MMP13-IN-2|935759-55-0|-陌孚医药/Medlife

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MMP13-IN-2

目录号: PL07394 纯度: ≥99%

CAS No. :935759-55-0

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中文名称	MMP13-IN-2
英文名称	MMP13-IN-2
英文别名	MMP13-IN-2
Cas No.	935759-55-0
分子式	C₂₄H₁₉FN₆O₄S
分子量	506.51
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	MMP13-IN-2 是一种有效、选择性和口服活性的 MMP-13 抑制剂。MMP13-IN-2 对 MMP-13 具有优异的效价 (IC₅₀=0.036 nM)，对 MMP-1、3、7、8、9、14 和 TACE 的选择性(大于 1500 倍)。MMP13-IN-2 在体外具有阻止软骨释放胶原蛋白的能力。MMP13-IN-2 具有胶原酶相关疾病研究的潜力。
生物活性	MMP13-IN-2 is a potent, selective and orally active MMP-13 inhibitor. MMP13-IN-2 exhibits excellent potency for MMP-13 (IC 50 =0.036 nM) and selectivities (greater than 1,500-fold) over MMP-1, 3, 7, 8, 9, 14, and TACE. MMP13-IN-2 has the ability to block the release of collagen from cartilage in vitro. MMP13-IN-2 has the potential for collagenase related disease research.
性状	Solid
IC50 & Target[1][2]	MMP-13 0.036 nM (IC50) MMP-2 180 nM (IC
体外研究(In Vitro)	In a bovine nasal cartilage (BNC) assay, the chondrocyte-mediated degradation of cartilage was studied using bovine nasal cartilage slices cultured for up to 14 days. MMP13-IN-2 (0.01-1 μM) is effective at preventing the IL-1/OSM induced in vitro degradation of BNC (-17.6%, 48.4% and 70.8% inhibition of cartilage degradation, respectively).. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	MMP13-IN-2 (oral gavage; 1 mg/kg) shows the best combination of CYP3A4 inhibition risk and oral exposure at a dose of 1 mg/kg in rats and mice (F% = 33 and 38, respectively). has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Hiroshi Nara, et al. Discovery of Novel, Highly Potent, and Selective Matrix Metalloproteinase (MMP)-13 Inhibitors with a 1,2,4-Triazol-3-yl Moiety as a Zinc Binding Group Using a Structure-Based Design Approach. J Med Chem. 2017 Jan 26;60(2):608-626.

溶解度数据	In Vitro: DMSO : 100 mg/mL (197.43 mM; ultrasonic and warming and heat to 60°C)配制储备液

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