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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
220 Results for "
Sigma
" in MedChemExpress (MCE) Product Catalog:
Products (220)
220 Results for "Sigma" in MCE Product Catalog:
13
13 Publications Verification
Cat. No.: HY-18100A
CAS No.: 75136-54-8
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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 .
12
12 Cited Publications
Cat. No.: HY-16996A
CAS No.: 138356-21-5
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BD-1047 dihydrobromide is a selective functional antagonist of sigma receptors. BD-1047 dihydrobromide attenuates Apomorphine (HY-12723)-induced climbing and Phencyclidine-induced head twitches .
7
7 Cited Publications
Synonyms: SA4503 dihydrochloride; AGY94806 dihydrochloride
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Cutamesine (SA4503) dihydrochloride is a potent and selective sigma 1 receptor agonist with an IC50 of 17.4 nM in guinea pig brain membranes. Cutamesine dihydrochloride shows >100-fold less affinity for the sigma 2 receptor (IC50 of 1784 nM). Cutamesine dihydrochloride has antidepressant effects .
7
7 Cited Publications
Synonyms: SA4503; AGY 94806
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Cutamesine (SA4503) is a potent and selective sigma 1 receptor agonist with an IC50 of 17.4 nM in guinea pig brain membranes. Cutamesine shows >100-fold less affinity for the sigma 2 receptor (IC50 of 1784 nM). Cutamesine has antidepressant effects .
6
6 Cited Publications
Synonyms: Lu 28-179 hydrochloride
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Siramesine (Lu 28-179) hydrochloride is a potent sigma-2 receptor agonist. Siramesine hydrochloride 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 hydrochloride triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity .
6
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Siramesine (Lu 28-179) is a potent sigma-2 receptor agonist. Siramesine 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 triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity .
5
5 Cited Publications
Synonyms: DHEA sulfate; Prasterone sulfate
Category:
Human Gut Microbiota Metabolites Microorganisms Disease markers Endocrine diseases Nervous System Disorder Endogenous metabolite
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5
5 Cited Publications
Synonyms: DHEA sulfate sodium; Prasterone sulfate sodium
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3
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Blarcamesine hydrochloride (Anavex 2-73) is a Sigma-1 Receptor agonist with an IC50 of 860 nM.
3
3 Cited Publications
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Blarcamesine is an orally bioavailable Sigma-1 receptor agonist and muscarinic receptor modulator, with anticonvulsant, anti-amnesic, neuroprotective and antidepressant properties. Blarcamesine ameliorates neurologic impairments in a mouse model of Rett syndrome .
3
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S1RA (E-52862) is a highly selective σ1 receptor (σ1R) antagonist with Kis of 17 nM and 23.5 nM for human σ1R and guinea pig σ1R, respectively. S1RA has Moderate antagonistic activity for human 5-HT2B receptor (Ki= 328 nM). S1RA has antinociceptive effects in neuropathic pain models. S1RA prevents mechanical and cold hypersensitivity in Oxaliplatin (HY-17371)-treated mice .
3
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S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a Ki value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (Ki >1000 nM). S1RA hydrochloride is a human 5-HT2B receptor antagonist with an IC50 value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization .
3
3 Cited Publications
Cat. No.: HY-B2215
CAS No.: 36304-84-4
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Dimemorfan phosphate is a sigma 1 receptor agonist, used as a potent antitussive.
3
3 Cited Publications
Cat. No.: HY-18101A
CAS No.: 206996-13-6
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BD-1063 dihydrochloride is a selective σ-1 receptor antagonist with inhibitory activity against TRPC5 and TRPM3. BD-1063 dihydrochloride exerts anti-hyperalgesic and anti-allodynic effects by inhibiting sustained calcium influx mediated by TRPC5 and TRPM3, and reverses the effects of Carrageenan (HY-125474). BD-1063 dihydrochloride also significantly reduces excessive ethanol self-administration behavior. BD-1063 dihydrochloride is widely used in studies on the mechanisms underlying neuropathic pain, inflammatory hyperalgesia, and alcohol abuse and dependence .
3
3 Cited Publications
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L-745870 is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors .
3
3 Cited Publications
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L-745870 hydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 hydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors .
2
2 Cited Publications
Synonyms: 1,3-Di-o-tolylguanidine; DTG
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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 .
2
Category:
Alkaloids Neurological Disease Quinoline Alkaloids Plants Papaver somniferum Linn. Disease Research Fields Inflammation/Immunology Papaveraceae
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2
2 Cited Publications
Synonyms: (S,R)-Noscapine hydrochloride
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Noscapine ((S,R)-Noscapine) hydrochloride is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine hydrochloride exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine hydrochloride disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine hydrochloride possesses anticancer, neuroprotective, anti-inflammatory activities, and can crosse the blood-brain barrier .
1
1 Cited Publications
Synonyms: CT1812; Sigma-2 receptor antagonist 1
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Zervimesine (CT1812) is an orally active and brain penetrant sigma-2 receptor antagonist with a Ki of 8.5 nM. Zervimesine can be used for the research of Alzheimer’s disease .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
