MRS5698
| Code | Size | Price |
|---|
| TAR-T28106-5mg | 5mg | £1,171.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
| TAR-T28106-50mg | 50mg | £2,303.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
| TAR-T28106-100mg | 100mg | £3,042.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃
Documents
Further Information
Bioactivity:
MRS5698 is a high affinity and selective agonist of A3 adenosine receptor (Ki ~ 3 nM) protects against chronic neuropathic pain. MRS5698 displays >1000-fold selectivity over A1 and A2A adenosine receptors
CAS:
1377273-00-1
Formula:
C28H23ClF2N6O3
Molecular Weight:
564.98
Purity:
0.98
SMILES:
[H][C@]12C[C@]1([C@@H](O)[C@@H](O)[C@@H]2n1cnc2c(NCc3cccc(Cl)c3)nc(nc12)C#Cc1ccc(F)c(F)c1)C(=O)NC
References
1. Carlin JL, Tosh DK, Xiao C, Pi?ol RA, Chen Z, Salvemini D, Gavrilova O, Jacobson KA, Reitman ML. Peripheral Adenosine A3 Receptor Activation Causes Regulated Hypothermia in Mice That Is Dependent on Central Histamine H1 Receptors. J Pharmacol Exp Ther. 2016 Feb;356(2):474-82. doi: 10.1124/jpet.115.229872. Epub 2015 Nov 25. PubMed PMID: 26606937; PubMed Central PMCID: PMC4746492.
2. Tosh DK, Padia J, Salvemini D, Jacobson KA. Efficient, large-scale synthesis and preclinical studies of MRS5698, a highly selective A3 adenosine receptor agonist that protects against chronic neuropathic pain. Purinergic Signal. 2015 Sep;11(3):371-87. doi: 10.1007/s11302-015-9459-2. Epub 2015 Jun 27. PubMed PMID: 26111639; PubMed Central PMCID: PMC4529848.
3. Ford A, Castonguay A, Cottet M, Little JW, Chen Z, Symons-Liguori AM, Doyle T, Egan TM, Vanderah TW, De Konnick Y, Tosh DK, Jacobson KA, Salvemini D. Engagement of the GABA to KCC2 signaling pathway contributes to the analgesic effects of A3AR agonists in neuropathic pain. J Neurosci. 2015 Apr 15;35(15):6057-67. doi: 10.1523/JNEUROSCI.4495-14.2015. Erratum in: J Neurosci. 2015 Jun 10;35(23):8971. PubMed PMID: 25878279; PubMed Central PMCID: PMC4397603.
4. Tosh DK, Finley A, Paoletta S, Moss SM, Gao ZG, Gizewski ET, Auchampach JA, Salvemini D, Jacobson KA. In vivo phenotypic screening for treating chronic neuropathic pain: modification of C2-arylethynyl group of conformationally constrained A3 adenosine receptor agonists. J Med Chem. 2014 Dec 11;57(23):9901-14. doi: 10.1021/jm501021n. Epub 2014 Nov 25. PubMed PMID: 25422861; PubMed Central PMCID: PMC4266358.