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MedKoo Cat#: 525608 | Name: GNF351
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Description:

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

GNF351 is a novel potent aryl hydrocarbon receptor (AHR) antagonist with the capacity to inhibit both DRE-dependent and -independent activity.

Chemical Structure

GNF351
GNF351
CAS#1227634-69-6

Theoretical Analysis

MedKoo Cat#: 525608

Name: GNF351

CAS#: 1227634-69-6

Chemical Formula: C24H25N7

Exact Mass: 411.2171

Molecular Weight: 411.51

Elemental Analysis: C, 70.05; H, 6.12; N, 23.83

Price and Availability

Size Price Availability Quantity
5mg USD 350.00 2 Weeks
10mg USD 600.00 2 Weeks
25mg USD 1,050.00 2 Weeks
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Related CAS #
No Data
Synonym
GNF351; GNF-351 GNF 351; NSC835774; NSC 835774; NSC-835774
IUPAC/Chemical Name
8-(2-(1H-indol-3-yl)ethyl)-9-isopropyl-2-(5-methylpyridin-3-yl)-9H-purin-6-amine
InChi Key
WWERDIHAUJLVQP-UHFFFAOYSA-N
InChi Code
InChI=1S/C24H25N7/c1-14(2)31-20(9-8-16-13-27-19-7-5-4-6-18(16)19)28-21-22(25)29-23(30-24(21)31)17-10-15(3)11-26-12-17/h4-7,10-14,27H,8-9H2,1-3H3,(H2,25,29,30)
SMILES Code
NC1=C2N=C(CCC3=CNC4=C3C=CC=C4)N(C(C)C)C2=NC(C5=CC(C)=CN=C5)=N1
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

Preparing Stock Solutions

The following data is based on the product molecular weight 411.51 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.

Recalculate based on batch purity %
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
1: van den Bogaard EH, Podolsky MA, Smits JP, Cui X, John C, Gowda K, Desai D, Amin SG, Schalkwijk J, Perdew GH, Glick AB. Genetic and pharmacological analysis identifies a physiological role for the AHR in epidermal differentiation. J Invest Dermatol. 2015 May;135(5):1320-8. doi: 10.1038/jid.2015.6. Epub 2015 Jan 20. PubMed PMID: 25602157; PubMed Central PMCID: PMC4402116. 2: Nguyen NT, Nakahama T, Nguyen CH, Tran TT, Le VS, Chu HH, Kishimoto T. Aryl hydrocarbon receptor antagonism and its role in rheumatoid arthritis. J Exp Pharmacol. 2015 Dec 1;7:29-35. doi: 10.2147/JEP.S63549. eCollection 2015. Review. PubMed PMID: 27186143; PubMed Central PMCID: PMC4863532. 3: Perkins A, Phillips JL, Kerkvliet NI, Tanguay RL, Perdew GH, Kolluri SK, Bisson WH. A Structural Switch between Agonist and Antagonist Bound Conformations for a Ligand-Optimized Model of the Human Aryl Hydrocarbon Receptor Ligand Binding Domain. Biology (Basel). 2014 Oct 17;3(4):645-69. doi: 10.3390/biology3040645. PubMed PMID: 25329374; PubMed Central PMCID: PMC4280506. 4: Liu T, Qian G, Wang W, Zhang Y. Molecular docking to understand the metabolic behavior of GNF-351 by CYP3A4 and its potential drug-drug interaction with ketoconazole. Eur J Drug Metab Pharmacokinet. 2015 Jun;40(2):235-8. doi: 10.1007/s13318-014-0201-1. Epub 2014 Apr 23. PubMed PMID: 24756863. 5: Fang ZZ, Krausz KW, Nagaoka K, Tanaka N, Gowda K, Amin SG, Perdew GH, Gonzalez FJ. In vivo effects of the pure aryl hydrocarbon receptor antagonist GNF-351 after oral administration are limited to the gastrointestinal tract. Br J Pharmacol. 2014 Apr;171(7):1735-46. doi: 10.1111/bph.12576. PubMed PMID: 24417285; PubMed Central PMCID: PMC3966752. 6: Lahoti TS, Hughes JM, Kusnadi A, John K, Zhu B, Murray IA, Gowda K, Peters JM, Amin SG, Perdew GH. Aryl hydrocarbon receptor antagonism attenuates growth factor expression, proliferation, and migration in fibroblast-like synoviocytes from patients with rheumatoid arthritis. J Pharmacol Exp Ther. 2014 Feb;348(2):236-45. doi: 10.1124/jpet.113.209726. Epub 2013 Dec 5. PubMed PMID: 24309559; PubMed Central PMCID: PMC3912548. 7: Lahoti TS, John K, Hughes JM, Kusnadi A, Murray IA, Krishnegowda G, Amin S, Perdew GH. Aryl hydrocarbon receptor antagonism mitigates cytokine-mediated inflammatory signalling in primary human fibroblast-like synoviocytes. Ann Rheum Dis. 2013 Oct;72(10):1708-16. doi: 10.1136/annrheumdis-2012-202639. Epub 2013 Jan 24. PubMed PMID: 23349129; PubMed Central PMCID: PMC4041386. 8: DiNatale BC, Smith K, John K, Krishnegowda G, Amin SG, Perdew GH. Ah receptor antagonism represses head and neck tumor cell aggressive phenotype. Mol Cancer Res. 2012 Oct;10(10):1369-79. doi: 10.1158/1541-7786.MCR-12-0216. Epub 2012 Aug 21. PubMed PMID: 22912337; PubMed Central PMCID: PMC3477495. 9: Smith KJ, Murray IA, Tanos R, Tellew J, Boitano AE, Bisson WH, Kolluri SK, Cooke MP, Perdew GH. Identification of a high-affinity ligand that exhibits complete aryl hydrocarbon receptor antagonism. J Pharmacol Exp Ther. 2011 Jul;338(1):318-27. doi: 10.1124/jpet.110.178392. Epub 2011 Apr 14. PubMed PMID: 21493753; PubMed Central PMCID: PMC3126639.