Tarafenacin

Product Name: Tarafenacin
CAS No.: 385367-47-5
Chemical Name: Tarafenacin
Synonyms: CS-929;SVT407776;Tarafenacin;Tarafenacin, >=98%;Tarafenacin(SVT-40776);SVT-40776 (Tarafenacin);SVT-40776; SVT40776; SVT 40776;[(3R)-1-azabicyclo[2.2.2]octan-3-yl] N-(3-fluorophenyl)-N-[(3,4,5-trifluorophenyl)methyl]carbamate;N-(3-Fluorophenyl)-N-[(3,4,5-trifluorophenyl)methyl]carbamic acid (3R)-1-azabicyclo[2.2.2]oct-3-yl ester;Carbamic acid, N-(3-fluorophenyl)-N-[(3,4,5-trifluorophenyl)methyl]-, (3R)-1-azabicyclo[2.2.2]oct-3-yl ester
CBNumber: CB22628444
Molecular Formula: C21H20F4N2O2
Formula Weight: 408.3893128
MOL File: 385367-47-5.mol

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Tarafenacin Property

Boiling point:: 483.4±45.0 °C(Predicted)
Density: 1.38
storage temp.: Store at -20°C
solubility: Soluble in DMSO
form: Powder
pka: 8.80±0.33(Predicted)

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ApexBio Technology

Product number: B1132
Product name: Tarafenacin
Packaging: 10mg
Price: $501
Updated: 2021/12/16

American Custom Chemicals Corporation

Product number: API0013711
Product name: TARAFENACIN
Purity: 95.00%
Packaging: 10MG
Price: $618.45
Updated: 2021/12/16

Biorbyt Ltd

Product number: orb180991
Product name: Tarafenacin(SVT-40776)
Purity: >98%
Packaging: 100mg
Price: $1208.7
Updated: 2021/12/16

American Custom Chemicals Corporation

Product number: API0013711
Product name: TARAFENACIN
Purity: 95.00%
Packaging: 100MG
Price: $2310
Updated: 2021/12/16

Biorbyt Ltd

Product number: orb180991
Product name: Tarafenacin(SVT-40776)
Purity: >98%
Packaging: 250mg
Price: $2395.3
Updated: 2021/12/16

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Tarafenacin Chemical Properties,Usage,Production

Uses

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). 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].

Biological Activity

tarafenacin is a selective antagonist of m3 muscarinic receptor with ki value of 0.19nm [1].tarafenacin is a novel quinuclidine derivative and is developed as an antimuscarinic drug for treatment of overactive bladder. it shows a 203-fold selectivity with m3 receptor over m2 receptor. tarafenacin reduces the maximum carbachol response at concentrations of 10nm and 100nm in mouse isolated bladder. in mouse atrial preparations, tarafenacin slightly attenuates the effects on heart rate caused by carbachol. tarafenacin shows a 199-fold urinary affinity against cardiac affinity. it is a highly potent antagonist in the bladder and lacks any relevant effect in atria at the same range of concentrations. in the guinea pig model, tarafenacin significantly changes the bladder contraction amplitude. it inhibits 25% of spontaneous bladder contractions at dose of 17.1nmol/kg [1].

IC 50

mAChR3

References

[1] salcedo c, davalillo s, cabellos j, et al. in vivo and in vitro pharmacological characterization of svt-40776, a novel m3 muscarinic receptor antagonist, for the treatment of overactive bladder. british journal of pharmacology, 2009, 156(5): 807-817.

Tarafenacin Preparation Products And Raw materials

Raw materials

Preparation Products

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Tarafenacin Suppliers

China 35 United Kingdom 1 United States 9 Global 45

Shanghai Boyle Chemical Co., Ltd.

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Bsisun HK Imoprt And Export Company Limited

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MedChemexpress LLC

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Guangzhou Isun Pharmaceutical Co., Ltd

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AdooQ BioScience, LLC

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CEG Chemical Science&Technology Co., Ltd.

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GIHI CHEMICALS CO.,LTD

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Credit Asia Chemical Co., Ltd.

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LETOPHARM LIMITED

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BOC Sciences

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385367-47-5, TarafenacinRelated Search:

SOLIFENACIN

Tarafenacin

SVT-40776 (Tarafenacin)

N-(3-Fluorophenyl)-N-[(3,4,5-trifluorophenyl)methyl]carbamic acid (3R)-1-azabicyclo[2.2.2]oct-3-yl ester

Tarafenacin, >=98%

SVT407776

[(3R)-1-azabicyclo[2.2.2]octan-3-yl] N-(3-fluorophenyl)-N-[(3,4,5-trifluorophenyl)methyl]carbamate

SVT-40776; SVT40776; SVT 40776

Tarafenacin(SVT-40776)

CS-929

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

385367-47-5

C21H20F4N2O2