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VU 0238429

  Cat. No.:  DC12159   Featured
Chemical Structure
1160247-92-6
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More than 5000 active chemicals with high quality for research!
Field of application
VU 0238429 is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5), with an EC50 of 1.16 μM.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1160247-92-6
Synonyms: VU 0238429;VU-0238429;VU0238429
SMILES: O=C1N(CC2=CC=C(OC)C=C2)C3=C(C=C(OC(F)(F)F)C=C3)C1=O
Formula: C17H12F3NO4
M.Wt: 351.28
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: VU 0238429 is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5), with an EC50 of 1.16 μM.
Target: EC50: 1.16 μM (mAChR5)[1].
In Vitro: VU 0238429 is positive allosteric modulator of mAChR5 (M5), with an EC50 of 1.16 μM, >30-fold selectivity versus M1 and M3, with no M2 or M4 potentiator activity[1].
References: [1]. Bridges TM, et al. Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
2018-0101
Cat. No. Product name Field of application
DC72833 Muscarine Muscarine ((+)-Muscarine) is a toxin that can stimulate the parasympathetic nervous system. Muscarine is an agonist of muscarinic acetylcholine receptor (mAChR).
DC72629 Eucatropine Eucatropine is a synthetic anticholinergic agent that acts as a potent inhibitor of muscarinic acetylcholine receptors (mAChRs). These receptors are part of the parasympathetic nervous system and play a key role in mediating the effects of acetylcholine, a neurotransmitter involved in various physiological processes such as smooth muscle contraction, glandular secretion, and heart rate regulation.
DC70216 ASP8302 ASP8302 (ASP 8302) is a potent, selective, positive allosteric modulator (PAM) of muscarinic M3 receptor.Threonine 230 (Thr 230) is the amino acid essential for the PAM effect of ASP8302.
DC48164 Aceclidine Aceclidine is a modulator of M3 muscarinic acetylcholine receptor. Aceclidine is a cycloplegic agent, a surfactant, a tonicity adjustor and optionally a viscosity enhancer and an antioxidant. Aceclidine has the potential for the research of disorders such as refractive errors of the eye, xerostomia, Sjogren's syndrome, glaucoma, conjunctivitis, lacrimal gland disease, and esotropia (extracted from patent US20150290125A1/US20110091459A1).
DC47237 PD 102807 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.
DC47080 Velufenacin Velufenacin is a muscarinic receptor antagonist.
DC46844 Emraclidine Emraclidine is a muscarinic M4 receptor positive allosteric modulator (WO2018002760, compound 11). Emraclidine can be used for the research of neurological diseases.
DC45324 Sofpironium bromide Sofpironium bromide (BBI 4000) is an anticholinergic agent used in the study of primary axillary hyperhidrosis (PAH). Sofpironium bromide reduces sweating by inhibiting M3 muscarinic receptors in eccrine glands at the application site. Sofpironium bromide also has a high afnity for the M1, M2, M4 and M5 subtypes.
DC44945 JHU37152 JHU37152 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.8 nM and 8.7 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.,hM4Di [1](Cell-free assay) hM3Dq [1](Cell-free assay) hM3Dq [1](Cell-free assay) hM4Di [1](Cell-free assay) 0.5 nM(EC50) 1.8 nM(Ki) 5 nM(EC50) 8.7 nM(Ki),JHU37152 is a potent DREADD agonist with high potency and efficacy in fluorescent and BRET-based assays in HEK-293 cells, whereas no responses are observed in untransfected HEK-293 cells.[1],JHU37152 exhibits high in vivo DREADD potency. JHU37152 exhibits selective [3H]clozapine displacement from DREADDs in brain tissue from WT and D1-DREADD mice.[1]
DC44944 JHU37160 JHU37160 is a potent and brain-penetrant DREADD agonist, with EC50s of 18.5 nM and 0.2 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37160 exhibits selective [3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue.
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