GSK172981
GSK172981 is a non-peptide tachykinin NK3 receptor antagonist. GSK172981 demonstrated high affinity for recombinant human (pK(i) value 7.7) and native guinea pig (pK(i) value 7.8) tachykinin NK(3) receptors. In vitro functional evaluations revealed GSK172981 to be a competitive antagonist (pA(2)=7.2) at cloned human tachykinin NK(3) receptor. GSK172981 also exhibited a competitive profile in antagonizing neurokinin B-stimulated neuronal activity recorded from the guinea pig medial habenula slices (apparent pK(B)=8.1). GSK172981 is potentially useful in the treatment of schizophrenia.
| Supplier | Ace Therapeutics |
|---|---|
| Product # | SMD1546 |
| CAS # | 1133705-99-3 |
| Pricing | Customizable size, Inquiry |
| Synonym | GSK172981; GSK-172981; GSK 172981. |
| Product Category | Lab-use Small Molecule Drugs |
| Chemical Formula | C26H22FN3O |
| Exact Mass | 411.1747 |
| Molecular Weight | 411.4804 |
| Elemental Analysis | C, 75.89; H, 5.39; F, 4.62; N, 10.21; O, 3.89 |
| IUPAC/Chemical Name | (S)-3-amino-N-(cyclopropyl(phenyl)methyl)-2-(3-fluorophenyl)quinoline-4-carboxamide |
| InChi Key | ZKGNLARKIMWKFE-XMMPIXPASA-N |
| InChi Code | InChI=1S/C26H22FN3O/c27-19-10-6-9-18(15-19)25-23(28)22(20-11-4-5-12-21(20)29-25)26(31)30-24(17-13-14-17)16-7-2-1-3-8-16/h1-12,15,17,24H,13-14,28H2,(H,30,31)/t24-/m1/s1 |
| SMILES Code | O=C(C1=C(N)C(C2=CC=CC(F)=C2)=NC3=CC=CC=C13)N[C@@H](C4CC4)C5=CC=CC=C5 |
| 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℃ for short term (days to weeks), or -20℃ for long term (months). |
| HS Tariff Code | 2934.99.9001 |