Carboxyamidotriazole Orotate
(Synonyms: L-651582 Orotate; CAI Orotate) 目录号 : GC39646
A non-selective calcium channel blocker
Cas No.:187739-60-2
Sample solution is provided at 25 µL, 10mM.
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Carboxyamidotriazole is an orally bioavailable, non-selective calcium channel blocker.1 It blocks L- and T-type calcium channels in GH3 rat pituitary cancer cells (IC50s = 0.5 and 1.5 μg/ml, respectively). It also inhibits calcium influx stimulated by the acetylcholine receptor agonist carbachol and the calcium ionophore A23187 in CHO cells expressing human recombinant muscarinic M5 receptors (IC50s = 935 and 359 nM, respectively).2 Carboxyamidotriazole inhibits the growth of T. gondii in non-cancerous human fibroblasts and HeLa human cervical cancer cells (IC50 = 0.06 μg/ml for both).3 It inhibits the growth of FaDu and EVSCC17M human squamous cell carcinoma cells (IC50s = 13 and 15 μM, respectively) and of human umbilical vein endothelial cells (HUVECs; IC50 = 1 μM) in vitro.4,5 Carboxyamidotriazole (20 μM) also inhibits angiogenesis in a chicken chorioallantoic membrane assay in vivo.5
1.Hupe, D.J., Boltz, R., Cohen, C.J., et al.The inhibition of receptor-mediated and voltage-dependent calcium entry by the antiproliferative L-651,582J. Biol. Chem.266(16)10136-10142(1991) 2.Felder, C.C., Ma, A.L., Liotta, L.A., et al.The antiproliferative and antimetastatic compound L651582 inhibits muscarinic acetylcholine receptor-stimulated calcium influx and arachidonic acid releaseJ. Pharmacol. Exp. Ther.257(3)967-971(1991) 3.Hupe, D.J., Pfefferkorn, E.R., Behrens, N.D., et al.L-651,582 inhibition of intracellular parasitic protozoal growth correlates with host-cell directed effectsJ. Pharmacol. Exp. Ther.256(2)462-467(1991) 4.Wu, Y., Palad, A.J., Wasilenko, W.J., et al.Inhibition of head and neck squamous cell carcinoma growth and invasion by the calcium influx inhibitor carboxyamido-triazoleClin. Cancer Res.3(11)1915-1921(1997) 5.Kohn, E.C., Alessandro, R., Spoonster, J., et al.Angiogenesis: Role of calcium-mediated signal transductionProc. Natl. Acad. Sci. USA92(5)1307-1311(1995)
| Cas No. | 187739-60-2 | SDF | |
| 别名 | L-651582 Orotate; CAI Orotate | ||
| Canonical SMILES | O=C(C(NC1=O)=CC(N1)=O)O.O=C(C2=C(N)N(CC3=CC(Cl)=C(C(C4=CC=C(Cl)C=C4)=O)C(Cl)=C3)N=N2)N | ||
| 分子式 | C22H16Cl3N7O6 | 分子量 | 580.76 |
| 溶解度 | DMSO: 5 mg/mL (8.61 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7219 mL | 8.6094 mL | 17.2188 mL |
| 5 mM | 0.3444 mL | 1.7219 mL | 3.4438 mL |
| 10 mM | 0.1722 mL | 0.8609 mL | 1.7219 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