竞争结合实验中,BU239对I1咪唑啉和I2咪唑啉受体具有高亲和力,IC50值分别为35 nM和47 nM[1]。咪唑啉受体参与循环系统,被分为两类:I1型和I2型。I1型对idazoxan和clonidine敏感,clonidine是具有咪唑啉结构的拮抗剂。I2型对idazoxan、cirazoline、guanabenz具有高亲和力,对clonidine具有中等程度的亲和力。咪唑啉I1受体在血压的中枢调节中起关键作用[2]。
体外实验:在大鼠内髓集合管(IMCD)中,1 μM的BU239逆转α2激动剂介导的对精氨酸加压素(AVP)刺激的水通透性的抑制[3]。此外,BU239显著逆转IMCD中胍丁胺诱导的对AVP刺激的尿素通透性(Pu)的抑制[4]。BU239产生正性肌力活性,观察到的最大效果为117.4%[2]。
体内:N/A
参考文献:
1. Flamez A, De Backer JP, Czerwiec E, Ladure P, Vauquelin G. Pharmacological characterization of I1 and I2 imidazoline receptors in human striatum. Neurochem Int. 1997;30(1):25-9.
2. Radwanska A, Dlugokecka J, Wasilewski R, Kaliszan R. Testing conception of engagement of imidazoline receptors in imidazoline drugs effects on isolated rat heart atria. J Physiol Pharmacol. 2009;60(1):131-42.
3. Kudo LH, Hebert CA, Rouch AJ. Inhibition of water permeability in the rat collecting duct: effect of imidazoline and alpha-2 compounds. Proc Soc Exp Biol Med. 1999;221(2):136-46.
4. Rouch AJ, Kudo LH. Agmatine inhibits arginine vasopressin-stimulated urea transport in the rat inner medullary collecting duct. Kidney Int. 2002;62(6):2101-8.
Storage | Desiccate at RT |
M.Wt | 234.69 |
Cas No. | 1217041-98-9 |
Formula | C11H10N4·HCl |
Solubility | <11.73mg/ml in DMSO |
Chemical Name | 2-(4,5-dihydro-1H-imidazol-2-yl)quinoxaline hydrochloride |
SDF | Download SDF |
Canonical SMILES | C12=CC=CC=C1N=C(C3=NCCN3)C=N2.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。 |