Orobol is one of the major soy isoflavones and has various pharmacological activities, including anti-skin-aging and anti-obesity effects. Orobol inhibits CK1ε, VEGFR2, MAP4K5, MNK1, MUSK, TOPK, and TNIK (IC50=1.24-4.45 μM). Orobol also inhibits PI3K isoforms (IC50=3.46-5.27 μM for PI3K α/β/γ/K/δ)[1][2].
体外研究 (In Vitro)
Orobol binds to CK1ε in an ATP-competitive manner and exerts anti-obesity effects by targeting casein kinase 1 epsilon[2]. Orobol (5-20 μM) effectively suppresses MDI (isobutylmethylxanthine, dexamethasone and insulin (MDI))-induced phosphorylation of 4E-BP1[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
Orobol attenuates high fat diet-induced weight gain and lipid accumulation without affecting food intake in C57BL/6J mice[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
HFD-induced obesity in C57BL/6J mice[2]
Dosage:
10 mg/kg
Administration:
Intragastrically; daily for 23 weeks
Result:
Significantly reduced body weight by 17.3% compared to the HFD group.
分子量
286.24
Formula
C15H10O6
CAS 号
480-23-9
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Kim MH, et al. Lipid Nanoparticles for Enhancing the Physicochemical Stability and Topical Skin Delivery of Orobol. Pharmaceutics. 2020;12(9):845. Published 2020 Sep 3.
AF12198 is a potent, selective and specific peptide antagonist for human type I interleukin-1 receptor (IL1-R1) (IC50=8 nM) but not the human type II receptor (IC50=6.7 µM) or the murine type I receptor (IC50>200 µM). AF12198 inhibits IL-1-induced IL-8 production (IC50=25 nM) and IL-1-induced intercellular adhesion molecule-1 (ICAM-1) expression (IC50=9 nM) in vitro. AF12198 has anti-inflammatory activities and blocks responses to IL-1 in vivo[1].
IC50 Target[1]
IL1R1
8 nM (IC50)
体外研究 (In Vitro)
AF12198 competes for binding of 125I-IL-1α with an IC50 of 8.0 nM, nearly equal to that of IL-1ra, IC50 of 4.0 nM for the type I receptor[1].AF12198 (0-5 ng; 8 hours) inhibits IL-6 induction with an IC50 of 15 μM whereas IL-1ra inhibits with an IC50 of 2 nM in heparinized human primate blood. Meanwhile, With blood from cynomolgus monkeys, the IC50 values are 17 μM for AF12198 and 30 nM for IL-1ra. Additionally, AF12198 or IL-1RA alone does not induce IL-6 in blood from either humans or cynomolgus monkeys[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
AF12198 (intravenous infusion; 16 mg/kg; 30 min before LPS intravenous injection) significantly attenuates the increase in lung MPO activity induced by LPS in acute lung inflammation and it reduces the lung microvascular leakage from rats inflamed with LPS at the 4 h (32.6%), 12 h (50.1%) and 24 h (65.3%) after LPS[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Male Wistar rats[2]
Dosage:
16 mg/kg
Administration:
Intravenous infusion; 30 min before LPS intravenous injection
Result:
Decreased pulmonary microvascular leakage in rats.
[1]. F Aimbire, et al. Low level laser therapy (LLLT) decreases pulmonary microvascular leakage, neutrophil influx and IL-1beta levels in airway and lung from rat subjected to LPS-induced inflammation. Inflammation
[2]. A L Akeson, et al.AF12198, a novel low molecular weight antagonist, selectively binds the human type I interleukin (IL)-1 receptor and blocks in vivo responses to IL-1. J Biol Chem. 1996 Nov 29;271(48):30517-23.
Dehydrobruceine A 是一个低活性的抗锥虫剂,对 Plasmodium falciparum 的 IC50 值为88.5 nM。
Dehydrobruceine A Chemical Structure
CAS No. : 73435-47-9
规格
是否有货
5 mg
询价
10 mg
询价
25 mg
询价
* Please select Quantity before adding items.
生物活性
Dehydrobruceine A is a low potent antitrypanosomal agent, with an IC50 of 88.5 nM for Plasmodium falciparum[1].
分子量
520.53
Formula
C26H32O11
CAS 号
73435-47-9
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Saw Bawm, et al. In vitro antitrypanosomal activities of quassinoid compounds from the fruits of a medicinal plant, Brucea javanica. Vet Parasitol. 2008 Dec 20;158(4):288-94.
8-Deoxygartanin, a prenylated xanthones from G. mangostana, is a selective inhibitor of butyrylcholinesterase (BChE)[1]. 8-Deoxygartanin exhibits antiplasmodial activity with an IC50 of 11.8 μM for the W2 strain of Plasmodium falciparum[2]. 8-Deoxygartanin inhibits NF-κB (p65) activation with an IC50 of 11.3 μM[3].
IC50 & Target
p65
11.3 μM (IC50)
分子量
380.43
Formula
C23H24O5
CAS 号
33390-41-9
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
参考文献
[1]. Khaw KY, et al. Prenylated xanthones from mangosteen as promising cholinesterase inhibitors and their molecular docking studies. Phytomedicine. 2014 Sep 25;21(11):1303-9.
[2]. Ngouamegne ET, et al. Endodesmiadiol, a friedelane triterpenoid, and other antiplasmodial compounds from Endodesmia calophylloides. Chem Pharm Bull (Tokyo). 2008 Mar;56(3):374-7.
[3]. Han AR, et al. Cytotoxic xanthone constituents of the stem bark of Garcinia mangostana (mangosteen). J Nat Prod. 2009 Nov;72(11):2028-31.
Rhodiosin, isolated from the root of Rhodiola crenulata, is a specific non-competitive cytochrome P450 2D6 inhibitor with an IC50 of 0.420 μM and a Ki of 0.535 μM[1]. Rhodiosin exhibits potent, dose-dependent inhibitory effects on acetylcholinesterase (AChE) with IC50 ranged from 57.50 to 2.43 μg/mL[2]. Rhodiosin exhibits potent DPPH free radical scavenging activities, with an IC50 of 27.77 μM[3].
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 MCE 网站选购。
参考文献
[1]. Xu W, et al. Two potent cytochrome P450 2D6 inhibitors found in Rhodiola rosea. Pharmazie. 2013 Dec;68(12):974-6.
[2]. Li FJ, et al. Molecular interaction studies of acetylcholinesterase with potential acetylcholinesterase inhibitors from the root of Rhodiola crenulata using molecular docking and isothermal titration calorimetry methods. Int J Biol Macromol. 2017 Nov;104(Pt A):527-532.
[3]. Choe KI, et al. The antioxidant and anti-inflammatory effects of phenolic compounds isolated from the root of Rhodiola sachalinensis A. BOR. Molecules. 2012 Sep 27;17(10):11484-94.