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385367-47-5 (Tarafenacin)

1

Identification

Tarafenacin Tarafenacin
Name Tarafenacin
Formula C21H20F4N2O2
MW 408.39
CAS No. 385367-47-5
EINECS
Smiles O=C(O[[email protected]]1CN2CCC1CC2)N(C3=CC=CC(F)=C3)CC4=CC(F)=C(F)C(F)=C4
Synonyms SVT-40776;SVT40776;SVT 40776; (R)-quinuclidin-3-yl (3-fluorophenyl)(3,4,5-trifluorobenzyl)carbamate
InChI InChI=1S/C21H20F4N2O2/c22-15-2-1-3-16(10-15)27(11-13-8-17(23)20(25)18(24)9-13)21(28)29-19-12-26-6-4-14(19)5-7-26/h1-3,8-10,14,19H,4-7,11-12H2/t19-/m0/s1
2

Introduction

Tarafenacin(SVT-40776) is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over M2 receptor. IC50 value: 0.19 nM (Ki) [1] Target: M3 muscarinic receptor in vitro: SVT-40776 is highly selective for M(3) over M(2) receptors (Ki = 0.19 nmol.L(-1) for M(3) receptor affinity).

Background Information

SVT-40776 is a novel M3 muscarinic receptor antagonist, for the treatment of overactive bladder. ......by AdooQ BioScience, LLC
Tarafenacin is a highly selective M3 muscarinic receptor antagonist. It was the most potent in inhibiting carbachol-induced bladder contractions of the anti-cholinergic agents tested, without affecting atrial contractions over the same range of concentra ......by BOC Sciences
Tarafenacin, also known as SVT-40776, is a novel M3 muscarinic receptor antagonist under development for the treatment of overactive bladder. SVT-40776 shows highly selective for M(3) over M(2) receptors (Ki = 0.19 nmol.L(-1) for M(3) receptor affinity). SVT-40776 is a potent inhibitor of M(3) receptor-related detrusor contractile activity. The absence of effects on isolated atria preparations represents an interesting characteristic and suggests that SVT-40776 may lack unwanted cardiac effects; a feature especially relevant in a compound intended to treat mainly elderly patients. ......by MedKoo Biosciences, Inc.
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance: EBNumber:EB000022940

Storage condition

Solubility

DMSO by MedChemexpress Co., Ltd.
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Mechanism and Indication

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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
Tarafenacin Kwang Dong Pharmaceutical Co Ltd Overactive bladder 2011/9/30 2013/4/9 Phase 2 Clinical
Tarafenacin Laboratorios SALVAT SA Overactive bladder 2006/9/30 2007/9/1 Phase 2 Clinical
Tarafenacin - Phase 2
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Safety Data of Tarafenacin

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
AdooQ BioScience, LLC USA
Apexbio Technology LLC USA
Ark Pharm, Inc. USA
BOC Sciences
Biochempartner Co., Ltd China
CHEMSCENE, LLC 10mg/USD410();50mg/USD1080() USA
KareBay Biochem 50mg/USD950() USA
MedChemexpress Co., Ltd. 10mg/USD410();50mg/USD1080() USA
MedKoo Biosciences, Inc. USA
Shanghai Haoyuan Chemexpress Co., Ltd. 10mg/USD410();50mg/USD1080() China
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Related Products

Other Forms of 385367-47-5

Name CAS No Formula MW
Tarafenacin (D-tartrate) 1159101-48-0 C25H26F4N2O8 558.48

Recommended Compounds in mAChR

Name CAS No Formula MW
Pilocarpine (Hydrochloride) 54-71-7 C11H17ClN2O2 244.72
Imidafenacin 170105-16-5 C20H21N3O 319.4
Flavoxate (hydrochloride) 3717-88-2 C24H26ClNO4 427.92
Homatropine (Bromide) 51-56-9 C16H22BrNO3 356.25
Benztropine (mesylate) 132-17-2 C22H29NO4S 403.54
Otilonium (bromide) 26095-59-0 C29H43BrN2O4 563.57
Arecoline (hydrobromide) 300-08-3 C8H14BrNO2 236.11
Trospium (chloride) 10405-02-4 C25H30ClNO3 427.96
Tiotropium (bromide hydrate) 139404-48-1 C19H24BrNO5S2 490.43
Revefenacin 864750-70-9 C35H43N5O4 597.747
Oxybutynin (chloride) 1508-65-2 C22H32ClNO3 393.95
Gallamine Triethiodide 65-29-2 C30H60I3N3O3 891.53
Bethanechol (chloride) 590-63-6 C7H17ClN2O2 196.68
Atropine (sulfate monohydrate) 5908-99-6 C34H50N2O11S 694.83
Methscopolamine (bromide) 155-41-9 C18H24BrNO4 398.29
Irsogladine (maleate) 84504-69-8 C13H11Cl2N5O4 372.16
Irsogladine 57381-26-7 C9H7Cl2N5 256.09
Tropicamide 1508-75-4 C17H20N2O2 284.35
Oxybutynin 5633-20-5 C22H31NO3 357.49
Ipratropium (bromide) 22254-24-6 C20H30BrNO3 412.36

Recommended Compounds in Same Indication

Name CAS No Formula MW
Mirabegron 223673-61-8 C21H24N4O2S 396.51
Solifenacin (Succinate) 242478-38-2 C27H32N2O6 480.55
Fesoterodine (fumarate) 286930-03-8 C30H41NO7 527.65
Tolterodine (Tartrate) 124937-52-6 C26H37NO7 475.57
NKP608 177707-12-9 C31H24ClF6N3O2 619.98
Darifenacin 133099-04-4 C28H30N2O2 426.55
Darifenacin (hydrobromide) 133099-07-7 C28H29BrN2O2 505.45
Tarafenacin (D-tartrate) 1159101-48-0 C25H26F4N2O8 558.48
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Route of Synthesis

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References

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More Information

Tarafenacin

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