sb258719 hydrochloride

Selective 5-HT7 receptor antagonist

SB-269970 hydrochloride (SB-269970A) , a hydrochloride salt form of SB-269970, is a 5-HT7 receptor antagonist (pKi of 8.3) and exhibits >50-fold selectivity against other receptors.

SB 258719 is a selective antagonist of 5-HT7 receptor(pKi of 7.5).

SB-224289 hydrochloride (SB-224289A) is a selective antagonist of 5-HT1B receptor, with anxiolytic effect.

SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, and orally active dopamine D3 receptor (D3R) antagonist that crosses the blood-brain barrier, with Ki values of 10.7 nM for rodent D3R and 11.2 nM for human D3R. It is 80-100 times more selective for D3 receptors than other dopamine receptors, acting on D3 receptors (pKi: 8.0), D2 receptors (pKi: 6.0), 5-HT1B receptors (pKi < 5.2), and 5-HT1D receptors (pKi: 5.9).

SB 216641 hydrochloride (SB-216641A) is a selective 5-HT1B/D receptor antagonist with anxiolytic properties that antagonizes the vasoconstrictor response mediated by sumatriptan. 10-O-Methylprotosapphosporin is an HbF inducer that can be used in the study of metabolic disorders and diabetes.

SB 203186 hydrochloride is a potent 5-HT4 receptor antagonist

SB 271046 hydrochloride (SB 271046A) is selective, orally active 5-HT6 antagonist (pKi values are 9.02-8.92, 6.35, 6.55, 6.27 at 5-HT6, 5-HT1A, 5-HT1D and D3, and 6.05, 5.95, 5.76, 5.73, 5.62, 5.55, 5.41, 5.39, 5.27 and < 4.99 at 5-HT1B, 5-HT1F, α1B, 5-HT2C, 5-HT2A, D2, 5-HT2B, 5-HT7, 5-HT4 and 5-HT1E respectively) and is > 200-fold selective over 55 other receptors, enzymes and ion channels. It increases extracellular aspartate and glutamate in the frontal cortex and exhibits anticonvulsant activity (EC50: 0.16 μM).

5-HT2B/5-HT2C receptor antagonist

SB 204070 hydrochloride is an inhibitor of beta-lactamase, it is isolated from Spondias mombin.

SB-505124 hydrochloride (SB505124 hydrochloride) is an orally available, selective and potent inhibitor of TGF-β type I receptors (ALK4, ALK5, ALK7) with IC50 values of 129 nM and 47 nM for ALK4 and ALK5, respectively. SB-505124 hydrochloride inhibits IL-6 production by synovial explants and reduces Th17 differentiation in mice by decreasing Il17a and Rorc gene expression and IL-17 protein production.SB-505124 hydrochloride is used in the study of colorectal cancer.

SB 258585 hydrochloride is a 5-HT6 receptor antagonist.

SB-435495 hydrochloride is a potent, selective, reversible, non-covalent, and orally active inhibitor of Lp-PLA2, with an IC50 of 0.06 nM [1] [3].

SB-743921 hydrochloride (SB743921 HCl) is an effective inhibitor of kinesin spindle protein, KSP, (Ki =0.1 nM).

SB 202190 hydrochloride is a selective, cell-permeable p38 MAPK inhibitor that targets p38α and p38β2 (IC50 = 50 100 nM). It exhibits anti-tumor activity and induces differentiation of human embryonic stem cells into cardiomyocytes.

SB 258741 hydrochloride is a potent antagonist of the 5-HT 7 receptor, designed specifically for studying schizophrenia [1].

SB-408124 Hydrochloride is a non-peptide OX1 receptor antagonist(Ki of 57 nM and 27 nM in both whole cell and membrane, respectively).

SB-612111 hydrochloride is a potent, novel orphan receptor for opioid receptors (ORL-1) antagonist with high affinity for hORL-1 and a Ki value of 0.33 nM. SB-612111 hydrochloride is able to act on mu-receptor (Ki: 57.6 nM), κ SB-612111 hydrochloride effectively antagonized the nociceptive effects of Nociceptin in an acute pain model.

SB 203580 hydrochloride (Adezmapimod hydrochloride) is a selective, ATP-competitive p38 MAPK inhibitor that induces mitochondrial autophagy and cytosolic autophagy and inhibits SAPK2a p38, SAPK2b p38β2, LCK, GSK3β, and PKBα. SB 203580 hydrochloride has been shown to be useful in antiretroviral therapy. 203580 hydrochloride inhibits amphoteric mechanical anomalous pain in a mouse model of antiretroviral-induced neuropathic pain.

SB-399885 hydrochloride is an antagonist of 5-HT6 receptor.

NOP receptor antagonist

SB 243213 hydrochloride is an orally active, selective, high-affinity antagonist of the 5-hydroxytryptamine (5-HT)2C receptor (pKi of 9.37 and pKb of 9.8), with an improved anxiolytic profile and potential for treating schizophrenia and motor disorders.