ELN441958
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.
ELN441958是一种新型的\有效的以及选择性的缓激肽B1受体拮抗剂,其Ki值为0.26 nM[1].
缓激肽B1受体属于G蛋白偶联受体,其主要配体为缓激肽.缓激肽B1受体在慢性疼痛与炎症中起着重要作用[1].
ELN441958是一种新型的\有效的以及选择性的缓激肽B1受体拮抗剂.在IMR-90肺成纤维细胞的细胞膜上,ELN441958竞争性地抑制激动剂[3H]DAKD结合人B1受体,其Ki值为0.26 nM.在表达天然人B1受体的IMR-90细胞中,ELN441958呈浓度依赖性地拮抗DAKD引起的钙动员,其KB值为0.12 nM.相对于B2受体,ELN441958对B1受体具有高选择性.ELN441958不能抑制B2受体激动剂BK引起的钙动员.此外,ELN441958也抑制人μ\δ和κ阿片受体以及毒蕈碱受体M1,其Ki值分别为0.13\0.69\1.5和0.37 μM.ELN441958也是δ阿片受体(EC50 = 0.76 μM)与μ阿片受体的激动剂.在体外,ELN441958具有良好的渗透性以及代谢稳定性[1].
在大鼠和恒河猴中,ELN441958具有较高的口服生物利用度以及适中的血浆半衰期.在恒河猴中,ELN441958呈剂量依赖性地减少角叉菜胶引起的热痛觉过敏,其ED50值约为3 mg/kg(皮下注射)[1].
参考文献:
[1]. Hawkinson JE, Szoke BG, Garofalo AW, et al. Pharmacological, pharmacokinetic, and primate analgesic efficacy profile of the novel bradykinin B1 Receptor antagonist ELN441958, J Pharmacol Exp Ther, 2007, 322(2): 619-630.
Storage | Store at -20°C |
M.Wt | 501.02 |
Cas No. | 913064-47-8 |
Formula | C29H29ClN4O2 |
Solubility | Soluble in DMSO |
Chemical Name | 7-chloro-2-(3-(9-(pyridin-4-yl)-3,9-diazaspiro[5.5]undecane-3-carbonyl)phenyl)isoindolin-1-one |
SDF | Download SDF |
Canonical SMILES | ClC1=CC=CC(CN2C3=CC=CC(C(N4CCC5(CC4)CCN(C6=CC=NC=C6)CC5)=O)=C3)=C1C2=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
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