GRA Ex-25

SKU: orb1225352

Description

A potent glucagon receptor inhibitor with IC50 of 56 and 55 nM for rat and human glucagon receptors; binds to human glucagon receptor with Ki of 63 nM, moderately inhibits glucagon induced adenylate cyclase (Ki=254 nM); significantly reduces blood glucose caused by exogenous administration of glucagon in rat model (3 mg/kg, i.v.).Diabetes Preclinical.

Key Properties

• CAS Number: 307983-31-9
• MW: 563.6085
• Purity: >98% (HPLC)
• Formula: C₂₉H₃₆F₃N₃O₅
• SMILES: C[C@](C1CC[C@H](N(C(NC2C=CC(OC(F)(F)F)=CC=2)=O)CC2C=CC(C(NCCC(O)=O)=O)=CC=2)CC1)(C)C
• Target: Glucagon Receptor
• Solubility: DMSO: ≥ 32 mg/mL

Bioactivity

• In Vivo:
  GRA Ex-25 (3 mg/kg, i. v.) significantly reduces blood glucose caused by exogenous administration of glucagon in rat model. GRA Ex-25 is able to inhibit the rise in blood glucose levels elicited by exogenous administered glucagon, most likely because of the direct inhibition of glucagon stimulated hepatic glucose output.
• In Vitro:
  GRA Ex-25 binds a human glucagon receptor (h-GlucRbind) with Ki of 63 nM and a moderate glucagon induced adenylate cyclase inhibition (h-GlucRcyclase) with Ki of 254 nM under our assay conditions. GRA Ex-25 has similar affinity to the rat and human glucagon receptors (IC50 = 56 and 55 nM, respectively).

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GRA Ex-25 | GRA Ex 25 | GRA Ex25 | GRAEx-25

Quick Database Links

Gene Symbol

Glucagon Receptor