Sarpogrelate-d3 (hydrochloride)
(Synonyms: MCI-9042-d3) 目录号 : GC48498
An internal standard for the quantification of sarpogrelate
Cas No.:2934185-00-7
Sample solution is provided at 25 µL, 10mM.
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Sarpogrelate-d3 is intended for use as an internal standard for the quantification of sarpogrelate (hydrochloride) by GC- or LC-MS. Sarpogrelate is a selective antagonist of the serotonin (5-HT) receptor subtypes 5-HT2A, 5-HT2B, and 5-HT2C (Kis = 3.02, 269, and 37.2 nM, respectively, for human recombinant receptors expressed in CHO-K1 cells).1 It is selective for 5-HT2 (Ki = 70.8 nM) over 5-HT1 (Ki = >26,000 nM), α1-, α2-, and β-adrenergic (Kis = 640-123,800 nM), and muscarinic receptors (Ki = >40,000 nM).2 In vitro, it inhibits aggregation of rat whole blood induced by collagen, 5-HT with collagen, and 5-HT with ADP .3 In vivo, it inhibits leukocyte-endothelial interactions in the femoral artery induced by a high-fat high-fructose diet (HFFD) in mice when administered at a dose of 5 mg/kg per day.4 Sarpogrelate (5 mg/kg per day) decreases ventricular hypertrophy and infarct size in a rat model of myocardial infarction.5
1.Rashid, M., Manivet, P., Nishio, H., et al.Identification of the binding sites and selectivity of sarpogrelate, a novel 5-HT2 antagonist, to human 5-HT2A, 5-HT2B and 5-HT2C receptor subtypes by molecular modelingLife Sci.73(2)193-207(2003) 2.Maruyama, K., Kinami, J., Sugita, Y., et al.MCI-9042: High affinity for serotonergic receptors as assessed by radioligand binding assayJ. Pharmacobiodyn.14(4)177-181(1991) 3.Kubacka, M., Kazek, G., Kotańska, M., et al.Anti-aggregation effect of aroxyalkyl derivatives of 2-methoxyphenylpiperazine is due to their 5-HT2A and α2-adrenoceptor antagonistic properties. A comparison with ketanserin, sarpogrelate, prazosin, yohimbine and ARC239Eur. J. Pharmacol.818263-270(2018) 4.Kataoka, H., Ariyama, Y., Deushi, M., et al.Inhibitory effect of serotonin antagonist on leukocyte-endothelial interactions in vivo and in vitroPLoS One11(1)e0147929(2016) 5.Brasil, D., Temsah, R.M., Kumar, K., et al.Blockade of 5-HT2A receptors by sarpogrelate protects the heart against myocardial infarction in ratsJ. Cardiovasc. Pharmacol. Ther.7(1)53-59(2002)
| Cas No. | 2934185-00-7 | SDF | |
| 别名 | MCI-9042-d3 | ||
| Canonical SMILES | CN(C)CC(OC(CCC(O)=O)=O)COC1=CC=CC=C1CCC2=CC(OC([2H])([2H])[2H])=CC=C2.Cl | ||
| 分子式 | C24H28D3NO6•HCl | 分子量 | 469 |
| 溶解度 | DMSO: soluble,Methanol: soluble,Water: soluble | 储存条件 | -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 | 2.1322 mL | 10.661 mL | 21.322 mL |
| 5 mM | 0.4264 mL | 2.1322 mL | 4.2644 mL |
| 10 mM | 0.2132 mL | 1.0661 mL | 2.1322 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: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet