GRA Ex-25 | CAS# 307983-31-9 | glucagon receptor inhibitor

MedKoo Cat#: 530399 | Name: GRA Ex-25

Description:

WARNING: This product is for research use only, not for human or veterinary use.

GRA Ex-25 is an inhibitor of glucagon receptor. Inhibiting the interaction between glucagon and its receptor has been reported to control hepatic glucose overproduction and thus GCGR has evolved as an attractive therapeutic target for the treatment of type II diabetes mellitus.

Chemical Structure

GRA Ex-25

CAS# 307983-31-9

Theoretical Analysis

MedKoo Cat#: 530399

Name: GRA Ex-25

CAS#: 307983-31-9

Chemical Formula: C29H36F3N3O5

Exact Mass: 563.2607

Molecular Weight: 563.62

Elemental Analysis: C, 61.80; H, 6.44; F, 10.11; N, 7.46; O, 14.19

Price and Availability

Size	Price	Availability
10mg	USD 350.00	2 Weeks
100mg	USD 950.00	2 Weeks
200mg	USD 1,650.00	2 Weeks
500mg	USD 2,150.00	2 Weeks
1g	USD 3,250.00	2 Weeks

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Synonym

GRA Ex-25; GRA Ex 25; GRA Ex25; GRAEx-25; GRAEx 25; GRAEx25.

IUPAC/Chemical Name

3-(4-((1-((1r,4r)-4-(tert-butyl)cyclohexyl)-3-(4-(trifluoromethoxy)phenyl)ureido)methyl)benzamido)propanoic acid

InChi Key

BZXMLCVDKDXRQY-AFARHQOCSA-N

InChi Code

InChI=1S/C29H36F3N3O5/c1-28(2,3)21-8-12-23(13-9-21)35(27(39)34-22-10-14-24(15-11-22)40-29(30,31)32)18-19-4-6-20(7-5-19)26(38)33-17-16-25(36)37/h4-7,10-11,14-15,21,23H,8-9,12-13,16-18H2,1-3H3,(H,33,38)(H,34,39)(H,36,37)/t21-,23-

SMILES Code

O=C(CCNC(C1=CC=C(C=C1)CN(C(NC2=CC=C(C=C2)OC(F)(F)F)=O)[C@H]3CC[C@@H](CC3)C(C)(C)C)=O)O

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

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

In vitro activity:

TBD

In vivo activity:

TBD

	Solvent	mg/mL	mM
Solubility
	DMF	25.0	44.36
	DMSO	28.5	50.57
	DMF:PBS (pH 7.2) (1:8)	0.1	0.18
	Ethanol	10.0	17.74

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 563.62 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

TBD

In vitro protocol:

TBD

In vivo protocol:

TBD

1: Grover S, Dhanjal JK, Goyal S, Grover A, Sundar D. Computational identification of novel natural inhibitors of glucagon receptor for checking type II diabetes mellitus. BMC Bioinformatics. 2014;15 Suppl 16:S13. doi: 10.1186/1471-2105-15-S16-S13. PubMed PMID: 25521597; PubMed Central PMCID: PMC4290642. 2: Guan HP, Yang X, Lu K, Wang SP, Castro-Perez JM, Previs S, Wright M, Shah V, Herath K, Xie D, Szeto D, Forrest G, Xiao JC, Palyha O, Sun LP, Andryuk PJ, Engel SS, Xiong Y, Lin S, Kelley DE, Erion MD, Davis HR, Wang L. Glucagon receptor antagonism induces increased cholesterol absorption. J Lipid Res. 2015 Nov;56(11):2183-95. doi: 10.1194/jlr.M060897. PubMed PMID: 26373568; PubMed Central PMCID: PMC4617405. 3: Mu J, Jiang G, Brady E, Dallas-Yang Q, Liu F, Woods J, Zycband E, Wright M, Li Z, Lu K, Zhu L, Shen X, Sinharoy R, Candelore ML, Qureshi SA, Shen DM, Zhang F, Parmee ER, Zhang BB. Chronic treatment with a glucagon receptor antagonist lowers glucose and moderately raises circulating glucagon and glucagon-like peptide 1 without severe alpha cell hypertrophy in diet-induced obese mice. Diabetologia. 2011 Sep;54(9):2381-91. doi: 10.1007/s00125-011-2217-2. PubMed PMID: 21695571. 4: Yu R, Wawrowsky K, Zhou C. A natural inactivating mutant of human glucagon receptor exhibits multiple abnormalities in processing and signaling. Endocrinol Nutr. 2011 Jun-Jul;58(6):258-66. doi: 10.1016/j.endonu.2011.04.002. PubMed PMID: 21680267. 5: Mu J, Qureshi SA, Brady EJ, Muise ES, Candelore MR, Jiang G, Li Z, Wu MS, Yang X, Dallas-Yang Q, Miller C, Xiong Y, Langdon RB, Parmee ER, Zhang BB. Anti-diabetic efficacy and impact on amino acid metabolism of GRA1, a novel small-molecule glucagon receptor antagonist. PLoS One. 2012;7(11):e49572. doi: 10.1371/journal.pone.0049572. PubMed PMID: 23185367; PubMed Central PMCID: PMC3501516. 6: Xu Y, Xie X. Glucagon receptor mediates calcium signaling by coupling to G alpha q/11 and G alpha i/o in HEK293 cells. J Recept Signal Transduct Res. 2009 Dec;29(6):318-25. doi: 10.3109/10799890903295150. PubMed PMID: 19903011. 7: Ikegami T, Krilov L, Meng J, Patel B, Chapin-Kennedy K, Bouscarel B. Decreased glucagon responsiveness by bile acids: a role for protein kinase Calpha and glucagon receptor phosphorylation. Endocrinology. 2006 Nov;147(11):5294-302. PubMed PMID: 16916948. 8: Malmgren S, Ahrén B. DPP-4 inhibition contributes to the prevention of hypoglycaemia through a GIP-glucagon counterregulatory axis in mice. Diabetologia. 2015 May;58(5):1091-9. doi: 10.1007/s00125-015-3518-7. PubMed PMID: 25660260. 9: Gong N, Xiao Q, Zhu B, Zhang CY, Wang YC, Fan H, Ma AN, Wang YX. Activation of spinal glucagon-like peptide-1 receptors specifically suppresses pain hypersensitivity. J Neurosci. 2014 Apr 9;34(15):5322-34. doi: 10.1523/JNEUROSCI.4703-13.2014. PubMed PMID: 24719110. 10: Li XC, Carretero OA, Shao Y, Zhuo JL. Glucagon receptor-mediated extracellular signal-regulated kinase 1/2 phosphorylation in rat mesangial cells: role of protein kinase A and phospholipase C. Hypertension. 2006 Mar;47(3):580-5. PubMed PMID: 16391176; PubMed Central PMCID: PMC2367309. 11: Sélley E, Kun S, Szijártó IA, Kertész M, Wittmann I, Molnár GA. Vasodilator Effect of Glucagon: Receptorial Crosstalk Among Glucagon, GLP-1, and Receptor for Glucagon and GLP-1. Horm Metab Res. 2016 Jul;48(7):476-83. doi: 10.1055/s-0042-101794. PubMed PMID: 26975347. 12: Gagnon J, Anini Y. Glucagon stimulates ghrelin secretion through the activation of MAPK and EPAC and potentiates the effect of norepinephrine. Endocrinology. 2013 Feb;154(2):666-74. doi: 10.1210/en.2012-1994. PubMed PMID: 23307791. 13: Li XC, Carretero OA, Zhuo JL. Cross-talk between angiotensin II and glucagon receptor signaling mediates phosphorylation of mitogen-activated protein kinases ERK 1/2 in rat glomerular mesangial cells. Biochem Pharmacol. 2006 Jun 14;71(12):1711-9. PubMed PMID: 16643859; PubMed Central PMCID: PMC2276839. 14: Ojima A, Ishibashi Y, Matsui T, Maeda S, Nishino Y, Takeuchi M, Fukami K, Yamagishi S. Glucagon-like peptide-1 receptor agonist inhibits asymmetric dimethylarginine generation in the kidney of streptozotocin-induced diabetic rats by blocking advanced glycation end product-induced protein arginine methyltranferase-1 expression. Am J Pathol. 2013 Jan;182(1):132-41. doi: 10.1016/j.ajpath.2012.09.016. PubMed PMID: 23159951. 15: Farr S, Baker C, Naples M, Taher J, Iqbal J, Hussain M, Adeli K. Central Nervous System Regulation of Intestinal Lipoprotein Metabolism by Glucagon-Like Peptide-1 via a Brain-Gut Axis. Arterioscler Thromb Vasc Biol. 2015 May;35(5):1092-100. doi: 10.1161/ATVBAHA.114.304873. PubMed PMID: 25675997. 16: Burmeister MA, Ayala J, Drucker DJ, Ayala JE. Central glucagon-like peptide 1 receptor-induced anorexia requires glucose metabolism-mediated suppression of AMPK and is impaired by central fructose. Am J Physiol Endocrinol Metab. 2013 Apr 1;304(7):E677-85. doi: 10.1152/ajpendo.00446.2012. PubMed PMID: 23341495. 17: Artinian SB, Al Lafi SM, Boutary SS, Bitar KM, Zwainy NS, Bikhazi AB. Assessment of glucagon-like peptide-1 analogue and renin inhibitor on the binding and regulation of GLP-1 receptor in type 1 diabetic rat hearts. Exp Diabetes Res. 2011;2011:489708. doi: 10.1155/2011/489708. PubMed PMID: 21747829; PubMed Central PMCID: PMC3124137. 18: Maida A, Hansotia T, Longuet C, Seino Y, Drucker DJ. Differential importance of glucose-dependent insulinotropic polypeptide vs glucagon-like peptide 1 receptor signaling for beta cell survival in mice. Gastroenterology. 2009 Dec;137(6):2146-57. doi: 10.1053/j.gastro.2009.09.004. PubMed PMID: 19766644. 19: Smith EP, An Z, Wagner C, Lewis AG, Cohen EB, Li B, Mahbod P, Sandoval D, Perez-Tilve D, Tamarina N, Philipson LH, Stoffers DA, Seeley RJ, D'Alessio DA. The role of β cell glucagon-like peptide-1 signaling in glucose regulation and response to diabetes drugs. Cell Metab. 2014 Jun 3;19(6):1050-7. doi: 10.1016/j.cmet.2014.04.005. PubMed PMID: 24836562; PubMed Central PMCID: PMC4109713. 20: Katagiri D, Hamasaki Y, Doi K, Okamoto K, Negishi K, Nangaku M, Noiri E. Protection of glucagon-like peptide-1 in cisplatin-induced renal injury elucidates gut-kidney connection. J Am Soc Nephrol. 2013 Dec;24(12):2034-43. doi: 10.1681/ASN.2013020134. PubMed PMID: 24092928; PubMed Central PMCID: PMC3839550.

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Description:

Chemical Structure

Theoretical Analysis

Price and Availability

Preparing Stock Solutions

View History

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