Search Result
Results for "
M 2 Antagonist
" in MedChemExpress (MCE) Product Catalog:
10
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-I0230
-
|
YM905 hydrochloride
|
mAChR
|
Neurological Disease
Cancer
|
|
Solifenacin hydrochloride (YM905 hydrochloride) is a muscarinic receptor antagonist, with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
|
-
-
- HY-A0002
-
|
YM905
|
mAChR
|
Neurological Disease
|
|
Solifenacin Succinate (YM905) is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
|
-
-
- HY-P1376A
-
|
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
|
G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis .
|
-
-
- HY-A0034
-
|
YM905 free base
|
mAChR
|
Neurological Disease
Cancer
|
|
Solifenacin (YM905 free base) is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
|
-
-
- HY-101586
-
-
-
- HY-U00104
-
|
|
mAChR
|
Endocrinology
|
|
YM-46303 is an mAChR antagonist which exhibits the highest affinities for M1 and M3 receptors, and selectivity for M3 over M2 receptor.
|
-
-
- HY-14825
-
|
SVT-40776
|
mAChR
|
Neurological Disease
|
|
Tarafenacin(SVT-40776) is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over M2 receptor.
|
-
-
- HY-129709
-
|
|
mAChR
|
Cardiovascular Disease
|
|
DAC 5945 is a potent muscarinic antagonist in the airways than in the heart, with pKi values of 8.3 and 7.52 for M1 and M2, respectively .
|
-
-
- HY-122510
-
|
Atropine oxidation
|
Parasite
|
Neurological Disease
|
|
Atropine Oxide (Atropine oxidation), a derivative of Atropine, acts as a competitive antagonist to the muscarinic acetylcholine receptors M1, M2, M3, M4, and M5, and is utilized in the treatment of specific nerve agent and pesticide poisonings.
|
-
-
- HY-135329
-
|
|
mAChR
|
Neurological Disease
|
|
Solifenacin D5 hydrochloride is a deuterium labeled Solifenacin hydrochloride. Solifenacin hydrochloride is a muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively .
|
-
-
- HY-122510A
-
|
Atropine oxidation hydrochloride
|
mAChR
|
|
|
Atropine Oxide (Atropine oxidation) hydrochloride, a derivative of Atropine, acts as a competitive antagonist to the muscarinic acetylcholine receptors M1, M2, M3, M4, and M5, and is utilized in the treatment of specific nerve agent and pesticide poisonings .
|
-
-
- HY-14825A
-
|
SVT-40776 D-tartrate
|
mAChR
|
Neurological Disease
|
|
Tarafenacin D-tartrate (SVT-40776 D-tartrate) is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over M2 receptor.
|
-
-
- HY-130431
-
|
|
Parasite
|
Infection
|
|
Vinclozolin M2 is an active metabolite of vinclozolin. It is formed from vinclozolin by successive esterase activity and decarboxylation of vinclozolin in C. elegans and by decarboxylation in human liver microsomes. Vinclozolin M2 is an antagonist of the mineralocorticoid receptor (IC50=1,400 nM) and androgen receptor (IC50=0.17 nM) in reporter assays using MCF-7 cells.
|
-
-
- HY-I0230S
-
|
|
Isotope-Labeled Compounds
mAChR
|
Neurological Disease
|
|
Solifenacin-d7 (hydrochloride) is the deuterium labeled Solifenacin hydrochloride. Solifenacin hydrochloride (YM905 hydrochloride) is a muscarinic receptor antagonist, with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
|
-
-
- HY-116294A
-
|
|
mAChR
|
Cardiovascular Disease
|
|
Methoctramine tetrahydrochloride is a potent and cardioselectivity antagonist of M2 muscarinic receptor. Methoctramine tetrahydrochloride can inhibit Muscarine-induced bradycardia in vivo .
|
-
-
- HY-B0461
-
|
|
mAChR
|
Neurological Disease
Cancer
|
|
Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors .
|
-
-
- HY-120792
-
|
|
mAChR
|
Others
|
|
DAU 5884 is a muscarinic receptor antagonist with activity that discriminates between different muscarinic receptor subtypes. DAU 5884 discriminates between M4 and M2 receptor sites and is a highly potent M1-selective antagonist with specific activity at different muscarinic receptors characterized by radioligand binding studies and functional assays.
|
-
-
- HY-A0002S
-
|
YM905-d5
|
Isotope-Labeled Compounds
mAChR
|
Neurological Disease
|
|
Solifenacin-d5 (succinate) is deuterium labeled Solifenacin (Succinate). Solifenacin Succinate (YM905) is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
|
-
-
- HY-120329
-
|
|
mAChR
|
Others
|
|
Lu 26-046 is the agonist for muscarinic M1 receptor and M2 receptor and a weak antagonist for M3 receptor, with Ki of 0.51, 26 and 5 nM, respectively. Lu 26-046 exhibits specific stimulus property, that can be recognized by rats .
|
-
-
- HY-101381
-
|
AF-DX 116
|
mAChR
|
Neurological Disease
Metabolic Disease
|
|
Otenzepad (AF-DX 116) is a selective and competitive M2 muscarinic acetylcholine receptor antagonist, with IC50 values of 640 nM and 386 nM for rabbit peripheral lung and rat heart, respectively .
|
-
-
- HY-107653
-
|
|
mAChR
|
Neurological Disease
|
|
J 104129 fumarate is a selective and orally active muscarinic M3 antagonist with Ki values of 4.2 nM and 490 nM for M3 and M2, respectively. J 104129 fumarate antagonized ACh-induced bronchoconstriction. J 104129 fumarate has the potential for the research of obstructive airway disease .
|
-
-
- HY-108171A
-
|
|
mAChR
|
Inflammation/Immunology
|
|
Hexocyclium methylsulfate is a potent mAChR antagonist with pKi values of 8.9, 7.7, 8.4, 8.8 for M1, M2, M3, and M4 subtype, respectively. Hexocyclium methylsulfate has the potential for the research of duodenal ulcer and irritable bowel syndrome .
|
-
-
- HY-119953
-
|
|
mAChR
|
Neurological Disease
|
|
BIBN-99 is a selective, BBB-penetrable and competitive muscarinic M2 receptor antagonist. BIBN-99 improves cognitive performancein rats with traumatic brain injury .
|
-
-
- HY-107646
-
|
|
mAChR
|
Neurological Disease
|
|
PD 102807 is a M4 muscarinic receptor antagonist with an IC50 of 90.7 nM. PD 102807 inhibits M1, M2, M3, M5 muscarinic receptor with IC50s of 6558.7, 3440.7, 950.0, and 7411.7 nM, respectively . Antidyskinetic effect.
|
-
-
- HY-A0034R
-
|
|
mAChR
|
Neurological Disease
Cancer
|
|
Solifenacin (Standard) is the analytical standard of Solifenacin. This product is intended for research and analytical applications. Solifenacin (YM905 free base) is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
|
-
-
- HY-101586A
-
|
Lu 25-109 maleate
|
mAChR
|
Neurological Disease
|
|
Alvameline (Lu 25-109) maleate is a partial agonist of M1 and an antagonist of M2/M3. Alvameline maleate competitively antagonizes contractions induced by ammonium chloride (HY-Y1269) and electrical field stimulation in human detrusor muscle, indicating its potential application in regulating bladder function. Additionally, alvameline maleate can improve cognitive function following traumatic brain injury in rats .
|
-
-
- HY-101679
-
|
|
mAChR
|
Neurological Disease
|
|
YM-58790 is a potent antagonist of mAChR. YM-58790 binds M1, M2, M3 with Ki values of 28 nM, 260 nM, and 15 nM. YM-58790 exhibits potent inhibitory activity on bladder pressuer in reflexly-evoked rhythmic contraction in rats .
|
-
-
- HY-A0002R
-
|
YM905 (Standard)
|
mAChR
|
Neurological Disease
Cancer
|
|
Solifenacin (Succinate) (Standard) is the analytical standard of Solifenacin (Succinate). This product is intended for research and analytical applications. Solifenacin Succinate (YM905) is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
|
-
-
- HY-U00302
-
|
|
mAChR
|
Inflammation/Immunology
|
|
CHF5407 is a selective, long-acting and competitive muscarinic M3 receptor antagonist. CHF5407 shows subnanomolar affinities for human muscarinic M1 (hM1), M2 (hM2) and M3 (hM3) receptors. CHF5407 shows a prolonged antibronchospastic activity .
|
-
-
- HY-A0030
-
|
|
mAChR
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB) .
|
-
-
- HY-70053
-
|
|
mAChR
|
Neurological Disease
Metabolic Disease
|
|
Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine is used for the overactive bladder (OAB) .
|
-
-
- HY-120418
-
|
|
mAChR
|
Others
|
|
L-687306 is a high affinity muscarinic M1 receptor partial agonist with activity as a partial agonist of M1 receptors in rat ganglia and as a high affinity competitive antagonist at guinea pig cardiac M2 and ileal M3 muscarinic receptors, useful for studying the receptor reserve of muscarinic receptors.
|
-
-
- HY-B0461S
-
|
|
mAChR
|
Neurological Disease
|
|
Trospium-d8 (chloride) is the deuterium labeled Trospium chloride. Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors[1][2].
|
-
-
- HY-106874B
-
|
rel-RS-15385-197
|
Adrenergic Receptor
Prostaglandin Receptor
|
Neurological Disease
|
|
rel-Delequamine (rel-RS-15385-197) is an orally active, brain-penetrant, potent and selective M2-adrenoceptor antagonist and α2-adrenoceptor antagonist. rel-Delequamine has a pKi of 9.45 for α2-adrenoceptors in the rat cortex. rel-Delequamine augments K +-evoked release of noradrenaline with an EC50 of 1 nM .
|
-
-
- HY-16489A
-
|
|
mAChR
Calcium Channel
|
Neurological Disease
|
|
Terodiline hydrochloride is an M1-selective muscarinic receptor (mAChR) antagonist with Kbs of 15, 160, 280, and 198 nM in rabbit vas deferens (M1), atria (M2), bladder (M3) and ileal muscle (M3), respectively. Terodiline hydrochloride also is a Ca 2+ blocker. Terodiline hydrochloride acts as a treatment for urinary frequency and urge incontinence .
|
-
-
- HY-107647
-
|
|
mAChR
Histamine Receptor
|
Inflammation/Immunology
|
|
(S)-(+)-Dimethindene maleate, an enantiomer, is a potent M2-selective muscarinic receptor antagonist (pA2 = 7.86/7.74; pKi = 7.78). (S)-(+)-Dimethindene maleate shows lower affinities for the muscarinic M1 (pA2 = 6.83/6.36; pKi = 7.08), the M3 (pA2 = 6.92/6.96; pKi = 6.70) and the M4 receptors (pKi = 7.00), respectively. (S)-(+)-Dimethindene maleate also is a histamine H1 receptor antagonist (pA2 = 7.48) .
|
-
-
- HY-P1376
-
|
|
mAChR
Adrenergic Receptor
|
Endocrinology
|
|
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
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-
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- HY-B0461R
-
|
|
mAChR
|
Neurological Disease
|
|
Trospium (chloride) (Standard) is the analytical standard of Trospium (chloride). This product is intended for research and analytical applications. Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors .
|
-
-
- HY-70053A
-
|
|
mAChR
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Fesoterodine L-mandelate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine L-mandelate is used for the overactive bladder (OAB) .
|
-
-
- HY-107656
-
|
|
mAChR
|
Neurological Disease
|
|
PTAC oxalate is a selective muscarinic receptor ligand. PTAC oxalate is an partial agonist of M2 and M4 but antagonist of M1, M3, and M5 (Ki values of 0.2-2.8 nM for hM1-5 in CHO cells). PTAC oxalate alleviates the mechanical allodynia on the neuropathic pain and has antidepression effects .
|
-
-
- HY-101679A
-
|
|
mAChR
|
Neurological Disease
|
|
YM-58790 free base is a potent antagonist of mAChR. YM-58790 free base binds M1, M2, M3 with Ki values of 28 nM, 260 nM, and 15 nM. YM-58790 free base exhibits potent inhibitory activity on bladder pressuer in reflexly-evoked rhythmic contraction in rats .
|
-
-
- HY-76570
-
|
(Rac)-Desfesoterodine; (Rac)-PNU-200577
|
mAChR
|
Neurological Disease
|
|
(Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research .
|
-
-
- HY-76570A
-
|
(Rac)-Desfesoterodine hydrochloride; (Rac)-PNU-200577 hydrochloride
|
mAChR
|
Neurological Disease
|
|
(Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine) hydrochloride, an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine hydrochloride can be used for overactive bladder research .
|
-
-
- HY-B0241
-
|
Sch 1000
|
mAChR
|
Neurological Disease
Inflammation/Immunology
|
|
Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with IC50s of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide relaxes smooth muscle, can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma .
|
-
-
- HY-135329S
-
|
|
Isotope-Labeled Compounds
mAChR
|
Neurological Disease
|
|
(1R,3S-)Solifenacin-d5 (hydrochloride) is the deuterium labeled Solifenacin D5 hydrochloride. Solifenacin D5 hydrochloride is a deuterium labeled Solifenacin hydrochloride. Solifenacin hydrochloride is a muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively[1].
|
-
-
- HY-B1332
-
|
Sch 1000 bromide hydrate
|
mAChR
|
Neurological Disease
Inflammation/Immunology
|
|
Ipratropium bromide (Sch 1000) hydrate is a muscarinic receptor antagonist, with IC50s of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide hydrate relaxes smooth muscle, can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma .
|
-
-
- HY-100979
-
|
HDMPPA
|
mAChR
|
Others
|
|
W-84 (dibromide) is a potent allosteric modulator of M2-cholinoceptors, which retards [ 3H]N-methylscopolamine dissociation. W-84 dibromide can stabilize cholinergic antagonist-receptor complexes. W-84 (dibromide) is a non-competitive muscarinic acetylcholine receptors antagonist with allosteric effects. W-84 (dibromide) protects over additively against an organophosphate-intoxication when applied in combination with atropine .
|
-
-
- HY-107652
-
|
|
mAChR
|
Neurological Disease
|
|
AF-DX 384 is a selective antagonist of M2 and M4 muscarinic acetylcholine receptors (Kis=6.03 and 10 nM, respectively) . AF-DX 384 reverses deficits in novel object recognition and passive avoidance in aged rats, as well as in young rats with impairments induced by scopolamine .
|
-
-
- HY-A0030S
-
|
|
mAChR
|
Metabolic Disease
|
|
Fesoterodine-d7 (fumarate) is the deuterium labeled Fesoterodine fumarate[1]. Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB)[2][3].
|
-
-
- HY-A0030R
-
|
|
mAChR
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Fesoterodine (fumarate) (Standard) is the analytical standard of Fesoterodine (fumarate). This product is intended for research and analytical applications. Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB) .
|
-
- HY-124223
-
|
|
mAChR
|
Neurological Disease
|
|
AF-DX 384 (methanesulfonate) is a selective antagonist of M2 and M4 muscarinic acetylcholine receptors (Kis=6.03 and 10 nM, respectively) . AF-DX 384 (methanesulfonate) reverses deficits in novel object recognition and passive avoidance in aged rats, as well as in young rats with impairments induced by scopolamine .
|
-
- HY-B0241S
-
|
Sch 1000-d3
|
mAChR
|
Neurological Disease
Inflammation/Immunology
|
|
Ipratropium-d3 (bromide) is the deuterium labeled Ipratropium bromide. Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with binding IC50 values of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma[1][2][3].
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-
- HY-B0241S1
-
|
Sch 1000-d7 (bromide)
|
mAChR
|
Neurological Disease
Inflammation/Immunology
|
|
Ipratropium-d7 (bromide)eis the deuterium labeled Ipratropium bromide. Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with binding IC50 values of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma[1][2][3].
|
-
- HY-148527
-
|
AZD8999
|
Adrenergic Receptor
mAChR
|
Others
|
|
LAS190792 (AZD8999) is a potent muscarinic antagonist and β2-adrenoceptor agonist with pIC50 8.9, 8.8, 8.8, 9.2, 8.2, 7.5, 9.1, 5.6 for M1, M2, M3, M4, M5, β1, β2, β3, respectively. LAS190792 can be used as a bronchodilator .
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- HY-136587
-
|
|
Histamine Receptor
mGluR
|
Inflammation/Immunology
|
|
Oxomemazine is a phenothiazine-based histamine H1-receptor blocker with pronounced antimuscarinic properties. Oxomemazine is a selective antagonist for muscarinic M1 receptor, displays about 20-fold difference in the affinity for high (Ki = 84 nM, M1 receptor) and low (Ki = 1.65 μM, M2 receptor) affinity sites . Oxomemazine an antihistamine and anticholinergic agent used for the study of cough treatment .
|
-
- HY-157956
-
|
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mAChR
|
Neurological Disease
|
|
LASSBio-873 is an orally active muscarinic cholinergic receptor (mAChR) agonist that crosses the blood-brain barrier. LASSBio-873 has potent analgesic effects on acute and inflammatory pain. The analgesic effect of LASSBio-873 can be inhibited by intrathecal injection of the M2 receptor antagonist methoctramine .
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- HY-B1339
-
|
Dicycloverine hydrochloride
|
mAChR
|
Neurological Disease
|
|
Dicyclomine hydrochloride is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine hydrochloride shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .
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-
- HY-B0241R
-
|
|
mAChR
|
Neurological Disease
Inflammation/Immunology
|
|
Ipratropium (bromide) (Standard) is the analytical standard of Ipratropium (bromide). This product is intended for research and analytical applications. Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with IC50s of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide relaxes smooth muscle, can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma .
|
-
- HY-B1332R
-
|
|
mAChR
|
Neurological Disease
Inflammation/Immunology
|
|
Ipratropium (bromide hydrate) (Standard) is the analytical standard of Ipratropium (bromide hydrate). This product is intended for research and analytical applications. Ipratropium bromide (Sch 1000) hydrate is a muscarinic receptor antagonist, with IC50s of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide hydrate relaxes smooth muscle, can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma .
|
-
- HY-B1339A
-
|
Dicycloverine
|
mAChR
|
Neurological Disease
|
|
Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .
|
-
- HY-122203
-
|
|
mAChR
Cholinesterase (ChE)
|
Neurological Disease
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PCS1055 dihydrochloride is a potent, selective and competitive muscarinic M4 receptor antagonist with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [ 3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 dihydrochloride exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 dihydrochloride is also a potent AChE inhibitor with IC50 s of 22 nM and 120 nM for electric eel and human AChE, respectively .
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- HY-76570S
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(Rac)-Desfesoterodine-d14; (Rac)-PNU-200577-d14
|
mAChR
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Neurological Disease
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(Rac)-5-Hydroxymethyl Tolterodine-d14 is the deuterium labeled (Rac)-5-Hydroxymethyl Tolterodine. (Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research[1].
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- HY-76570S1
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Isotope-Labeled Compounds
mAChR
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Neurological Disease
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5-Hydroxymethyl Tolterodine-d14 (formate) is deuterium labeled (Rac)-5-Hydroxymethyl Tolterodine. (Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research[1].
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- HY-136587R
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Histamine Receptor
mGluR
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Inflammation/Immunology
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Oxomemazine (Standard) is the analytical standard of Oxomemazine. This product is intended for research and analytical applications. Oxomemazine is a phenothiazine-based histamine H1-receptor blocker with pronounced antimuscarinic properties. Oxomemazine is a selective antagonist for muscarinic M1 receptor, displays about 20-fold difference in the affinity for high (Ki = 84 nM, M1 receptor) and low (Ki = 1.65 μM, M2 receptor) affinity sites . Oxomemazine an antihistamine and anticholinergic agent used for the study of cough treatment .
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- HY-B1339R
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mAChR
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Neurological Disease
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Dicyclomine (hydrochloride) (Standard) is the analytical standard of Dicyclomine (hydrochloride). This product is intended for research and analytical applications. Dicyclomine hydrochloride is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine hydrochloride shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .
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- HY-B1339AS
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Dicycloverine-d4
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mAChR
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Neurological Disease
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Dicyclomine-d4 is the deuterium labeled Dicyclomine[1]. Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively[2]. Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo[3].
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- HY-B1101
-
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Pimetixene
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5-HT Receptor
Histamine Receptor
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Neurological Disease
Endocrinology
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Pimethixene is antihistamine and antiserotonergic compound, acts as an antimigraine agent.
Pimethixene is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively .
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- HY-B1101A
-
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Pimetixene maleate
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5-HT Receptor
Histamine Receptor
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Neurological Disease
Endocrinology
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Pimethixene maleate is antihistamine and antiserotonergic compound, acts as an antimigraine agent.
Pimethixene maleate is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively .
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- HY-101343
-
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5-HT Receptor
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Neurological Disease
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RS 39604 is a potent, selective, and orally active 5-HT4 receptor antagonist with a pKi of 9.1 in guinea pig striatal membranes. RS 39604 displays a low affinity (pKi<6.5) for 5-HT1A, 5-HT2C, 5-HT3, α1c, D1, D2, M1, M2, AT1, B1 and opioid mu receptors and moderate affinity for δ1, (pKi=6.8) and δ2 (pKi=7.8) sites .
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- HY-B1101AR
-
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5-HT Receptor
Histamine Receptor
|
Neurological Disease
Endocrinology
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|
Pimethixene maleate (Standard) is the analytical standard of Pimethixene maleate. This product is intended for research and analytical applications. Pimethixene maleate is antihistamine and antiserotonergic compound, acts as an antimigraine agent.
Pimethixene maleate is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively .
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- HY-16375
-
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D-63153
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GnRH Receptor
Apoptosis
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Cancer
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Ozarelix (D-63153) is a GnRH antagonist. Ozarelix induces cell apoptosis and arrests cell in G2/M phase. Ozarelix can be used in the research of prostate cancer .
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- HY-107644
-
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mAChR
|
Cardiovascular Disease
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AQ-RA 741 is a potent and selective M 2 antagonist. AQ-RA 741 inhibits the vagally or agonist-induced bradycardia in rats, cats and guinea-pigs. AQ-RA 741 is used in bradycardiac disorders research .
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- HY-151801
-
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mAChR
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Others
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DIBA-Cy5 is a fluorescent DIBA antagonist made up be DIBA-alkyne binding Cyanine5 fluorophores (Cy5) and polyethylene glycol (PEG) biomolecules. DIBA-Cy5 can serve as a fluorescent ligand, suitable for probe attachment through click chemistry. DIBA-Cy5 exerts a high binding affinity to type-2 mAChR (M2R) with the Kd value of 1.80 nM, can directly stain M2R receptors in the sinoatrial node of a mouse heart .
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- HY-117087
-
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Phosphatase
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Cancer
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K103 is an inhibitor discovered from the screen that is an analog of the serotonin antagonist benzazocine. K103 exhibited inhibition of SHIP homologues, labelling it a pan-SHIP1/2 inhibitor, but the molecule had no effect on another 5' inositol phosphatase, OCRL. In line with the "two PIPs hypothesis", the molecule exhibited significant anti-tumour effects against a variety of cell lines, particularly breast cancer cells. Additional studies with K103 revealed that inhibition of SHIP1/2 in multiple myeloma cells resulted in G2/M cell cycle arrest followed by extensive apoptosis via activation of the caspase cascade. K103 fits the commonly used small molecule agent property profile, but while this work was being conducted, it was discovered that K103 caused psychoactive effects in mice, which limited the utility of the molecule in vivo. Therefore, certain synthetic studies were conducted on this tryptamine to identify the features that needed to be present in the molecule to maintain pan-SHIP1/2 inhibition in order to design an inhibitor with favourable pharmacodynamic properties and an improved side effect profile.
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| Cat. No. |
Product Name |
Type |
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- HY-151801
-
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Fluorescent Dyes/Probes
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DIBA-Cy5 is a fluorescent DIBA antagonist made up be DIBA-alkyne binding Cyanine5 fluorophores (Cy5) and polyethylene glycol (PEG) biomolecules. DIBA-Cy5 can serve as a fluorescent ligand, suitable for probe attachment through click chemistry. DIBA-Cy5 exerts a high binding affinity to type-2 mAChR (M2R) with the Kd value of 1.80 nM, can directly stain M2R receptors in the sinoatrial node of a mouse heart .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P1376A
-
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mAChR
Adrenergic Receptor
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Endocrinology
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G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis .
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- HY-P1376
-
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mAChR
Adrenergic Receptor
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Endocrinology
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G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of Gi or Go and inhibits Gs activation by β-adrenoceptors.
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-
- HY-16375
-
|
D-63153
|
GnRH Receptor
Apoptosis
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Cancer
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|
Ozarelix (D-63153) is a GnRH antagonist. Ozarelix induces cell apoptosis and arrests cell in G2/M phase. Ozarelix can be used in the research of prostate cancer .
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| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0241S
-
|
|
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Ipratropium-d3 (bromide) is the deuterium labeled Ipratropium bromide. Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with binding IC50 values of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma[1][2][3].
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-
- HY-I0230S
-
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Solifenacin-d7 (hydrochloride) is the deuterium labeled Solifenacin hydrochloride. Solifenacin hydrochloride (YM905 hydrochloride) is a muscarinic receptor antagonist, with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
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-
-
- HY-A0002S
-
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Solifenacin-d5 (succinate) is deuterium labeled Solifenacin (Succinate). Solifenacin Succinate (YM905) is a novel muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
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-
-
- HY-B0461S
-
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Trospium-d8 (chloride) is the deuterium labeled Trospium chloride. Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with high affinity, but not nicotinic, cholinergic receptors[1][2].
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-
-
- HY-135329S
-
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(1R,3S-)Solifenacin-d5 (hydrochloride) is the deuterium labeled Solifenacin D5 hydrochloride. Solifenacin D5 hydrochloride is a deuterium labeled Solifenacin hydrochloride. Solifenacin hydrochloride is a muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively[1].
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-
-
- HY-A0030S
-
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Fesoterodine-d7 (fumarate) is the deuterium labeled Fesoterodine fumarate[1]. Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB)[2][3].
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-
-
- HY-B0241S1
-
|
|
|
Ipratropium-d7 (bromide)eis the deuterium labeled Ipratropium bromide. Ipratropium bromide (Sch 1000) is a muscarinic receptor antagonist, with binding IC50 values of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma[1][2][3].
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-
-
- HY-76570S
-
|
|
|
(Rac)-5-Hydroxymethyl Tolterodine-d14 is the deuterium labeled (Rac)-5-Hydroxymethyl Tolterodine. (Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research[1].
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-
-
- HY-76570S1
-
|
|
|
5-Hydroxymethyl Tolterodine-d14 (formate) is deuterium labeled (Rac)-5-Hydroxymethyl Tolterodine. (Rac)-5-Hydroxymethyl Tolterodine ((Rac)-Desfesoterodine), an active metabolite of Tolterodine, is a mAChR antagonist (Ki values of 2.3 nM, 2 nM, 2.5 nM, 2.8 nM, and 2.9 nM for M1, M2, M3, M4, and M5 receptors, respectively). (Rac)-5-Hydroxymethyl Tolterodine can be used for overactive bladder research[1].
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-
-
- HY-B1339AS
-
|
|
|
Dicyclomine-d4 is the deuterium labeled Dicyclomine[1]. Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively[2]. Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo[3].
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-120329
-
|
|
|
Alkynes
|
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Lu 26-046 is the agonist for muscarinic M1 receptor and M2 receptor and a weak antagonist for M3 receptor, with Ki of 0.51, 26 and 5 nM, respectively. Lu 26-046 exhibits specific stimulus property, that can be recognized by rats .
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