BQR-695 (NVP-BQR695)
(Synonyms: NVP-BQR695) 目录号 : GC32163
An antimalarial compound
Cas No.:1513879-21-4
Sample solution is provided at 25 µL, 10mM.
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BQR-695 is an antimalarial compound.1 It inhibits recombinant P. vivax and human phosphatidylinositol 4-kinase (PI4K; IC50s = 3.5 and 90 nM, respectively). BQR-695 induces schizont-stage arrest and death of P. falciparum (IC50 = ~70 nM) without inducing cytotoxicity in mature red blood cells (RBCs).
1.McNamara, C.W., Lee, M.C., Lim, C.S., et al.Targeting Plasmodium phosphatidylinositol 4-kinase to eliminate malariaNature504(7479)248-253(2013)
Cell experiment: | A clonal population of P. falciparum Dd2 parasites is used to initiate two or three independent parasite cultures under the initial selection pressure of 12 nM KAI407, 1 nM KAI715 or 40 nM BQR695. Stepwise drug evolution continues until the final concentration is at least 3-fold higher than the initial concentration (typically 80 to 120 days). For each of the ten resistant strains, copy number variations (CNVs) and single nucleotide variations (SNVs) are detected using a whole-genome tiling array and analyzed with PfGenominator. The susceptibility of each resistant strain to KAI407, KAI715, KDU691 and BQR695 is determined by the 72-hr SYBR Green cell proliferation assay with four independent experiments assayed in duplicate[2]. |
References: [1]. Fowler ML, et al. Using hydrogen deuterium exchange mass spectrometry to engineer optimized constructs for crystallization of protein complexes: Case study of PI4KIIIβ with Rab11. Protein Sci. 2016 Apr;25(4):826-39. | |
| Cas No. | 1513879-21-4 | SDF | |
| 别名 | NVP-BQR695 | ||
| Canonical SMILES | COC(C(OC)=C1)=CC=C1C2=CC3=NC(NCC(NC)=O)=CN=C3C=C2 | ||
| 分子式 | C19H20N4O3 | 分子量 | 352.39 |
| 溶解度 | DMSO : 100 mg/mL (283.78 mM) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.8378 mL | 14.1888 mL | 28.3776 mL |
| 5 mM | 567.6 μL | 2.8378 mL | 5.6755 mL |
| 10 mM | 283.8 μL | 1.4189 mL | 2.8378 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet