HC 067047
目录号 : GC12260
A selective TRPV4 antagonist
Cas No.:883031-03-6
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
HC-067047 is a potent and selective TRPV4 antagonist and reversibly inhibits currents through the human, rat, and mouse TRPV4 orthologs with IC50 values of 48 nM, 133 nM, and 17 nM, respectively[1].
HC-067047 (1 µM; 24 hours; HEI-OC1 cells) treatment significantly decreases mRNA expression in high glucose cultured HEI-OC1 cells[2].HC-067047 (1 µM; 24 hours; HEI-OC1 cells) treatment significantly decreases the expression of TRPV4 protein[2].HC-067047 (1 µM; 48 hours; HEI-OC1 cells) treatment inhibits cell proliferation[2].HC-067047 (1 µM; 48 hours; HEI-OC1 cells) treatment promotes cell apoptosis[2].
HC-067047 (0-50 mg/kg; intraperitoneal injection; for 30 minutes; cyclophosphamide-treated WT and Trpv4−/− mice, and naive WT mice) treatment increases functional bladder capacity and reduces micturition frequency in WT mice with cystitis. HC-067047 do not affect bladder function in Trpv4−/− mice[1].
References:
[1]. Everaerts W et al. Inhibition of the cation channel TRPV4 improves bladder function in mice and rats with cyclophosphamide-induced cystitis.Proc Natl Acad Sci U S A. 2010 Nov 2;107(44):19084-9.
[2]. Xing Y, et al. Decreased Expression of TRPV4 Channels in HEI-OC1 Cells Induced by High Glucose Is Associated with Hearing Impairment. Yonsei Med J. 2018 Nov;59(9):1131-1137.
| Cas No. | 883031-03-6 | SDF | |
| 化学名 | 2-methyl-1-(3-morpholinopropyl)-5-phenyl-N-(3-(trifluoromethyl)phenyl)-1H-pyrrole-3-carboxamide | ||
| Canonical SMILES | FC(F)(C1=CC(NC(C2=C(C)N(C(C3=CC=CC=C3)=C2)CCCN4CCOCC4)=O)=CC=C1)F | ||
| 分子式 | C26H28F3N3O2 | 分子量 | 471.51 |
| 溶解度 | ≥ 47.2mg/mL in DMSO | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1208 mL | 10.6042 mL | 21.2085 mL |
| 5 mM | 0.4242 mL | 2.1208 mL | 4.2417 mL |
| 10 mM | 0.2121 mL | 1.0604 mL | 2.1208 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。