Sigma Receptor Agonist

Oxeladin citrate is an orally active and brain-penetrant cough suppressant as well as a selective sigma 1 receptor agonist (K_i = 25 nM). Oxeladin can be used for pulmonary diseases and stroke research.

S1R agonist 1 (Compound 6b) hydrochloride is a selective S1R agonist with K_is of 0.93 nM and 72 nM for S1R and S2R, respectively. S1R agonist 1 hydrochloride exhibits neuroprotection against ROS and NMDA-induced neurotoxicity.

Ditolylguanidine (Standard) is the analytical standard of Ditolylguanidine. This product is intended for research and analytical applications. Ditolylguanidine (1,3-Di-o-tolylguanidine) is an agonist of sigma receptor (σ1/σ2 receptor) with Ki values of 69 and 21 nM for σ1 and σ2 receptors, respectively. Ditolylguanidine effectively inhibits the growth of small cell lung cancer cells. Ditolylguanidine can be used for the research of lung cancer.

Siramesine (Lu 28-179) fumarate is a potent sigma-2 receptor agonist. Siramesine fumarate has a subnanomolar affinity for sigma-2 receptors (IC₅₀=0.12?nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC₅₀=17?nM). Siramesine fumarate triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity.

(Rac)-AF710B is the racemate of AF710B (HY-116586). AF710B is a highly potent and selective allosteric M1 muscarinic and σ1 receptor agonist. AF710B can be used for the research of Alzheimer’s disease.

(2S,3S)-E1R (Compound 2d) is an enantiomer of E1R. (2S,3S)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders.

PRE-084 (hydrochloride) (Standard) is the analytical standard of PRE-084 (hydrochloride). This product is intended for research and analytical applications. PRE-084 hydrochloride is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 44 nM. PRE-084 hydrochloride exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 hydrochloride also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway.

threo Ifenprodil hemitartrate is a σ receptor agonist, with K_is of 59.1 and 2 nM for σ1 and σ2 receptors, respectively. threo Ifenprodil hemitartrate is also a NR2B subunit-selective NMDA receptor antagonist (IC₅₀=0.22 μM). threo Ifenprodil hemitartrate is a hERG potassium channel inhibitor, with an IC ₅₀ of 88 nM, showing antiarrhythmic activity.

SW43 is a Sigma-2 selective ligand and agonist. SW43 is an ideal molecule for the development of cancer-targeted drug compounds. SW43 conjugated with DOX-L-NETA (⁸⁹Y) exhibits antitumor activity in a VX2 cancer liver tumor allograft rabbit model. SW 43 conjugated with SW IV-52s to form SW III-123 activates the NF-κB pathway, has potent cytotoxicity against ovarian cancer cell lines, and induces apoptosis.

(Rac)-E1R (Compound 2) is the racemate of E1R. (Rac)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) used for the research of cognition/memory disorders.

(2R,3S)-E1R (Compound 2c) is an enantiomer of E1R. (2R,3S)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders.

(2R,3R)-E1R (Compound 2b) is an enantiomer of E1R. (2R,3R)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders.

WLB-87848 is a selective, orally active, and blood-brain barrier (BBB) permeable σ1 receptor agonist with the K_i of 9 nM. WLB-87848 rescues recognition memory impairment.

Pentoxyverine (citrate) (Standard) is the analytical standard of Pentoxyverine (citrate). This product is intended for research and analytical applications. Pentoxyverine (Carbetapentane) citrate is an orally active sigma-1 receptor agonist, with Kis of 41 nM, 894 nM and 75 nM for σ1, σ2 and guinea-pig brain membrane σ1, respectively. Pentoxyverine citrate is a muscarinic antagonist. Pentoxyverine citrate is a potent antitussive, anticonvulsant, and spasmolytic agent. Pentoxyverine citrate can be used for inhibiting bronchial interceptor, weakening of cough reflex, bronchial smooth muscle relaxation and reduction of airway resistance[4].

(±)-PPCC oxalate is a sigma-1 agonist that mainly interacts with sigma-1 receptors with K_i of 1.5 nM. (±)-PPCC oxalate has effective anti-amnesia effects in rats with mild or severe cognitive impairment, and can improve the cognitive abilities of rats.

S1R agonist 2 (Compound 8b) hydrochloride is a selective S1R agonist with K_is of 1.1 nM and 88 nM for S1R and S2R, respectively. S1R agonist 2 hydrochloride exhibits neuroprotection against ROS and NMDA-induced neurotoxicity.

AF710B is an orally effective allosteric agonist for the M1 muscarinic receptor and σ1 receptor. AF710B activates the downstream phosphorylated ERK1/2 and phosphorylated CREB signaling pathways. AF710B simultaneously improves cognitive function and alleviates the core pathological features of Alzheimer's disease, including Aβ deposition, excessive Tau phosphorylation and neuroinflammation. AF710B is applicable to the research of Alzheimer's disease.

CM572 is a selective irreversible partial sigma-2 receptor agonist. CM572 has antitumor activity. CM572 induces dose-dependent cell death, with an EC₅₀ of 7.6 μM in SK-N-SH neuroblastoma cells. CM572 can be used for the research of kinds of diseases such as neuroblastoma, breast cancer.

PRE-084 is a highly selective σ1 receptor (S1R) agonist, with an IC₅₀ of 44 nM. PRE-084 exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway.

(±)-PPCC is a sigma-1 agonist that mainly interacts with sigma-1 receptors with K_i of 1.5 nM. (±)-PPCC has effective anti-amnesia effects in rats with mild or severe cognitive impairment, and can improve the cognitive abilities of rats.