1. GPCR/G Protein
  2. Glucagon Receptor
  3. GRA Ex-25

GRA Ex-25 

Cat. No.: HY-50675 Purity: 99.70%
Handling Instructions

GRA Ex-25 is an inhibitor of glucagon receptor, with IC50 of 56 and 55 nM for rat and human glucagon receptors, respectively.

For research use only. We do not sell to patients.

GRA Ex-25 Chemical Structure

GRA Ex-25 Chemical Structure

CAS No. : 307983-31-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 223 In-stock
Estimated Time of Arrival: December 31
2 mg USD 96 In-stock
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 252 In-stock
Estimated Time of Arrival: December 31
50 mg USD 840 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1440 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

GRA Ex-25 is an inhibitor of glucagon receptor, with IC50 of 56 and 55 nM for rat and human glucagon receptors, respectively.

IC50 & Target

IC50: 56 nM (rat glucagon receptor), 55 nM (human glucagon receptor)[2]

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[1]. GRA Ex-25 has similar affinity to the rat and human glucagon receptors (IC50=56 and 55 nM, respectively)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

563.61

Formula

C₂₉H₃₆F₃N₃O₅

CAS No.
SMILES

O=C(O)CCNC(C1=CC=C(CN([[email protected]]2CC[[email protected]](C(C)(C)C)CC2)C(NC3=CC=C(OC(F)(F)F)C=C3)=O)C=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 32 mg/mL (56.78 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.44 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.44 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.44 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[2]

Non-fasted male Sprague Dawley rats (200 g) are maintained in the anaesthetized state during the test by s.c. administration of a 1:1 mixture of Hypnorm (fentanyl, 0.05 mg/mL and fluanizone, 2.5 mg/mL) and Dormicum (Midazolam, 1.25 mg/mL). Acatheter is inserted in a jugular vein for administration of compounds. Approximately 60 min after initiation of anesthesia, test compounds (0, 1, 3, 10 and 30 mg/kg) and glucagon (3 μg/kg) are administered in 5 min intervals, respectively. Samples for determination of blood glucose concentrations are taken from the tail tip 25 and 5 min prior to administration of the compound to represent average basal values and again 10 min after administration of glucagon (time for peak response of glucagon). The results are expressed as delta values calculated as the value obtained 10 min after alucagon administration minus the average of the two basal values.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

GRA Ex-25GRA Ex25GRA Ex 25Glucagon ReceptorGCGRInhibitorinhibitorinhibit

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Product Name:
GRA Ex-25
Cat. No.:
HY-50675
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