AR-M 1896
目录号 : GC11955
选择性 GAL2 激动剂
Cas No.:367518-31-8
Sample solution is provided at 25 µL, 10mM.
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Binding IC50: 1.76 nM for rGalR2; 879 nM for hGalR1
Galanin is a 29-aa neuropeptide with a complex role in pain processing. Galanin receptor subtypes are present in dorsal root ganglia and spinal cord with a differential distribution. Three galanin receptors, GalR1, GalR2 and GalR3, have been identified and cloned. AR-M1896 is a specific galanin R2 (GalR2) agonist.
In vitro: Additional removal of the glycine residue in position 1 resulted in AR-M1896 with almost unchanged GalR2 affinity and functional activity, and 500-fold selectivity for GalR2-Rs over GalR1-Rs. This compound represents a truly GalR2-selective galanin analog and, thus, could be used as a pharmacological tool to differentiate between these two receptors [1].
In vivo: In normal rats mechanical and cold allodynia of the hindpaw are induced by intrathecal infusion of low-dose galanin. The same effect is seen with equimolar doses of AR-M1896 or AR-M961 (an agonist both at GalR1 and GalR2 receptors). In allodynic Bennett model rats, the mechanical threshold dose-dependently increased after intrathecal injection of a high AR-M961dose, whereas no effect was observed in the control or AR-M1896 group. No effect of either compounds was observed in nonallodynic Bennett model rats [1].
Clinical trial: Up to now, AR-M1896 is still in the preclinical development stage.
Reference:
[1] Liu HX, Brumovsky P, Schmidt R, Brown W, Payza K, Hodzic L, Pou C, Godbout C, Hökfelt T.
Receptor subtype-specific pronociceptive and analgesic actions of galanin in the spinal cord: selective actions via GalR1 and GalR2 receptors. Proc Natl Acad Sci U S A. 2001 Aug 14;98(17):9960-4.
| Cas No. | 367518-31-8 | SDF | |
| Canonical SMILES | CC(C[C@@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/C/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](N)([H])CC1=CNC2=CC=CC=C12)([H])[C@@](O)([H])C)([H])CC(C)C)([H])CC(O)=N)([H])CO)([H])C)([H])CC3=CC=C(O)C=C3)([H])CC(C)C)([H])C(O)=N)C | ||
| 分子式 | C54H81N13O14 | 分子量 | 1136.31 |
| 溶解度 | Soluble to 1 mg/ml in 20% formic acid | 储存条件 | Desiccate 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 | 0.88 mL | 4.4002 mL | 8.8004 mL |
| 5 mM | 0.176 mL | 0.88 mL | 1.7601 mL |
| 10 mM | 0.088 mL | 0.44 mL | 0.88 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet