MedKoo Cat#: 522534 | Name: GYKI-53784

Description:

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

GYKI-53784, also known as LY 303070, is a potent and selective AMPA receptor antagonist. GYKI 53784 blocks action potential generation and excitotoxicity in the guinea pig cochlea. GYKI 53784 had the same potency as DNQX and was 10 times more potent than GYKI 52466 in reducing auditory nerve activity. GYKI 53784 completely blocked excitotoxicity (i.e. destruction of the afferent nerve endings) induced by AMPA and kainate. The histochemical detection of Co(2+) uptake was used to study Ca(2+) influx within the primary auditory nerve cells.

Chemical Structure

GYKI-53784
GYKI-53784
CAS#161832-71-9

Theoretical Analysis

MedKoo Cat#: 522534

Name: GYKI-53784

CAS#: 161832-71-9

Chemical Formula: C19H20N4O3

Exact Mass: 352.1535

Molecular Weight: 352.39

Elemental Analysis: C, 64.76; H, 5.72; N, 15.90; O, 13.62

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Synonym
GYKI-53784; GYKI53784; GYKI 53784; LY 303070; LY-303070; LY303070.
IUPAC/Chemical Name
(R)-5-(4-aminophenyl)-N,8-dimethyl-8,9-dihydro-7H-[1,3]dioxolo[4',5':4,5]benzo[1,2-d][1,2]diazepine-7-carboxamide
InChi Key
SMGACXZFVXKEAX-LLVKDONJSA-N
InChi Code
InChI=1S/C19H20N4O3/c1-11-7-13-8-16-17(26-10-25-16)9-15(13)18(22-23(11)19(24)21-2)12-3-5-14(20)6-4-12/h3-6,8-9,11H,7,10,20H2,1-2H3,(H,21,24)/t11-/m1/s1
SMILES Code
O=C(N1N=C(C2=CC=C(N)C=C2)C3=CC(OCO4)=C4C=C3C[C@H]1C)NC
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, not in water
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 352.39 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: Ruel J, Guitton MJ, Puell JL. Negative allosteric modulation of AMPA-preferring receptors by the selective isomer GYKI 53784 (LY303070), a specific non-competitive AMPA antagonist. CNS Drug Rev. 2002 Fall;8(3):235-54. Review. PubMed PMID: 12353057. 2: Ruel J, Bobbin RP, Vidal D, Pujol R, Puel JL. The selective AMPA receptor antagonist GYKI 53784 blocks action potential generation and excitotoxicity in the guinea pig cochlea. Neuropharmacology. 2000 Aug 23;39(11):1959-73. PubMed PMID: 10963740. 3: Kapus G, Bódi I, Pataki A, Gueritaud J, Székely JI, Tarnawa I. Differential modulation of the GYKI 53784-induced inhibition of AMPA currents by various AMPA-positive modulators in cerebellar Purkinje cells. Eur J Pharmacol. 2000 May 26;397(1):43-7. PubMed PMID: 10844097. 4: Ruiz A, Durand J. Modulation of kainate-induced responses by pentobarbitone and GYKI-53784 in rat abducens motoneurons in vivo. Brain Res. 1999 Feb 13;818(2):421-30. PubMed PMID: 10082828.