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MedKoo Cat#: 464495 | Name: Darifenacin-d4
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Darifenacin-d4 is intended for use as an internal standard for the quantification of darifenacin by GC- or LC-MS. Darifenacin is an antagonist of M3 muscarinic acetylcholine receptors. It is selective for M3 over M1, M2, M4, and M5 mAChRs (Kis = 7.08, 44.67, 45.71, and 9.33 nM, respectively). Darifenacin selectively inhibits contractions in isolated guinea pig ileum, bladder, and trachea (pA2s = 9.44, 8.66, and 8.7, respectively), tissues that endogenously express high levels of M3 mAChRs, over isolated rabbit vas deferens and isolated guinea pig atria (pA2s = 7.9 and 7.48, respectively), which endogenously express M1 and M2 mAChRs, respectively. It inhibits micturition pressure (ED50 = 0.089 mg/kg, i.v.), as well as micturition interval and volume in rats. Formulations containing darifenacin have been used in the treatment of overactive bladder.

Chemical Structure

Darifenacin-d4
Darifenacin-d4
CAS#1189701-43-6

Theoretical Analysis

MedKoo Cat#: 464495

Name: Darifenacin-d4

CAS#: 1189701-43-6

Chemical Formula: C28H26D4N2O2

Exact Mass: 430.2558

Molecular Weight: 430.58

Elemental Analysis: C, 78.11; H, 7.96; N, 6.51; O, 7.43

Price and Availability

Size Price Availability Quantity
1mg USD 450.00 2 Weeks
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Synonym
Darifenacin-d4; Darifenacin d4; (±)-Darifenacin-d4; rac Darifenacin-d4
IUPAC/Chemical Name
2-(1-(2-(2,3-dihydrobenzofuran-5-yl)ethyl-1,1,2,2-d4)pyrrolidin-3-yl)-2,2-diphenylacetamide
InChi Key
HXGBXQDTNZMWGS-MIMPEXOTSA-N
InChi Code
InChI=1S/C28H30N2O2/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)/i13D2,16D2
SMILES Code
NC(C(C1=CC=CC=C1)(C2CN(CC2)C([2H])(C([2H])(C3=CC=C4OCCC4=C3)[2H])[2H])C5=CC=CC=C5)=O
Appearance
Solid powder
Purity
>99% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 430.58 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
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Newer Medications for Lower Urinary Tract Symptoms Attributed to Benign Prostaic Hyperplasia: A Review [Internet]. Rockville (MD): Agency for Healthcare Research and Quality (US); 2016 May. Report No.: 16-EHC024-EF. PMID: 27336104. 8: McFerren SC, Gomelsky A. Treatment of Overactive Bladder in the Elderly Female: The Case for Trospium, Oxybutynin, Fesoterodine and Darifenacin. Drugs Aging. 2015 Oct;32(10):809-19. doi: 10.1007/s40266-015-0301-x. PMID: 26391900. 9: Orme S, Morris V, Gibson W, Wagg A. Managing Urinary Incontinence in Patients with Dementia: Pharmacological Treatment Options and Considerations. Drugs Aging. 2015 Jul;32(7):559-67. doi: 10.1007/s40266-015-0281-x. PMID: 26169438. 10: Oelke M, Becher K, Castro-Diaz D, Chartier-Kastler E, Kirby M, Wagg A, Wehling M. Appropriateness of oral drugs for long-term treatment of lower urinary tract symptoms in older persons: results of a systematic literature review and international consensus validation process (LUTS-FORTA 2014). Age Ageing. 2015 Sep;44(5):745-55. doi: 10.1093/ageing/afv077. Epub 2015 Jun 23. PMID: 26104505; PMCID: PMC4615806. 11: Samuelsson E, Odeberg J, Stenzelius K, Molander U, Hammarström M, Franzen K, Andersson G, Midlöv P. Effect of pharmacological treatment for urinary incontinence in the elderly and frail elderly: A systematic review. Geriatr Gerontol Int. 2015 May;15(5):521-34. doi: 10.1111/ggi.12451. Epub 2015 Feb 5. PMID: 25656412. 12: Matera C, Tata AM. Pharmacological approaches to targeting muscarinic acetylcholine receptors. Recent Pat CNS Drug Discov. 2014;9(2):85-100. doi: 10.2174/1574889809666141120131238. PMID: 25413004. 13: Russo P, Del Bufalo A, Milic M, Salinaro G, Fini M, Cesario A. Cholinergic receptors as target for cancer therapy in a systems medicine perspective. Curr Mol Med. 2014;14(9):1126-38. doi: 10.2174/1566524014666141015152601. PMID: 25324001. 14: Institute for Quality and Efficiency in Health Care. Mirabegron -- Benefit Assessment According to §35a Social Code Book V [Internet]. Cologne, Germany: Institute for Quality and Efficiency in Health Care (IQWiG); 2014 Aug 28. Extract of Dossier Assessment No. A14-19. PMID: 26677503. 15: Cetinel B, Onal B. Rationale for the use of anticholinergic agents in overactive bladder with regard to central nervous system and cardiovascular system side effects. Korean J Urol. 2013 Dec;54(12):806-15. doi: 10.4111/kju.2013.54.12.806. Epub 2013 Dec 10. PMID: 24363860; PMCID: PMC3866282. 16: Maman K, Aballea S, Nazir J, Desroziers K, Neine ME, Siddiqui E, Odeyemi I, Hakimi Z. Comparative efficacy and safety of medical treatments for the management of overactive bladder: a systematic literature review and mixed treatment comparison. Eur Urol. 2014 Apr;65(4):755-65. doi: 10.1016/j.eururo.2013.11.010. Epub 2013 Nov 18. PMID: 24275310. 17: Veenboer PW, Bosch JL. Long-term adherence to antimuscarinic therapy in everyday practice: a systematic review. J Urol. 2014 Apr;191(4):1003-8. doi: 10.1016/j.juro.2013.10.046. Epub 2013 Oct 16. PMID: 24140548. 18: National Collaborating Centre for Women's and Children's Health (UK). Urinary Incontinence in Women: The Management of Urinary Incontinence in Women. London: Royal College of Obstetricians and Gynaecologists (UK); 2013 Sep. PMID: 25340217. 19: Natalin R, Lorenzetti F, Dambros M. Management of OAB in those over age 65. Curr Urol Rep. 2013 Oct;14(5):379-85. doi: 10.1007/s11934-013-0338-5. PMID: 23922134. 20: Leone Roberti Maggiore U, Scala C, Venturini PL, Ferrero S. Imidafenacin for the treatment of overactive bladder. Expert Opin Pharmacother. 2013 Jul;14(10):1383-97. doi: 10.1517/14656566.2013.796930. Epub 2013 May 6. Erratum in: Expert Opin Pharmacother. 2014 Feb;15(2):301. PMID: 23641864.

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