. Timcodar | VX-853 | CAS#179033-51-3 | MedKoo Biosciences

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MedKoo product information:

 

Timcodar

 

Description of Timcodar: Timcodar, also known as VX-853,  is a novel multidrug resistance Inhibitor. Timcodar was under clinical trials to treat cancaners and other diseases. Timcodar potentiated the activity of ethidium bromide (EtBr), a model efflux substrate, against three clinically significant gram-positive pathogens: Staphylococcus aureus, Enterococcus faecalis, and Streptococcus pneumoniae. Similar to reserpine,  VX-853 directly blocked EtBr efflux in S. aureus. Furthermore, VX-853 was  effective in lowering the MICs of several clinically used antibiotics, including fluoroquinolones, suggesting that  VX-853 are representatives of a new class of bacterial efflux inhibitors with the potential for use in combination therapy. [source: Antimicrob Agents Chemother. 2004 Nov;48(11):4171-6.] (last updated: 1/12/2015)

 

Current developer:    Vertex (Originator).

 

MedKoo Cat#: 202926

Name: Timcodar

CAS#: 179033-51-3 (Timcodar free base).183313-30-6 (Timcodar dimesilate)

Synonym: Timcodar dimesilate, VX-853; VX853; VX 853

IUPAC/Chemical name: 

(S)-N-benzyl-3-(4-chlorophenyl)-N-(1,5-di(pyridin-4-yl)pentan-3-yl)-2-(N-methyl-2-oxo-2-(3,4,5-trimethoxyphenyl)acetamido)propanamide.

Canonical SMILES: O=C(N(CC1=CC=CC=C1)C(CCC2=CC=NC=C2)CCC3=CC=NC=C3)[C@@H](N(C)C(C(C4=CC(OC)=C(OC)C(OC)=C4)=O)=O)CC5=CC=C(Cl)C=C5

Chemical structure

Theoretical analysis

Timcodar structure

MedKoo Cat#: 202926
Name: Timcodar
CAS#: 179033-51-3

Chemical Formula: C43H45ClN4O6

Exact Mass: 748.30276

Molecular Weight: 749.29

Elemental Analysis: C, 68.93; H, 6.05; Cl, 4.73; N, 7.48; O, 12.81   

 

Availability and price:

Timcodar, purity > 98%, is available through custom synthesis. Minimum 1 gram order is requested. Current shipping out time is about 70 days after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Shipping fee:  $30.00 (USA); from $45.00 (Canada); from $70.00 (international).

10mg / not available

25mg / not available

50mg / not available

100mg / not available

200mg / not available

500mg / not available

1.0g / Ask price

2.0g / Ask price

5.0g / Ask price

Please ask price and availability of other quantity.

 

 

Technical data

Appearance:

Solid powder

Purity:

>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

View CoA: current batch, Lot# (will be available for download when it's in stock)

QC data:

View QC data: current batch, Lot#  (will be available for download when it's in stock)

Safety Data Sheet (MSDS):

View Material Safety Data Sheet (MSDS)  (will be available for download when it's in stock)

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).

Note: The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

 

Protocols from literature

In vitro protocol::

XXX

In vivo protocol:

XXX

Clinical study:

XXX

Review papers:

XXX 

 

 

Information about this agent

  

 

References

1: Grossman TH, Shoen CM, Jones SM, Jones PL, Cynamon MH, Locher CP. The Efflux Pump Inhibitor Timcodar (VX-853) Improves the Potency of Anti-Mycobacterial Agents. Antimicrob Agents Chemother. 2014 Dec 22. pii: AAC.04271-14. [Epub ahead of print] PubMed PMID: 25534740.

2: Hinds TD, Stechschulte LA, Elkhairi F, Sanchez ER. Analysis of FK506, timcodar (VX-853) and FKBP51 and FKBP52 chaperones in control of glucocorticoid receptor activity and phosphorylation. Pharmacol Res Perspect. 2014 Dec;2(6):e00076. doi: 10.1002/prp2.76. Epub 2014 Sep 1. PubMed PMID: 25505617; PubMed Central PMCID: PMC4186452.

3: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2006 Oct;28(8):533-91. PubMed PMID: 17136234.

4: Hahn K, Sirdofsky M, Brown A, Ebenezer G, Hauer P, Miller C, Polydefkis M. Collateral sprouting of human epidermal nerve fibers following intracutaneous axotomy. J Peripher Nerv Syst. 2006 Jun;11(2):142-7. PubMed PMID: 16787512.

5: Polydefkis M, Sirdofsky M, Hauer P, Petty BG, Murinson B, McArthur JC. Factors influencing nerve regeneration in a trial of timcodar dimesylate. Neurology. 2006 Jan 24;66(2):259-61. PubMed PMID: 16434669.

6: Mitchell AM, Tom M, Mortimer RH. Thyroid hormone export from cells: contribution of P-glycoprotein. J Endocrinol. 2005 Apr;185(1):93-8. PubMed PMID: 15817830.

7: Mullin S, Mani N, Grossman TH. Inhibition of antibiotic efflux in bacteria by the novel multidrug resistance inhibitors biricodar (VX-710) and timcodar (VX-853). Antimicrob Agents Chemother. 2004 Nov;48(11):4171-6. PubMed PMID: 15504837; PubMed Central PMCID: PMC525397.

 

 

 

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