{{cart_num}}
My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Metabolic Enzyme & Protease > OdanacatibCAS：603139-19-1
Molecular Formula：C25H27F4N3O3S
Molecular Weight：525.56
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to brown Solid
Qty：
Size：
| CAS | 603139-19-1 |
| Name | Odanacatib |
| Molecular Formula | C25H27F4N3O3S |
| Molecular Weight | 525.56 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to brown Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 682-460-8 |
| MDL | MFCD11042419 |
| SMILES | N#CC1(NC([C@@H](N[C@H](C(F)(F)F)C2=CC=C(C3=CC=C(S(=O)(C)=O)C=C3)C=C2)CC(C)(F)C)=O)CC1 |
| Target Point | Cathepsin |
| Passage | Metabolic Enzyme&Protease |
| Background | Odanacatib/MK-0822 is a potent and selective cathepsin K inhibitor. |
| Biological Activity | Odanacatib 是有效, 选择性的组织蛋白酶K抑制剂, IC50 分别为0.2 nM 和 1 nM[1-4]。 |
| IC50 | IC50: 0.2nM (Human Cathepsin K) ， 1nM (Rabbit Cathepsin K) [1-4] |
| In Vitro | 与同一试验中的Cat S抑制剂LHVS(IC50 =0.001μM)相比，Odanacatib是抗原呈递的弱抑制剂，在小鼠B细胞系中测量(IC50 = 1.5±0.4μM)。与LHVS相比，Odanacatib还显示对小鼠脾细胞中MHC II恒定链蛋白Iip10的加工的抑制作用较弱(最小抑制浓度分别为1-10μM和0.01μM)[1]。通过CTx释放(IC50 = 9.4nM)或再吸收面积(IC50 = 6.5nM)测量，Odanacatib降低了再吸收活性，但对OC活化没有影响。 Odanacatib剂量依赖性地降低CTx释放，IC50 = 9.4±1.0nM。 Odanacatib处理的OC在含CatK的囊泡中积累标记的降解骨基质蛋白[2]。 |
| In Vivo | Odanacatib(30mg / kg，口服，每日一次)持续抑制骨吸收标志物和血清骨形成标志物与载体处理的OVX猴。 Odanacatib显示对小梁与皮质骨形成的隔室特异性作用，治疗导致卵巢切除猴骨膜骨形成和皮质厚度显着增加，而骨小梁形成减少[3]。 OVX + ODN-h组的骨体积/总体积(BV / TV)和骨矿物质密度(BMD)显着高于OVX + Veh组(p <0.05)。 OVX + ODN-h组中Runx2，Collagen-1，BSP，Osterix，OPN和SPP1的表达显着低于OVX + Veh组(p <0.01)。与OVX + Veh组相比，OVX + ODN-1组中Collagen-I，BSP，Osterix，OPN和ALP的表达降低，但在OVX + ODN-h组中上调[4]。 |
| Cell Experiment | 为了评估细胞存活，将大约7×10 4个细胞/ cm 2的分化的破骨细胞(OC)重新接种在具有或不具有100nM Odanacatib(ODN)的牛骨切片上。骨片在第2，4，6和12天固定，没有媒体变化。对样品进行TRAP活性和OC编号的染色。 |
| Animal Experiment | 将16只8个月大的雌性Sprague-Dawley(SD)大鼠(体重，385±55g)在温度受控的环境中随意给予水和软饮食，定期12小时光照和黑暗循环。将大鼠随机分成4组，每组4只：假手术组，OVX + Veh组，OVX + ODN-1组和OVX + ODN-h组。植入插入后，Odanacatib(ODN，5 mg / mL)分别以1 mL / kg和6 mL / kg的浓度给予OVX + ODN-1和OVX + ODN-h组，每天一次灌胃8周。 OVX + Veh组在相同的持续时间内用浓度为6mL / kg的0.5％羧甲基纤维素钠强饲。灌胃给药后，静脉注射戊巴比妥钠处死各组大鼠。收获植入物并将其与周围的骨一起固定在10％缓冲的福尔马林中。 |
| Data Literature Source | [1]. Jacques Yves Gauthier， et al. The discovery of odanacatib (MK-0822) ， a selective inhibitor of cathepsin K. Bioorg Med Chem Lett. 2008 Feb 1; 18 (3) :923-8. [2]. Leung P， et al. The effects of the cathepsin K inhibitor odanacatib on osteoclastic bone resorption and vesicular trafficking. Bone. 2011 Oct; 49 (4) :623-635. [3]. Ng KW. Potential role of odanacatib in the treatment of osteoporosis. Clin Interv Aging. 2012; 7:235-47. [4]. Yi C， et al. Inhibition of cathepsin K promotes osseointegration of titanium implants in ovariectomised rats. Sci Rep. 2017 Mar 17; 7:44682 |
| Unit | Bottle |
| Specification | 10mg 50mg 100mg |
是有效，选择性的组织蛋白酶K抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
Note：
1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
Sorry, there is no more information.
Sorry, there is no more information.
Sorry, there is no more information.
Manual Download
