MedKoo Cat#: 319859 | Name: Tarafenacin

Description:

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

Tarafenacin, also known as SVT-40776, is a novel M3 muscarinic receptor antagonist under development for the treatment of overactive bladder. SVT-40776 shows highly selective for M(3) over M(2) receptors (Ki = 0.19 nmol.L(-1) for M(3) receptor affinity). SVT-40776 is a potent inhibitor of M(3) receptor-related detrusor contractile activity. The absence of effects on isolated atria preparations represents an interesting characteristic and suggests that SVT-40776 may lack unwanted cardiac effects; a feature especially relevant in a compound intended to treat mainly elderly patients.

Chemical Structure

Tarafenacin
Tarafenacin
CAS#385367-47-5

Theoretical Analysis

MedKoo Cat#: 319859

Name: Tarafenacin

CAS#: 385367-47-5

Chemical Formula: C21H20F4N2O2

Exact Mass: 408.1461

Molecular Weight: 408.40

Elemental Analysis: C, 61.76; H, 4.94; F, 18.61; N, 6.86; O, 7.84

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
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Synonym
SVT-40776, SVT 40776, SVT40776, Tarafenacin
IUPAC/Chemical Name
(3R)-1-azabicyclo[2.2.2]octan-3-yl (3-fluorophenyl)[(3,4,5-trifluorophenyl)methyl]carbamate
InChi Key
UXZDMXYRRQJIBJ-IBGZPJMESA-N
InChi Code
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
SMILES Code
O=C(O[C@H]1CN2CCC1CC2)N(C3=CC=CC(F)=C3)CC4=CC(F)=C(F)C(F)=C4
Appearance
Solid powder
Purity
>98% (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
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
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 408.40 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
1: Song M, Kim JH, Lee KS, Lee JZ, Oh SJ, Seo JT, Choi JB, Kim SW, Rhee SJ, Choo MS. 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. Int J Clin Pract. 2015 Feb;69(2):242-50. doi: 10.1111/ijcp.12540. Epub 2014 Nov 1. PubMed PMID: 25363415. 2: Zacche MM, Giarenis I, Cardozo L. Phase II drugs that target cholinergic receptors for the treatment of overactive bladder. Expert Opin Investig Drugs. 2014 Oct;23(10):1365-74. doi: 10.1517/13543784.2014.925877. Epub 2014 Jun 5. Review. PubMed PMID: 24899225.