For research use only. Not for therapeutic Use.
LY3130481 (Cat.No:I007835) is the the first α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonist that is dependent on the presence of TARP γ-8. LY3130481 is fully protective against pentylenetetrazole-induced convulsions in rats without the motor impairment associated with non-TARP-dependent AMPA receptor antagonists. Compound (−)-25 could be utilized to provide proof of concept for antiepileptic efficacy with reduced motor side effects in patients.
| Catalog Number | I007835 |
| CAS Number | 1610802-47-5 |
| Synonyms | LY3130481; LY-3130481; LY 3130481.;(S)-6-(1-(1-(5-(2-hydroxyethoxy)pyridin-2-yl)-1H-pyrazol-3-yl)ethyl)benzo[d]thiazol-2(3H)-one |
| Molecular Formula | C19H18N4O3S |
| Purity | ≥95% |
| Target | AMPA receptor antagonist |
| Solubility | Soluble in DMSO, not in water |
| Storage | 0 - 4°C for short term , or -20°C for long term. |
| IUPAC Name | 6-[(1S)-1-[1-[5-(2-hydroxyethoxy)pyridin-2-yl]pyrazol-3-yl]ethyl]-3H-1,3-benzothiazol-2-one |
| InChI | InChI=1S/C19H18N4O3S/c1-12(13-2-4-16-17(10-13)27-19(25)21-16)15-6-7-23(22-15)18-5-3-14(11-20-18)26-9-8-24/h2-7,10-12,24H,8-9H2,1H3,(H,21,25)/t12-/m0/s1 |
| InChIKey | HLTKOFPQDKJCAN-LBPRGKRZSA-N |
| SMILES | CC(C1=CC2=C(C=C1)NC(=O)S2)C3=NN(C=C3)C4=NC=C(C=C4)OCCO |
| Reference | </br>1:Kato AS, Burris KD, Gardinier KM, Gernert DL, Porter WJ, Reel J, Ding C, Tu Y, Schober DA, Lee MR, Heinz BA, Fitch TE, Gleason SD, Catlow JT, Yu H, Fitzjohn SM, Pasqui F, Wang H, Qian Y, Sher E, Zwart R, Wafford KA, Rasmussen K, Ornstein PL, Isaac JT, Nisenbaum ES, Bredt DS, Witkin JM. Forebrain-selective AMPA-receptor antagonism guided by TARP γ-8 as an antiepileptic mechanism. Nat Med. 2016 Nov 7. doi: 10.1038/nm.4221. [Epub ahead of print] PubMed PMID: 27820603.</br>2:Gardinier KM, Gernert DL, Porter WJ, Reel JK, Ornstein PL, Spinazze P, Stevens FC, Hahn P, Hollinshead SP, Mayhugh D, Schkeryantz J, Khilevich A, De Frutos O, Gleason SD, Kato AS, Luffer-Atlas D, Desai PV, Swanson S, Burris KD, Ding C, Heinz BA, Need AB, Barth VN, Stephenson GA, Diseroad BA, Woods TA, Yu H, Bredt D, Witkin JM. Discovery of the First α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist Dependent upon Transmembrane AMPA Receptor Regulatory Protein (TARP) γ-8. J Med Chem. 2016 May 26;59(10):4753-68. doi: 10.1021/acs.jmedchem.6b00125. PubMed PMID: 27067148. |
