生物活性
TP-472N is a negative control probe for TP-472 (catalog no. SML1862). TP-472 is a selective probe for bromodomain-containing proteins BRD9 and BRD7. The BRD9/7 probe was developed out of a collaborative effort by Takeda and the SGC, and is of a different chemotype from BRD9/7 probes previously available. TP-472 has a KD value of 33nM for BRD9 and 340nM for BRD7 by ITC, is >30 fold selective for BRD9 over all other bromodomain family members except BRD7, and is suitable for in vivo applications. The negative control TP-472N is inactive against other bromodomains (>20μM against BRD9). For full characterization details of TP-472 and TP-472N, please visit theTP-472 probe summaryon the Structural Genomics Consortium (SGC) website.
化学数据
分子量 | 306.36 |
分子式 | C19H18N2O2 |
CAS号 | 2080306-24-5 |
纯度 | >98% |
溶解性(25°C) | DMSO: 15 mg/mL clear |
储存和运输条件 | 固体粉末: -20°C 冷藏长期储存 常温运输及临时存放 |
不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
动物 A的Km系数 |
例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 3.2641 mL | 16.3207 mL | 32.6413 mL |
5 mM | 0.6528 mL | 3.2641 mL | 6.5283 mL |
10 mM | 0.3264 mL | 1.6321 mL | 3.2641 mL |