1. Metabolic Enzyme/Protease
  2. MMP
  3. MMP13-IN-2

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。

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MMP13-IN-2 Chemical Structure

MMP13-IN-2 Chemical Structure

CAS No. : 935759-55-0

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Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ¥4400
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1 mg ¥1818
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5 mg ¥4000
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10 mg ¥6800
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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 (IC50=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[1].

IC50 & Target[1]

MMP-13

0.036 nM (IC50)

MMP-2

180 nM (IC50)

MMP-3

1100 nM (IC50)

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).[1].

MCE 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)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

506.51

Formula

C24H19FN6O4S

CAS 号
非同位 CAS

性状

固体

颜色

White to off-white

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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (197.43 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9743 mL 9.8715 mL 19.7429 mL
5 mM 0.3949 mL 1.9743 mL 3.9486 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

MMP13-IN-2 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9743 mL 9.8715 mL 19.7429 mL 49.3574 mL
5 mM 0.3949 mL 1.9743 mL 3.9486 mL 9.8715 mL
10 mM 0.1974 mL 0.9871 mL 1.9743 mL 4.9357 mL
15 mM 0.1316 mL 0.6581 mL 1.3162 mL 3.2905 mL
20 mM 0.0987 mL 0.4936 mL 0.9871 mL 2.4679 mL
25 mM 0.0790 mL 0.3949 mL 0.7897 mL 1.9743 mL
30 mM 0.0658 mL 0.3290 mL 0.6581 mL 1.6452 mL
40 mM 0.0494 mL 0.2468 mL 0.4936 mL 1.2339 mL
50 mM 0.0395 mL 0.1974 mL 0.3949 mL 0.9871 mL
60 mM 0.0329 mL 0.1645 mL 0.3290 mL 0.8226 mL
80 mM 0.0247 mL 0.1234 mL 0.2468 mL 0.6170 mL
100 mM 0.0197 mL 0.0987 mL 0.1974 mL 0.4936 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
MMP13-IN-2
目录号:
HY-122624
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