BX 513 hydrochloride
目录号 : GC13299
Selective CCR1 antagonist
Cas No.:1216540-18-9
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
Ligands for the CCR1 receptor (MIP-1α and RANTES) have been implicated in plenty of chronic inflammatory diseases, most notably multiple sclerosis and rheumatoid arthritis. BX 513 is a novel non-peptide CCR1 receptor antagonists.
In vitro: BX 513 has been shown to have at least 200-fold selectivity for CCR1 inhibition over other human 7-TM receptors, including other chemokine receptors. In addition, data obtained from in-vitro functional assays demonstrated the functional antagonism of BX 513 and structurally related analogues against the CCR1 receptor in a dose-dependent manner [1]. BX 513 also showed concentration-dependent inhibition of MIP-1α-induced extracellular acidification and Ca2+ mobilization demonstrating functional antagonism. When given alone, the compound did not elicit any responses, suggesting the absence of intrinsic agonist activity. BX 513 inhibited MIP-1α- and RANTES-induced migration in peripheral blood cells in a dose-responsive manner. Selectivity testing against a panel of 7 transmembrane domain receptors indicated that BX 513 is inactive on a number of receptors at concentrations up to 10 μM [2].
In vivo: Currently, there is no animal in-vivo data available.
Clinical trial: Up to now, BX 513 is still in the preclinical development stage.
Reference:
[1] Ng HP, May K, Bauman JG, Ghannam A, Islam I, Liang M, Horuk R, Hesselgesser J, Snider RM, Perez HD, Morrissey MM. Discovery of novel non-peptide CCR1 receptor antagonists. J Med Chem. 1999 Nov 4;42(22):4680-94.
[2] Hesselgesser J, Ng HP, Liang M, Zheng W, May K, Bauman JG, Monahan S, Islam I, Wei GP, Ghannam A, Taub DD, Rosser M, Snider RM, Morrissey MM,Perez HD, Horuk R. Identification and characterization of small molecule functional antagonists of the CCR1 chemokine receptor. J Biol Chem. 1998 Jun 19;273(25):15687-92.
| Cas No. | 1216540-18-9 | SDF | |
| 化学名 | 5-(4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl)-2,2-diphenylpentanenitrile hydrochloride | ||
| Canonical SMILES | ClC1=CC=C(C(CC2)(O)CCN2CCCC(C3=CC=CC=C3)(C4=CC=CC=C4)C#N)C=C1.Cl | ||
| 分子式 | C28H29ClN2O.HCl | 分子量 | 481.46 |
| 溶解度 | <48.15mg/ml in DMSO; <24.07mg/ml in ethanol | 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 | 2.077 mL | 10.3851 mL | 20.7702 mL |
| 5 mM | 0.4154 mL | 2.077 mL | 4.154 mL |
| 10 mM | 0.2077 mL | 1.0385 mL | 2.077 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。