GRA Ex-25
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MedKoo CAT#: 530399

CAS#: 307983-31-9

Description: 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.


Price and Availability

Size Price Shipping out time Quantity
100mg USD 950 2 Weeks
200mg USD 1650 2 Weeks
500mg USD 2150 2 Weeks
1g USD 3250 2 Weeks
2g USD 5850 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-10-28. Prices are subject to change without notice.

GRA Ex-25, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 530399
Name: GRA Ex-25
CAS#: 307983-31-9
Chemical Formula: C29H36F3N3O5
Exact Mass: 563.2607
Molecular Weight: 563.6182
Elemental Analysis: C, 61.80; H, 6.44; F, 10.11; N, 7.46; O, 14.19


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

IUPAC/Chemical Name: 3-(4-((1-(4-(tert-butyl)cyclohexyl)-3-(4-(trifluoromethoxy)phenyl)ureido)methyl)benzamido)propanoic acid

InChi Key: BZXMLCVDKDXRQY-LOSWNTGBSA-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: 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


Technical Data

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


References

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.