GRA Ex-25

Name: GRA Ex-25
Brand: MedChemExpress
SKU: HY-50675
Rating: 4.5 (1 reviews)

Cat. No.: HY-50675 Purity: 98.59%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 307983-31-9

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 172	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 172	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 139	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 211	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 422	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 633	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 950	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Protocol
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References
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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 K_i of 63 nM and a moderate glucagon induced adenylate cyclase inhibition (h-GlucRcyclase) with K_i 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].

MedChemExpress (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].

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

Molecular Weight

563.61

Formula

C₂₉H₃₆F₃N₃O₅

CAS No.

307983-31-9

Appearance

Solid

Color

White to off-white

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 32 mg/mL (56.78 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.69 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.69 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.59%

Select Batch:

Data Sheet (271 KB) SDS (393 KB)

COA (246 KB) HNMR (288 KB) LCMS (269 KB)

Handling Instructions (2659 KB)

References

[1]. Kurukulasuriya R, et al. Biaryl amide glucagon receptor antagonists. Bioorg Med Chem Lett. 2004 May 3;14(9):2047-50. [Content Brief]

[2]. Kurukulasuriya R, et al. Biaryl amide glucagon receptor antagonists. Bioorg Med Chem Lett. 2004 May 3;14(9):2047-50. [Content Brief]

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

[1]. Kurukulasuriya R, et al. Biaryl amide glucagon receptor antagonists. Bioorg Med Chem Lett. 2004 May 3;14(9):2047-50. [Content Brief]

[2]. Kurukulasuriya R, et al. Biaryl amide glucagon receptor antagonists. Bioorg Med Chem Lett. 2004 May 3;14(9):2047-50. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7743 mL	8.8714 mL	17.7428 mL	44.3570 mL
	5 mM	0.3549 mL	1.7743 mL	3.5486 mL	8.8714 mL
	10 mM	0.1774 mL	0.8871 mL	1.7743 mL	4.4357 mL
	15 mM	0.1183 mL	0.5914 mL	1.1829 mL	2.9571 mL
	20 mM	0.0887 mL	0.4436 mL	0.8871 mL	2.2179 mL
	25 mM	0.0710 mL	0.3549 mL	0.7097 mL	1.7743 mL
	30 mM	0.0591 mL	0.2957 mL	0.5914 mL	1.4786 mL
	40 mM	0.0444 mL	0.2218 mL	0.4436 mL	1.1089 mL
	50 mM	0.0355 mL	0.1774 mL	0.3549 mL	0.8871 mL

GRA Ex-25 Related Classifications

Metabolic Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GRA Ex-25307983-31-9GRA Ex25GRA Ex 25GCGRGlucagon ReceptorInhibitorinhibitorinhibit

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GRA Ex-25

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