SVT-40776

Product Name: SVT-40776
CAS No.: 1159101-48-0
Chemical Name: SVT-40776
Synonyms: CS-268;SVT-40776;SVT40776 D-tartrate;SVT-40776 D-tartrate;SVT 40776 D-tartrate;Tarafenacin (D-tartrate);Tarafenacin Dtartrate,Tarafenacin D tartrate;SVT-40776 D-TARTRATE;SVT40776 D-TARTRATE;SVT 40776 D-TARTRATE;N-(3-fluorophenyl)-N-[(3,4,5-trifluorophenyl)methyl]-Carbamic acid (3R)-1-azabicyclo[2.2.2]oct-3-yl ester (2S,3S)-2,3-dihydroxybutanedioate (1:1);CarbaMic acid, N-(3-fluorophenyl)-N-[(3,4,5-trifluorophenyl)Methyl]-, (3R)-1-azabicyclo[2.2.2]oct-3-yl ester, (2S,3S)-2,3-dihydroxybutanedioate (1:1)
CBNumber: CB02648138
Molecular Formula: C25H26F4N2O8
Formula Weight: 558.4761528
MOL File: 1159101-48-0.mol

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SVT-40776 Property

storage temp.: Store at -20°C
solubility: Soluble in DMSO
form: Powder
color: White to off-white

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-2113
Product name: TarafenacinD-tartrate
Purity: 99.70%
Packaging: 10mg
Price: $410
Updated: 2021/12/16

ApexBio Technology

Product number: B1133
Product name: TarafenacinD-tartrate
Packaging: 10mg
Price: $501
Updated: 2021/12/16

ChemScene

Product number: CS-2113
Product name: TarafenacinD-tartrate
Purity: 99.70%
Packaging: 50mg
Price: $1080
Updated: 2021/12/16

ApexBio Technology

Product number: B1133
Product name: TarafenacinD-tartrate
Packaging: 50mg
Price: $1319
Updated: 2021/12/16

ChemScene

Product number: CS-2113
Product name: TarafenacinD-tartrate
Purity: 99.70%
Packaging: 100mg
Price: $1836
Updated: 2021/12/16

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SVT-40776 Chemical Properties,Usage,Production

Uses

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. 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). SVT-40776 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 concentrations. SVT-40776 exhibited the highest urinary versus cardiac selectivity (199-fold) [1]. SVT-40776 has a much higher binding affinity (K(d) = 0.4 nM) to M5 mAChR than that of solifenacin (K(d) = 31 nM) with the same reeptor. The calculated binding free energy change (-2.3 ± 0.3 kcal/mol) from solifenacin to SVT-40776 is in good agreement with the experimentally derived binding free energy change (-2.58 kcal/mol), suggesting that our modeled M5 mAChR structure and its complexes with the antagonists are reliable [2]. in vivo: In the guinea pig in vivo model, SVT-40776 inhibited 25% of spontaneous bladder contractions at a very low dose (6.97 microg.kg(-1) i.v), without affecting arterial blood pressure [1].

IC 50

mAChR3

References

[1] Salcedo C, et al. In vivo and in vitro pharmacological characterization of SVT-40776, a novel M3 muscarinic receptor antagonist, for the treatment of overactive bladder. Br J Pharmacol. 2009 Mar;156(5):807-17. DOI:10.1111/j.1476-5381.2008.00082.x
[2] Huang X, et al. Microscopic binding of M5 muscarinic acetylcholine receptor with antagonists by homology modeling, molecular docking, and molecular dynamics simulation. J Phys Chem B. 2012 Jan 12;116(1):532-41. DOI:10.1021/jp210579b

SVT-40776 Preparation Products And Raw materials

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Preparation Products

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SVT-40776 Suppliers

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1159101-48-0, SVT-40776Related Search:

SVT-40776

CarbaMic acid, N-(3-fluorophenyl)-N-[(3,4,5-trifluorophenyl)Methyl]-, (3R)-1-azabicyclo[2.2.2]oct-3-yl ester, (2S,3S)-2,3-dihydroxybutanedioate (1:1)

Tarafenacin (D-tartrate)

N-(3-fluorophenyl)-N-[(3,4,5-trifluorophenyl)methyl]-Carbamic acid (3R)-1-azabicyclo[2.2.2]oct-3-yl ester (2S,3S)-2,3-dihydroxybutanedioate (1:1)

SVT 40776 D-tartrate

SVT-40776 D-tartrate

SVT40776 D-tartrate

SVT-40776 D-TARTRATE;SVT40776 D-TARTRATE;SVT 40776 D-TARTRATE

CS-268

Tarafenacin Dtartrate,Tarafenacin D tartrate

1159101-48-0

C21H20F4N2O2C4H6O6

C25H26F4N2O8