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 : GC31379
GRA Ex-25 是一种有效的胰高血糖素受体抑制剂，对大鼠和人类胰高血糖素受体的 IC50 分别为 56 和 55 nM。
Cas No.:307983-31-9
Sample solution is provided at 25 µL, 10mM.
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GRA Ex-25 is a potent glucagon receptor inhibitor with IC50 of 56 and 55 nM for rat and human glucagon receptors, respectively. GRA Ex-25 binds to the human glucagon receptor (h-GlucRbind) with a Ki of 63 nM and moderates glucagon-induced adenylate cyclase inhibition (h-GlucRcyclase) with a Ki of 254 nM[2]. GRA Ex-25 has similar affinity for rat and human glucagon receptors (IC50 of 56 and 55 nM, respectively). GRA Ex-25 (3 mg/kg, iv) reduces blood glucose levels induced by exogenous glucagon in a rat model, possibly due to direct inhibition of glucagon-stimulated hepatic glucose output[2].
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.
[2].Lau J, Behrens C, et,al . New beta-alanine derivatives are orally available glucagon receptor antagonists. J Med Chem. 2007 Jan 11;50(1):113-28. doi: 10.1021/jm058026u. PMID: 17201415.
GRA Ex-25 是一种有效的胰高血糖素受体抑制剂，对大鼠和人类胰高血糖素受体的 IC50 分别为 56 和 55 nM。GRA Ex-25 与人类胰高血糖素受体 (h-GlucRbind) 结合，Ki 为 63 nM，并缓和胰高血糖素诱导的腺苷酸环化酶抑制 (h-GlucRcyclase)，Ki 为 254 nM[2]。GRA Ex-25 对大鼠和人类胰高血糖素受体具有相似的亲和力（IC50 分别为 56 和 55 nM）。GRA Ex-25（3 mg/kg，iv）降低大鼠模型中外源性胰高血糖素诱导的血糖水平，可能是由于直接抑制胰高血糖素刺激的肝葡萄糖输出[2]。
| Molecular Docking of the Receptor¨CLigand Complex[1]: | |
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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. |
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Applications |
Gra Ex-25 is bonded to Ser350 and Lys349 amino acids of GCGR through hydrogen bonding. |
| Animal experiment [2]: | |
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Animal models |
Glucagon challenged rats |
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Preparation Method |
Anesthetized animals were given an intravenous dose of GRA Ex-25 min prior to a 3 ¦̧/kg glucagon load. |
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Dosage form |
1-3mg/ml GRA Ex-25 |
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Applications |
GRA Ex-25 (3 mg/kg) significantly reduced blood glucose levels in rats with elevated blood glucose induced by exogenous glucagon. |
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References:
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| 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 | |||
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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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet