A-317491 sodium salt hydrate
目录号 : GC35211
A P2X3 and P2X2/3 receptor antagonist
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
A-317491 is a non-nucleotide antagonist of the purinergic receptors P2X3 and P2X2/3 (Kis = 22-92 nM in a calcium influx assay) that is selective over other purinergic and neurotransmitter receptors, ion channels, and enzymes (IC50s = >10 ?M).1 It reduces thermal hyperalgesia induced by complete Freund’s adjuvant in rats (ED50 = 30 ?mol/kg, s.c.) and nociceptive responses to chemically-induced pain. Chronic administration of A-317491 (30 ?mol/kg, twice daily) reduces early, but not late, phase pain in a mouse model of bone cancer.2 A-317491 does not readily cross the blood-brain barrier and reduces pain responses when applied topically in a rat model of inflammatory pain, indicating that it acts primarily at peripheral purinergic receptors.3
1.Jarvis, M.F., Burgard, E.C., McGaraughty, S., et al.A-317491, a novel potent and selective non-nucleotide antagonist of P2X3 and P2X2/3 receptors, reduces chronic inflammatory and neuropathic pain in the ratProc. Natl. Acad. Sci. USA99(26)17179-17184(2002) 2.Hansen, R.R., Nasser, A., Falk, S., et al.Chronic administration of the selective P2X3, P2X2/3 receptor antagonist, A-317491, transiently attenuates cancer-induced bone pain in miceEur. J. Pharmacol.688(1-3)27-34(2012) 3.Wu, G., Whiteside, G.T., Lee, G., et al.A-317491, a selective P2X3/P2X2/3 receptor antagonist, reverses inflammatory mechanical hyperalgesia through action at peripheral receptors in ratsEur. J. Pharmacol.504(1-2)45-53(2004)
| Cas No. | SDF | ||
| Canonical SMILES | O=C(C1=CC(C(N(CC2=CC=CC(OC3=CC=CC=C3)=C2)[C@H]4CCCC5=C4C=CC=C5)=O)=C(C(O)=O)C=C1C(O)=O)O.[Na].O | ||
| 分子式 | C33H29NNaO9 | 分子量 | 606.57 |
| 溶解度 | Water: ≥ 100 mg/mL (164.86 mM); DMSO: ≥ 100 mg/mL (164.86 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 | 1.6486 mL | 8.2431 mL | 16.4861 mL |
| 5 mM | 0.3297 mL | 1.6486 mL | 3.2972 mL |
| 10 mM | 0.1649 mL | 0.8243 mL | 1.6486 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。