GRA Ex-25
(Synonyms: N-[4-[[[反式-4-(1,1-二甲基乙基)环己基][[[4-(三氟甲氧基)苯基]氨基]羰基]氨基]甲基]苄基]-B-丙氨酸) 目录号 : GC31379GRAEx-25是一种glucagon受体的抑制剂,抑制大鼠和人的glucagon受体,IC50值分别为56和55nM。
Cas No.:307983-31-9
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Molecular Docking of the Receptor¨CLigand Complex[1]: | |
Preparation Method |
The receptor and small ligand molecules Gra EX-25 were used to conduct molecular docking of 5XEZ-A with dauricine and Gra Ex-25 using Vina computing under the calculation conditions screened. In addition, scoring data and PyMol were used to analyze the ligand and receptor amino acid binding way. |
Applications |
Gra Ex-25 is bonded to Ser350 and Lys349 amino acids of GCGR through hydrogen bonding. |
Animal experiment [2]: | |
Animal models |
Glucagon challenged rats |
Preparation Method |
Anesthetized animals were given an intravenous dose of GRA Ex-25 min prior to a 3 ¦̧/kg glucagon load. |
Dosage form |
1-3mg/ml GRA Ex-25 |
Applications |
GRA Ex-25 (3 mg/kg) significantly reduced blood glucose levels in rats with elevated blood glucose induced by exogenous glucagon. |
References: [1]. Li L, Dai S, et,al . Antagonistic Effect and In Vitro Activity of Dauricine on Glucagon Receptor. J Nat Prod. 2022 Aug 26;85(8):2035-2043. doi: 10.1021/acs.jnatprod.2c00446. Epub 2022 Jul 14. PMID: 35834753. |
Cas No. | 307983-31-9 | SDF | |
别名 | N-[4-[[[反式-4-(1,1-二甲基乙基)环己基][[[4-(三氟甲氧基)苯基]氨基]羰基]氨基]甲基]苄基]-B-丙氨酸 | ||
Canonical SMILES | O=C(O)CCNC(C1=CC=C(CN([C@H]2CC[C@H](C(C)(C)C)CC2)C(NC3=CC=C(OC(F)(F)F)C=C3)=O)C=C1)=O | ||
分子式 | C29H36F3N3O5 | 分子量 | 563.61 |
溶解度 | DMSO : ≥ 32 mg/mL (56.78 mM) | 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 | 1.7743 mL | 8.8714 mL | 17.7428 mL |
5 mM | 0.3549 mL | 1.7743 mL | 3.5486 mL |
10 mM | 0.1774 mL | 0.8871 mL | 1.7743 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。