(R)-SLV 319
目录号 : GC10028
The inactive enantiomer of SLV 319
Cas No.:656827-86-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Ki: 7.8 and 7943 nM for CB1 and CB2 receptors, respectively by SLV 319
(R)-SLV 319 is a CB1 receptor antagonist.
Central cannabinoid (CB1) receptor antagonists can be used in the treatment of various diseases including cognitive disorders, neuroinflammatory disorders, obesity, septic shock, psychosis, addiction, as well as gastrointestinal disorders.
In vitro: (R)-SLV 319 is the inactive enantiomer of SLV 319 with 100-fold less affinity for the CB1 receptor. SLV 319 was identified as a potent and selective CB1 receptor antagonist with Ki values of 7.8 and 7,943 nM for CB1 and peripheral cannabinoid (CB2) receptors, respectively. SLV 319 was found to be less lipophilic and thus more water soluble than other known CB1 receptor ligands [1,2].
In vivo: A previous animal study examined the chronic effects of SLV 319 in hyperinsulinemic Zucker rats to determine their chronic effects on insulinemia. Results showed that R SLV 319 at 10 mg·kg-1·day-1 elicited body weight-independent improvements in insulinemia and glycemia during 10 wk of chronic treatment. Moreover, SLV 319 treatment caused glucose intolerance in CB1 but not SUR1-KO mice [3].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Lange, J. H.M.,Coolen, H.K.A.C.,van Stuivenberg, H.H., et al. Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB1 cannabinoid receptor antagonists. Journal of Medicinal Chemistry 47(3), 627-643 (2004).
[2] Lange, J. H.M.,van Stuivenberg, H.H.,Veerman, W., et al. Novel 3,4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity. Bioorganic & Medicinal Chemistry Letters 15, 4794-4798 (2005).
[3] Lynch CJ, Zhou Q, Shyng SL, Heal DJ, Cheetham SC, Dickinson K, Gregory P, Firnges M, Nordheim U, Goshorn S, Reiche D, Turski L, Antel J. Some cannabinoid receptor ligands and their distomers are direct-acting openers of SUR1 K(ATP) channels. Am J Physiol Endocrinol Metab. 2012 Mar 1;302(5):E540-51.
| Cas No. | 656827-86-0 | SDF | |
| 化学名 | 3-(4-chlorophenyl)-N-[(4-chlorophenyl)sulfonyl]-4,5-dihydro-N'-methyl-4R-phenyl-1H-pyrazole-1-carboximidamide | ||
| Canonical SMILES | C/N=C(\NS(=O)(=O)c1ccc(Cl)cc1)/N1N=C(c2ccc(Cl)cc2)[C@@H](C1)c1ccccc1 | ||
| 分子式 | C23H20Cl2N4O2S | 分子量 | 487.4 |
| 溶解度 | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | 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 | 2.0517 mL | 10.2585 mL | 20.517 mL |
| 5 mM | 0.4103 mL | 2.0517 mL | 4.1034 mL |
| 10 mM | 0.2052 mL | 1.0259 mL | 2.0517 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。