| Bioactivity | SB 218795 is a potent and selective non-peptide NK3 receptor antagonist, with a Ki 13 nM for hNK3. SB 218795 shows about 90-fold and 7000-fold selectivity for hNK3 over hNK2 and hNK1, respectively. SB 218795 can inhibit NK3 receptor-mediated pupillary constriction of the rabbit[1][2]. |
| Invitro | SB 218795 (3-30 nM) antagonizes the contractile responses induced by the NK3 receptor agonist senktide in a surmountable and concentration-dependent manner[2].SB 218795 (0.3-3 μM) does not affect the contractile responses of the NK3 receptor agonist [MePhe7]-NKB in the rabbit iris sphincter muscle[2]. |
| In Vivo | SB 218795 (0.25-1 mg/kg; i.v.) inhibits Senktide-induced miosis in rabbits by the maximum inhibition of 78%[2]. |
| Name | SB 218795 |
| CAS | 174635-53-1 |
| Formula | C25H20N2O3 |
| Molar Mass | 396.44 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Giardina GA, et, al. Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 1. Identification of the 4-quinolinecarboxamide framework. J Med Chem. 1997 Jun 6;40(12):1794-807. [2]. Medhurst AD, et, al. In vitro and in vivo characterization of NK3 receptors in the rabbit eye by use of selective non-peptide NK3 receptor antagonists. Br J Pharmacol. 1997 Oct;122(3):469-76. [3]. Valero MS, et, al. Contractile effect of tachykinins on rabbit small intestine. Acta Pharmacol Sin. 2011 Apr;32(4):487-94. |
SB 218795
CAS: 174635-53-1 F: C25H20N2O3 W: 396.44
SB 218795 is a potent and selective non-peptide NK3 receptor antagonist, with a Ki 13 nM for hNK3. SB 218795 shows about
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