| CAS NO: | 656222-54-7 |
iKIX1 is an antifungal agent that can re-sensitize drug-resistant Candida glabrata to azole antifungals. C. glabrata fungal infections that are resistant to azoles are an increasing problem. Drug-resistant C. glabrata most commonly contain point mutations in Pdr1 that render it active. iKIX1 acts by inhibiting the protein–protein interaction between the fungal transcription factor Pdr1 and the KIX domain of the MED15 subunit of the co-activator Mediator, thus inhibiting Pdr1-dependent gene activation of key regulators of the multidrug resistance pathway. iKIX1 reduced efflux pump gene expression and restored azole-sensitivity to PDR1 gain-of-function mutant Candida glabrata strains in plate assays. In mouse assays, combination treatment with iKIX1 and fluconazole showed significant reduction of fungal burden in mice injected with two different azole-resistant C. glabrata strains.
| 分子量 | 303.17 |
| 分子式 | C10H8Cl2N4OS |
| CAS号 | 656222-54-7 |
| 纯度 | >98% |
| 溶解性（25°C） | DMSO: 25 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 |
| 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。
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 | 3.2985 mL | 16.4924 mL | 32.9848 mL |
| 5 mM | 0.6597 mL | 3.2985 mL | 6.597 mL |
| 10 mM | 0.3298 mL | 1.6492 mL | 3.2985 mL |
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