GYKI-53784

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

MedKoo CAT#: 522534

CAS#: 161832-71-9

Description: 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

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GYKI-53784
CAS# 161832-71-9
Instruction

Theoretical Analysis

MedKoo Cat#: 522534
Name: GYKI-53784
CAS#: 161832-71-9
Chemical Formula: C19H20N4O3
Exact Mass: 352.15
Molecular Weight: 352.394
Elemental Analysis: C, 64.76; H, 5.72; N, 15.90; O, 13.62

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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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:

Biological target:
In vitro activity:
In vivo activity:

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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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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.