- Cat. No.
- A21518
mAChR-IN-1
mAChR-IN-1 is a potent muscarinic cholinergic receptor(mAChR) antagonist with IC50 of 17 nM.
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- Cat. No.
- A21519
VU 0238429
VU 0238429 is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5), with an EC50 of 1.16 μM.
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- Cat. No.
- A21769
VU0152100
Synonyms: VU152100
VU0152100 is a potent and selective allosteric potentiator of M4 mAChR with an EC50 of 380 ± 93 nM.
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- Cat. No.
- A21820
Levetimide
Levetimide is a potent and stereoselective inhibitor of [3H](+)pentazocine binding, with a Ki of 2.2 nM.
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- Cat. No.
- A21917
Biperiden
Synonyms: KL 373
Biperiden(KL 373) is an antiparkinsonian agent, which is the selective central M1 cholinoreceptors blocker.
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- Cat. No.
- A21936
Aclidinium Bromide
Synonyms: LAS 34273; LAS-W 330
Aclidinium Bromide(LAS 34273; LAS-W 330) is a long-acting, inhaled muscarinic antagonist as a maintenance treatment for chronic obstructive pulmonary disease (COPD).
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- Cat. No.
- A21939
(Rac)-VU 6008667
Synonyms: VU6008667
(Rac)-VU 6008667 is a selective negative allosteric modulator of muscarinic acetylcholine receptor subtype 5 (M5 NAM) (IC50=1.8 μM, pIC50= 5.75), has high CNS penetration.
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- Cat. No.
- A21977
Oxotremorine M iodide
Oxotremorine M iodide is a potent and non-selective muscarinic acetylcholine receptor (mAChR) agonist.
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- Cat. No.
- A22204
Perlapine
Perlapine is a potent and selective hM3Dq DREADD agonist (EC50 = 2.8 nM). This drug exhibits >10,000-fold selectivity for hM3Dq over hM3.
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- Cat. No.
- A22589
Benzetimide hydrochloride
Synonyms: R4929
Benzetimide hydrochloride is a muscarinic acetylcholine receptor antagonist.
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- Cat. No.
- A22684
Nor-benzetimide
Nor-benzetimide is a major metabolite of Benzetimide. Benzetimide is a mAChR antagonist with anticholinergic activity.
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- Cat. No.
- A24149
Penehyclidine hydrochloride
Synonyms: Penequinine hydrochloride
Penehyclidine hydrochloride (also known as Penequinine hydrochloride) is a selective anticholinergic agent that acts as an antagonist of muscarinic M1 and M3 receptors. It exerts anti-inflammatory effects by modulating immune signaling in lung tissue, notably through activation of the NF-κB pathway and inhibition of pro-inflammatory cytokine release. In preclinical studies, Penehyclidine hydrochloride has been shown to alleviate pulmonary inflammation in rat models of chronic obstructive pulmonary disease (COPD), particularly under conditions of mechanical ventilation. These properties suggest its potential utility in managing respiratory inflammatory conditions and improving outcomes in mechanically ventilated patients with COPD.
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- Cat. No.
- A34054
GS 283
GS 283 is a muscarinic acetylcholine receptor (mAChR) antagonist that exhibits calcium antagonist properties. This compound effectively modulates smooth muscle contraction by inhibiting contractions induced by carbachol and histamine in guinea pig tracheal smooth muscle, as well as high H+ levels in both guinea pig and rat tracheal smooth muscle. Additionally, GS 283 has been shown to inhibit Ca2+-induced contractions, and at elevated concentrations, it can completely abolish carbachol-induced contractions in a Ca2+-free environment. This makes GS 283 a valuable tool for research related to respiratory physiology and the pharmacological modulation of smooth muscle activity.
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- Cat. No.
- A39183
Azacyclonol hydrochloride
Synonyms: γ-pipradol hydrochloride
Azacyclonol hydrochloride is a selective ligand for the M3 muscarinic acetylcholine receptor, demonstrating significant inhibition of proliferation in androgen-refractory cancer cell lines, including DU145 and PC-3. This compound exhibits notable anticancer activity, particularly in A549 human lung cancer cells, by inhibiting NOX-derived reactive oxygen species. Additionally, Azacyclonol hydrochloride has shown antitumor effects in xenografted chorioallantoic membrane models. Beyond its anticancer applications, it is also explored for its potential in the treatment of chronic schizophrenia.
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- Cat. No.
- A45983
Isopteropodine
Isopteropodine is a positive modulator that selectively targets muscarinic acetylcholine receptors (mAChRs), exhibiting notable agonistic activity. It demonstrates an EC50 of 9.92 μM for acetylcholine and 14.5 μM for 5-hydroxytryptamine (5-HT), highlighting its potential in neuroscience research related to cognitive function. Additionally, Isopteropodine displays antibacterial efficacy against Gram-positive bacteria, with minimum inhibitory concentrations (MICs) of 150 μg/mL for Staphylococcus aureus and 250 μg/mL for Bacillus subtilis, making it suitable for studies in antimicrobial activity and cognitive impairment.
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- Cat. No.
- A57573
VU0364572 TFA
VU0364572 TFA is a selective allosteric agonist of the M1 muscarinic receptor, exhibiting an EC50 of 0.11 μM. This compound demonstrates neuroprotective properties, making it a potential candidate for mitigating memory impairments and alleviating neuropathology associated with Alzheimer's Disease. Additionally, VU0364572 TFA is capable of penetrating the central nervous system, thus enabling its application in neurological research.
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- Cat. No.
- A57576
VU0364572
VU0364572 is a selective allosteric agonist of the M1 muscarinic receptor, exhibiting an EC50 of 0.11 μM. It demonstrates neuroprotective effects, making it a valuable tool in investigating memory impairments and neuropathological changes associated with Alzheimer’s Disease. Additionally, VU0364572 is orally bioactive and capable of penetrating the central nervous system, enhancing its utility in neuropharmacological research.
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- Cat. No.
- A58273
p-F-HHSiD hydrochloride
Synonyms: p-Fluorohexahydrosiladifenidol hydrochloride
p-F-HHSiD hydrochloride is a potent and selective antagonist of the M3 muscarinic acetylcholine receptor (mAChR). This compound also demonstrates antagonistic properties towards other mAChR subtypes and the alpha1-adrenoceptor. p-F-HHSiD hydrochloride is useful for research applications involving cancer, metabolic disorders, neurological conditions, and cardiovascular diseases, including colon cancer, Alzheimer’s disease, and diabetes.
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- Cat. No.
- A58355
Batefenterol Succinate
Synonyms: GSK961081 Succinate; TD-5959 Succinate
Batefenterol Succinate is an inhaled bifunctional bronchodilator that acts as a muscarinic acetylcholine receptor (mAChR) antagonist and a beta2-adrenoceptor agonist. This dual mechanism results in effective smooth muscle relaxation, enhancing respiratory function. Batefenterol Succinate is primarily utilized in research focused on chronic obstructive pulmonary disease (COPD) and other respiratory conditions, providing insights into therapeutic strategies for airway obstruction.
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- Cat. No.
- A58500
Muscarinic toxin 3
Synonyms: MT3
Muscarinic toxin 3 (MT3) is a selective and non-competitive antagonist of muscarinic acetylcholine receptors (mAChRs) and adrenergic receptors. It exhibits high potency with pIC50 values of 6.71, 8.79, 8.86, 7.57, 8.13, and 8.49 against M1, M4, α1A, α1B, α1D, α2A, α2B, and α2C receptors, respectively, highlighting its prominent adrenoceptor activity. This compound is valuable in studying receptor signaling pathways and has potential applications in pharmacological research focused on nervous system disorders and cardiovascular diseases.
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- Cat. No.
- A58583
β2AR/M-receptor agonist-1
β2AR/M-receptor agonist-1 is a dual-function compound acting as a muscarinic receptor antagonist and β2 adrenoceptor agonist. It exhibits a potent agonistic effect on the β2 adrenoceptor, with an EC50 value of 9.2 nM, and also demonstrates antagonistic activity against the muscarinic receptor, characterized by a Ki value of 30.2 nM. This compound is valuable for research applications involving modulation of adrenergic and muscarinic signaling pathways.
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- Cat. No.
- A58625
PF-4348235
Synonyms: β2AR/M-receptor agonist-2
PF-4348235 is a potent M3 muscarinic receptor antagonist. It demonstrates strong inhibitory activity against the human cloned M3 receptor with a Ki value of 0.73 nM, while also acting as a β2 adrenoceptor agonist with an EC50 of 3.7 nM. This compound is primarily utilized in research related to chronic obstructive pulmonary disease (COPD) due to its significant bronchodilator properties. Its dual action makes it a valuable tool in the study of respiratory disorders.
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- Cat. No.
- A58677
p-F-HHSiD
Synonyms: p-Fluorohexahydrosiladifenidol
p-F-HHSiD (p-Fluorohexahydrosiladifenidol) functions as a selective antagonist of the M3 muscarinic acetylcholine receptor (mAChR). This compound exhibits antagonistic activity against various muscarinic receptor subtypes as well as the alpha-1 adrenergic receptor. p-F-HHSiD is valuable for research in cancer, metabolic disorders, neurological pathologies, and cardiovascular diseases, including colon cancer, Alzheimer's disease, and diabetes.
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- Cat. No.
- A59853
Clozapine N-oxide dihydrochloride
Clozapine N-oxide dihydrochloride is a selective agonist for designer receptors exclusively activated by designer drugs (DREADDs), specifically targeting hM3Dq and hM4Di. This compound plays a crucial role in neuronal circuit manipulation for experimental purposes. It is notable for its inability to cross the blood-brain barrier, making it useful for in vivo studies to modulate neuronal activity without central nervous system effects. Clozapine N-oxide dihydrochloride is integral in research applications related to neuroscience, enabling the dissection of gene function and behavior in animal models.
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- Cat. No.
- A59871
Sabcomeline hydrochloride
Synonyms: SB-202026 hydrochloride; Memric hydrochloride
Sabcomeline hydrochloride is a muscarinic receptor agonist with the ability to penetrate the blood-brain barrier. It exhibits strong affinity for human muscarinic receptor subtypes hM1 to hM5 (pKi=6.72-7.23) and functions as a near-full agonist at the hM3 receptor, leading to extracellular acidification. This compound also influences dopamine D2 receptor binding kinetics via neural network modulation, while exhibiting minimal effects on cardiovascular parameters. Sabcomeline hydrochloride is valuable in research related to Alzheimer's disease and other neurodegenerative disorders, especially for investigating its effects on spatial memory and taste aversion in rodent models.
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