Tanaproget
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.
Tanaproget(NSP989)是一种新型的非甾体类孕酮受体激动剂,其IC50值为1.7 nM[1]。
孕酮受体(PR)是核受体超家族的成员,通过与孕酮结合引起PR构象变化,进而改变基因表达。孕酮在女性生殖中扮演重要作用[1]。
在T47D细胞中,tanaproget可引发碱性磷酸酶活性,其EC50值为0.1 nM。在哺乳动物双杂交试验中,tanaproget展现的效果为孕酮的50倍。在子宫内膜分离的基质细胞中,tanaproget(1 nM)显著地抑制了pro-MMP-3的分泌。此外,tanaproget显著地阻碍了IL-1α刺激的pro-MMP-3分泌[2]。
在腹壁膜层有人类病变的子宫内膜异位症小鼠模型中,58%的小鼠经tanaproget治疗后完全恢复。另外在治疗结束后,相比安慰剂处理的小鼠,病变也变得更小且更少[2]。在健康女性当中,估计tanaproget半衰期(t(1/2))为12至30 h。Tanaproget可降低宫颈黏液评分,这表示宫颈黏液的量和质均有下降[3]。
参考文献:
[1]. Zhang Z, Olland AM, Zhu Y, et al. Molecular and pharmacological properties of a potent and selective novel nonsteroidal progesterone receptor agonist tanaproget. J Biol Chem, 2005, 280(31): 28468-28475.
[2]. Bruner-Tran KL, Zhang Z, Eisenberg E, et al. Down-regulation of endometrial matrix metalloproteinase-3 and -7 expression in vitro and therapeutic regression of experimental endometriosis in vivo by a novel nonsteroidal progesterone receptor agonist, tanaproget. J Clin Endocrinol Metab, 2006, 91(4): 1554-1560.
[3]. Bapst JL, Ermer JC, Ferron GM, et al. Pharmacokinetics and safety of tanaproget, a nonsteroidal progesterone receptor agonist, in healthy women. Contraception, 2006, 74(5): 414-418.
Storage | Store at -20°C |
M.Wt | 297.37 |
Cas No. | 304853-42-7 |
Formula | C16H15N3OS |
Synonyms | NSP-989;NSP 989;NSP989 |
Solubility | Soluble in DMSO |
Chemical Name | 5-(4,4-dimethyl-2-sulfanylidene-1H-3,1-benzoxazin-6-yl)-1-methylpyrrole-2-carbonitrile |
SDF | Download SDF |
Canonical SMILES | CC1(C2=C(C=CC(=C2)C3=CC=C(N3C)C#N)NC(=S)O1)C |
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。 |
描述 | Tanaproget(NSP989)是一种新型的非甾体类孕酮受体激动剂。 | |||||
靶点 | progesterone receptor | |||||
IC50 | 0.1 nM (EC50, induce alkaline phosphatase activity) |