AR 231453
目录号 : GC14944
An agonist of GPR119
Cas No.:733750-99-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
AR 231453 is an agonist of GPR119 with EC50 value of 0.68nM [1].
AR 231453 is the first subnanomolar agonist of GPR119. It is highly selective against GPR119 over a 76 receptor and enzyme profiling panel (CEREP) including the known incretin receptors. It also has no activity to 140 known and orphan GPCRs in melanophore dispersion assays. Besides that, AR 231453 is reported to stimulate cAMP production via endogenously expressed GPR119 in HIT-T15 cell line with EC50 value of 4.7nM [1].
In vivo assay shows that AR 231453 has activity in rodents. It can enhance glucose-dependent insulin release and improve oral glucose tolerance in wild-type C57/bl6J mice but not in GPR119-deficient mice at a dose of 20 mg/kg. Due to its activity to active GPR119, AR 231453 is expected to be a potent anti-diabetic agent [1].
References:
[1] Semple G, Fioravanti B, Pereira G, Calderon I, Uy J, Choi K, Xiong Y, Ren A, Morgan M, Dave V, Thomsen W, Unett DJ, Xing C, Bossie S, Carroll C, Chu ZL, Grottick AJ, Hauser EK, Leonard J, Jones RM. Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119. J Med Chem. 2008 Sep 11;51(17):5172-5.
| Cas No. | 733750-99-7 | SDF | |
| 化学名 | N-(2-fluoro-4-methylsulfonylphenyl)-5-nitro-6-[4-(3-propan-2-yl-1,2,4-oxadiazol-5-yl)piperidin-1-yl]pyrimidin-4-amine | ||
| Canonical SMILES | CC(C)C1=NOC(=N1)C2CCN(CC2)C3=C(C(=NC=N3)NC4=C(C=C(C=C4)S(=O)(=O)C)F)[N+](=O)[O-] | ||
| 分子式 | C21H24FN7O5S | 分子量 | 505.52 |
| 溶解度 | ≥ 49.3 mg/mL in DMSO with gentle warming | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.9782 mL | 9.8908 mL | 19.7816 mL |
| 5 mM | 0.3956 mL | 1.9782 mL | 3.9563 mL |
| 10 mM | 0.1978 mL | 0.9891 mL | 1.9782 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。