TarafenacinM3 muscarinic receptor antagonist CAS# 385367-47-5 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 385367-47-5 | SDF | Download SDF |
| PubChem ID | 25147683 | Appearance | Powder |
| Formula | C21H20F4N2O2 | M.Wt | 408.39 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | SVT-40776 | ||
| Solubility | Soluble in DMSO | ||
| Chemical Name | [(3R)-1-azabicyclo[2.2.2]octan-3-yl] N-(3-fluorophenyl)-N-[(3,4,5-trifluorophenyl)methyl]carbamate | ||
| SMILES | C1CN2CCC1C(C2)OC(=O)N(CC3=CC(=C(C(=C3)F)F)F)C4=CC(=CC=C4)F | ||
| Standard InChIKey | UXZDMXYRRQJIBJ-IBGZPJMESA-N | ||
| Standard 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 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | 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]. References: | |||||
Tarafenacin Dilution Calculator
Tarafenacin Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.4486 mL | 12.2432 mL | 24.4864 mL | 48.9728 mL | 61.216 mL |
| 5 mM | 0.4897 mL | 2.4486 mL | 4.8973 mL | 9.7946 mL | 12.2432 mL |
| 10 mM | 0.2449 mL | 1.2243 mL | 2.4486 mL | 4.8973 mL | 6.1216 mL |
| 50 mM | 0.049 mL | 0.2449 mL | 0.4897 mL | 0.9795 mL | 1.2243 mL |
| 100 mM | 0.0245 mL | 0.1224 mL | 0.2449 mL | 0.4897 mL | 0.6122 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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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].
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.
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The efficacy and tolerability of tarafenacin, a new muscarinic acetylcholine receptor M3 antagonist in patients with overactive bladder; randomised, double-blind, placebo-controlled phase 2 study.[Pubmed:25363415]
Int J Clin Pract. 2015 Feb;69(2):242-50.
OBJECTIVES: To evaluate the dose-response relationship of Tarafenacin, an antimuscarinic agent in development phase, for efficacy and safety, at daily doses of 0.2 and 0.4 mg for the treatment of overactive bladder (OAB) PATIENTS AND METHODS: This multicentre, placebo-controlled, randomised, double-blind, phase 2b study was conducted. Patients were randomised to Tarafenacin 0.2 mg, Tarafenacin 0.4 mg or placebo daily for 12 weeks. Adult patients with OAB for at least 6 months, with an average of >/= 8 micturitions per day and >/= 3 incontinence episodes or a total of >/= 6 urgency episodes per 3 days were enrolled. The primary objective was to compare the mean changes in the number of micturitions per 24 h of the two doses of Tarafenacin compared with placebo from baseline to 12 weeks after treatment. RESULTS: A total of 334 patients were screened, of whom 235 patients were randomised. The mean decrease in the number of micturitions per 24 h from baseline to 12 weeks was statistically higher in the Tarafenacin 0.4 mg group (-2.43 +/- 2.21 times per day, p = 0.033) and non-statistically significant in the Tarafenacin 0.2 mg group (-1.92 +/- 2.45 times per day, p = 0.393) when compared with the placebo group (-1.77 +/- 2.95 times per day). There were no statistically significant differences in the mean change of urgency episodes per 24 h among three groups. The most common adverse event was dry mouth. There were no significant differences in blurred vision and constipation compared with placebo. CONCLUSIONS: Tarafenacin 0.4 mg decreased the number of micturitions in patients with OAB after 12 weeks compared with placebo, and the dose-response relationship of Tarafenacin 0.2 and 0.4 mg was confirmed. Both dose levels of Tarafenacin were well tolerated.
