产品说明书

Buloxibutid

Print
Chemical Structure| 477775-14-7 同义名 : Compound 21;AT2 Agonist C21;M24;C21;AT2 receptor agonist C21
CAS号 : 477775-14-7
货号 : A775035
分子式 : C23H29N3O4S2
纯度 : 98%
分子量 : 475.624
MDL号 : MFCD26936332
存储条件:

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(220.76 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 AT2R Agonist C21 is an angiotensin II type 2 receptor agonist. Compound 21 (0.12 mg/kg/day for 4 weeks, p.o.) treatment improved fine motor skills after MCAO (middle cerebral artery occlusion) through modulation of the microglia/macrophage inflammatory properties. In addition, C21 increased M2 polarization and reduced the M1:M2 ratio in vitro. Thus, delayed administration of C21 downregulates post-stroke inflammation in female diabetic animals[3]. AT2R agonist C21 effectively prevents the development of PSCI in aged animals[4]. The administration of C21 (0.1-10 μM/15 min) increased the surface levels of TRKB (tropomyosin-related kinase B receptors) but was not sufficient to increase the levels of phosphorylated TRKB (pTRKB) in cultured cortical neurons from rat embryos. Consistent with increased TRKB surface expression, C21 (10 μM/15 min or 3 days) facilitated the effect of BDNF (0.1 ng/mL/15 min) on pTRKB in these cells[5]. In cultured human RPE cells, activation of AT2R with C21 significantly blocked Angiotensin II, LPS and hydrogen peroxide -induced NF-κB activation and inflammatory cytokine expression[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.10mL

0.42mL

0.21mL

10.51mL

2.10mL

1.05mL

21.03mL

4.21mL

2.10mL

参考文献

[1]Murugaiah AM, Wu X, et al. From the first selective non-peptide AT(2) receptor agonist to structurally related antagonists. J Med Chem. 2012 Mar 8;55(5):2265-78.

[2]Wan Y, Wallinder C, et al. Design, synthesis, and biological evaluation of the first selective nonpeptide AT2 receptor agonist. J Med Chem. 2004 Nov 18;47(24):5995-6008.

[3]Jackson-Cowan L, Eldahshan W, Dumanli S, Dong G, Jamil S, Abdul Y, Althomali W, Baban B, Fagan SC, Ergul A. Delayed Administration of Angiotensin Receptor (AT2R) Agonist C21 Improves Survival and Preserves Sensorimotor Outcomes in Female Diabetic Rats Post-Stroke through Modulation of Microglial Activation. Int J Mol Sci. 2021 Jan 29;22(3):1356

[4]Ahmed HA, Ishrat T, Pillai B, Bunting KM, Vazdarjanova A, Waller JL, Ergul A, Fagan SC. Angiotensin receptor (AT2R) agonist C21 prevents cognitive decline after permanent stroke in aged animals-A randomized double- blind pre-clinical study. Behav Brain Res. 2019 Feb 1;359:560-569

[5]Laukkanen L, Diniz CRAF, Foulquier S, Prickaerts J, Castrén E, Casarotto PC. Facilitation of TRKB Activation by the Angiotensin II Receptor Type-2 (AT2R) Agonist C21. Pharmaceuticals (Basel). 2021 Aug 6;14(8):773

[6]Verma A, Zhu P, de Kloet A, Krause E, Sumners C, Li Q. Angiotensin receptor expression revealed by reporter mice and beneficial effects of AT2R agonist in retinal cells. Exp Eye Res. 2019 Oct;187:107770