GDC-0310
目录号 : GC64206
GDC-0310是选择性酰基磺酰胺电压门控型钠离子通道1.7（NaV1.7）抑制剂，IC50值为0.6nM。
Cas No.:1788063-52-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
GDC-0310 is a selective acylsulfonamide voltage-gated sodium channel 1.7 (NaV1.7) inhibitor with an IC50 value of 0.6nM[1]. NaV1.7 is a complex protein with multiple druggable sites that plays a vital role in the transmission of pain signals[2]. GDC-0310 is an orally available small molecule NaV1.7 inhibitor that can be used to treat pain[3, 4]. Compared with GDC-0276 (Catalog No.: GC39559), GDC-0310 exhibits better metabolic stability, NaV selectivity and pharmacokinetic characteristics[5].
References:
[1] Safina B S, McKerrall S J, Sun S, et al. Discovery of acyl-sulfonamide NaV1. 7 inhibitors GDC-0276 and GDC-0310[J]. Journal of medicinal chemistry, 2021, 64(6): 2953-2966.
[2] McKerrall S J, Sutherlin D P. Nav1. 7 inhibitors for the treatment of chronic pain[J]. Bioorganic & medicinal chemistry letters, 2018, 28(19): 3141-3149.
[3] Stevens E B, Stephens G J. Recent advances in targeting ion channels to treat chronic pain[J]. British journal of pharmacology, 2018, 175(12): 2133.
[4] Stumpf A, Cheng Z K, Beaudry D, et al. Improved synthesis of the Nav1. 7 inhibitor GDC-0276 via a highly regioselective SNAr reaction[J]. Organic Process Research & Development, 2019, 23(9): 1829-1840.
[5] Asiri Y I, Hassan M Z. An Overview of Ion Channels Therapeutics in the Treatment of Pain[J]. Arabian Journal of Chemistry, 2023: 105180.
GDC-0310是选择性酰基磺酰胺电压门控型钠离子通道1.7（NaV1.7）抑制剂，IC50值为0.6nM[1]。NaV1.7是一种具有多个成药位点的复杂蛋白质，在疼痛信号的传递中起着至关重要的作用[2]。GDC-0310是一种口服小分子NaV1.7抑制剂，能够用于治疗疼痛[3, 4]。与GDC-0276（目录号：GC39559）相比，GDC-0310表现出更好的代谢稳定性、NaV选择性和药代动力学特征[5]。
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.84 mL | 9.2 mL | 18.3999 mL |
| 5 mM | 0.368 mL | 1.84 mL | 3.68 mL |
| 10 mM | 0.184 mL | 0.92 mL | 1.84 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。