Darifenacin HBr

CAS# 133099-07-7

Darifenacin HBr

Catalog No. BCC4567----Order now to get a substantial discount!

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Darifenacin HBr: 5mg $35 In Stock
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Chemical structure

Darifenacin HBr

3D structure

Chemical Properties of Darifenacin HBr

Cas No. 133099-07-7 SDF Download SDF
PubChem ID 444030 Appearance Powder
Formula C28H31BrN2O2 M.Wt 507.48
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 33.33 mg/mL (65.68 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
Chemical Name 2-[(3S)-1-[2-(2,3-dihydro-1-benzofuran-5-yl)ethyl]pyrrolidin-3-yl]-2,2-diphenylacetamide;hydrobromide
SMILES C1CN(CC1C(C2=CC=CC=C2)(C3=CC=CC=C3)C(=O)N)CCC4=CC5=C(C=C4)OCC5.Br
Standard InChIKey UQAVIASOPREUIT-VQIWEWKSSA-N
Standard InChI InChI=1S/C28H30N2O2.BrH/c29-27(31)28(23-7-3-1-4-8-23,24-9-5-2-6-10-24)25-14-17-30(20-25)16-13-21-11-12-26-22(19-21)15-18-32-26;/h1-12,19,25H,13-18,20H2,(H2,29,31);1H/t25-;/m1./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.
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.
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.

Biological Activity of Darifenacin HBr

DescriptionDarifenacin HBr(UK88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9. IC50 value: 8.9 (pKi) [1] Target: M3 receptor in vitro: Darifenacin exerts non-parallel rightward displacement of the agonist curve and also significant depression of the maximum response (+)-cis-Dioxolane produced concentration-dependent contraction of the isolated bladder of rat [1]. Darifenacin produces a concentration dependent increase in R123 (P-gp probe) accumulation in MDCK cells. Darifenacin stimulates ATPase activity in P-gp membrane in a clear concentration dependent response manner with an estimated ED50 value of 1.6?μM. Darifenacin (100 nM) shows a significantly greater permeability for darifenacin in the basolateral to apical direction resulting in an efflux ratio in BBMEC monolayers of approximately 2.6 [2]. in vivo: Darifenacin produces dose-dependent inhibition of amplitude of volume-induced bladder contractions(VIBCAMP), producing 35% inhibition at dose of 283.3 nmol/kg and maximal inhibition of approximately 50–55% [1]. Darifenacin (0.1 mg/kg i.v.) reduces bladder afferent activity in both Aδ and C fibers in female Sprague-Dawley rats, the decrease in afferent spikes in C fibers may be more pronounced than that in Aδ fibers [3].

References:
[1]. Hegde SS, et al. Functional role of M2 and M3 muscarinic receptors in the urinary bladder of rats in vitro and in vivo. Br J Pharmacol, 1997, 120(8), 1409-1418. [2]. Miller DW, et al. Evaluation of drug efflux transporter liabilities of darifenacin in cell culture models of the blood-brain and blood-ocular barriers. Neurourol Urodyn, 2011, 30(8), 1633-1638. [3]. Iijima K, et al. Effects of the M3 receptor selective muscarinic antagonist darifenacin on bladder afferent activity of the rat pelvic nerve. Eur Urol, 2007, 52(3), 842-847.

Darifenacin HBr Dilution Calculator

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Darifenacin HBr Molarity Calculator

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Preparing Stock Solutions of Darifenacin HBr

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.9705 mL 9.8526 mL 19.7052 mL 39.4104 mL 49.263 mL
5 mM 0.3941 mL 1.9705 mL 3.941 mL 7.8821 mL 9.8526 mL
10 mM 0.1971 mL 0.9853 mL 1.9705 mL 3.941 mL 4.9263 mL
50 mM 0.0394 mL 0.1971 mL 0.3941 mL 0.7882 mL 0.9853 mL
100 mM 0.0197 mL 0.0985 mL 0.1971 mL 0.3941 mL 0.4926 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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Background on Darifenacin HBr

Darifenacin HBr(UK88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9.

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Description

Darifenacin hydrobromide (UK-88525 hydrobromide) is a selective M3 muscarinic receptor antagonist with pKi of 8.9.

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