GCGR antagonist 2
Modify Date: 2024-01-12 11:21:41
GCGR antagonist 2 structure
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Common Name | GCGR antagonist 2 | ||
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| CAS Number | 280134-25-0 | Molecular Weight | 450.53200 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C28H26N4O2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of GCGR antagonist 2GCGR antagonist 2, a Furan-2-carbohydrazide, is an orally active glucagon receptor antagonist. GCGR antagonist 2 binds to hGluR with an Kd value of 2.3 nM, and inhibits rat receptor with an IC50 value of 0.43 nM. GCGR antagonist 2 inhibits glucagon-stimulated glycogenolysis[1][2]. |
| Name | 3-Cyano-4-hydroxy-N'-{(E)-[1-(2,3,5,6-tetramethylbenzyl)-1H-indol -4-yl]methylene}benzohydrazide |
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| Description | GCGR antagonist 2, a Furan-2-carbohydrazide, is an orally active glucagon receptor antagonist. GCGR antagonist 2 binds to hGluR with an Kd value of 2.3 nM, and inhibits rat receptor with an IC50 value of 0.43 nM. GCGR antagonist 2 inhibits glucagon-stimulated glycogenolysis[1][2]. |
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| Related Catalog | |
| In Vitro | GCGR antagonist 2 (化合物 74) (25 nM, 250 nM 和 2500 nM；70 min) 抑制 5 nM 胰高血糖素诱导的原代大鼠肝细胞糖原分解，IC50 为 160 nM[1]。 GCGR antagonist 2 (25 nM, 250 nM 和 2500 nM；60 min) 在 BHK 细胞中，抑制重组人胰高血糖素受体抑制胰高血糖素刺激的 cAMP 水平[1]。 GCGR antagonist 2 (1 nM, 10 nM 和100 nM；60 min) 抑制分离的大鼠肝脏胰高血糖素受体抑制 BHK 细胞中胰高血糖素刺激的 cAMP 水平[1]。 |
| In Vivo | GCGR antagonist 2 (0.5 mg/kg 静脉注射，或 2 mg/kg 口服；单次剂量) 的平均半衰期分别为 1.11 h 和 1.40 h[1]。 GCGR antagonist 2 (0 mg/kg, 3 mg/kg 和 10 mg/kg；口服) 在受胰高血糖素刺激的 Sprague-Dawley 大鼠中，至少部分地抑制了内源性胰高血糖素，并维持正糖状态[1]。 |
| References |
| Molecular Formula | C28H26N4O2 |
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| Molecular Weight | 450.53200 |
| Exact Mass | 450.20600 |
| PSA | 93.90000 |
| LogP | 5.83918 |