| INT-777TGR5 receptor agonist, potent and selective |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Cell experiment [1]: | |
Cell lines | RAW264.7 cells |
Preparation method | Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reaction Conditions | 37oC |
Applications | Combined LPS-INT-777 treatment significantly attenuates the transient increase in mRNA levels for Tnfa, monocyte chemoattractant protein 1 (Mcp-1), Il-6, and Il-1b. INT-777 also markedly diminishes p65 translocation via TGR5 activation; in contrast to the unchanged the phosphorylation of c-Jun. |
| Animal experiment [1]: | |
Animal models | TGR5 genetic models |
Dosage form | 30 mg/kg/day. |
Applications | INT-777 inhibits atherosclerosis through activation of TGR5 in leukocytes. In Ldlr-/- mice transplanted with bone marrow of Tgr5+/+ mice, INT-777 treatment causes less vascular lesion, indicating the solid inhibitory effect of INT-777 on development of atherosclerosis. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: 1. Pols TW, Nomura M, Harach T et al. TGR5 activation inhibits atherosclerosis by reducing macrophage inflammation and lipid loading. Cell Metab. 2011 Dec 7;14(6):747-57. | |
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| Cas No. | 1199796-29-6 | SDF | Download SDF |
| Formula | C27H46O5 | M.Wt | 450.65 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
INT-777 (S-EMCA) is a potent and selective agonist of TGR5 receptor with EC50 value of 0.82 μM [1].
TGR5 receptor is a G protein-coupled receptor and functions as a cell surface receptor for bile acids. TGR5 receptor plays an important role in the regulation of energy homeostasis by bile acids and suppression of macrophage functions [1].
INT-777 (S-EMCA) is a potent and selective TGR5 receptor agonist [1]. In macrophages, INT-777 inhibited proinflammatory cytokine production by TGR5-induced cAMP signaling and subsequent NF-kB inhibition [2]. In pancreatic β cell line MIN6, INT-777 selectively activated Gαs and increased intracellular cAMP and Ca2+. INT-777 also increased phosphoinositide (PI) hydrolysis and insulin release, which was dependent on Gs/cAMP/Ca2+ pathway [3]. In human podocytes with high glucose, INT-777 induced mitochondrial biogenesis, increased fatty acid β-oxidation and decreased oxidative stress [4].
In Ldlr- /- Tgr5+/+ mice, INT-777 activated TGR5 and attenuated atherosclerosis, which was associated with less plaque macrophage content and decreased intraplaque inflammation [2]. In diabetic db/db mice, INT-777 decreased mitochondrial H2O2 production and increased SOD2 activity, then reduced proteinuria, mesangial expansion, podocyte injury, fibrosis, and CD68 macrophage infiltration in the kidney [4].
References:[1]. Pellicciari R, Gioiello A, Macchiarulo A, et al. Discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity. J Med Chem, 2009, 52(24): 7958-7961.[2]. Pols TW, Nomura M, Harach T, et al. TGR5 activation inhibits atherosclerosis by reducing macrophage inflammation and lipid loading. Cell Metab, 2011, 14(6): 747-757. [3]. Kumar DP, Rajagopal S, Mahavadi S, et al. Activation of transmembrane bile acid receptor TGR5 stimulates insulin secretion in pancreatic β cells. Biochem Biophys Res Commun, 2012, 427(3): 600-605. [4]. Wang XX, Edelstein MH, Gafter U, et al. G Protein-Coupled Bile Acid Receptor TGR5 Activation Inhibits Kidney Disease in Obesity and Diabetes. J Am Soc Nephrol, 2015. pii: ASN.2014121271.
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上海好多的供应商的，具体还是看你选择了，其实试剂盒产品都差不多，什么远慕生物，古朵生物...好多的额
用双氧水去除过氧化物酶时，我是自己配的3%双氧水滴到片上而非将片浸入双氧水，这样可否？
用博士德的DAB染色，配制方法为：1mlH20中加入DAB、H2O2、TBS各一滴，我配制的时候发现将DAB加入H20时很容易沉淀，要震荡才能混匀，且将配好的DAB滴到玻片上时，DAB会结为很小块的微颗粒悬浮在液体中但并不染色，是否DAB有问题？
现在打算换中衫的试剂盒，代理商说中衫的试剂盒包括了二抗和DAB，想请教一下该试剂盒的具体内容有些什么？
万分感谢！
