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GRA Ex-25 Sale

(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

GRAEx-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。

GRA Ex-25 Chemical Structure

Cas No.:307983-31-9

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,660.00
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2mg
¥714.00
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5mg
¥1,339.00
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10mg
¥1,874.00
现货
50mg
¥6,248.00
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100mg
¥10,710.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

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.
[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.

Chemical Properties

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
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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
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