| (±)-5'-Chloro-5'-deoxy-ENBAadenosine A1 receptor agonist, selective and high-affinity |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.
(±)-5"-Chloro-5"-deoxy-ENBA Dilution Calculator
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| Cas No. | 103626-26-2 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | (2R,3R,4S,5S)-2-(6-((1R,2R,4R)-bicyclo[2.2.1]heptan-2-ylamino)-9H-purin-9-yl)-5-(chloromethyl)tetrahydrofuran-3,4-diol | ||
| Canonical SMILES | ClC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)N2C(N=CN=C3N[C@H]4[C@H](CC5)C[C@@H]5C4)=C3N=C2 | ||
| Formula | C17H22ClN5O3 | M.Wt | 379.84 |
| Solubility | <37.98mg l="" in="" dmso;=""><37.98mg l="" in="" ethanol=""> | Storage | Store at -20°C |
| Physical Appearance | White solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| 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. | ||
(±)-5"-Chloro-5"-deoxy-ENBA is a selective and high-affinity adenosine A1 receptor agonist with Ki values of 0.51 [1]. Adenosine A1 receptor mediated neuroand cardioprotection (an antiarrhythmic effect), reduction of lipolysis in adipose tissue and reduction of neuropathic pain [1].In mice injected with formalin at doses between 1 and 2mg/kg, (±)-5"-Chloro-5"-deoxy-ENBA inhibited the first and the second phases of the nocifensive response induced by formalin [1]. In a mouse model of neuropathic pain (the Spared Nerve Injury (SNI) of the sciatic nerve), (±)-5"-Chloro-5"-deoxy-ENBA (0.5 mg/kg) reduced thermal hyperalgesia and mechanical allodynia 7 and 3 days post-SNI without significantly changed the motor coordination and arterial blood pressure. Also, (±)-5"-Chloro-5"-deoxy-ENBA chronic treatment reduced activated and hypertrophic microglia [2]. In a Parkinson"s disease (PD) mouse model, (±)-5"-Chloro-5"-deoxy-ENBA prevented the increase in sIPSC frequency and eIPSC amplitude produced by SKF. In mice with unilateral DA denervation, (±)-5"-Chloro-5"-deoxy-ENBA reduced the development of abnormal involuntary movements induced by L-DOPA [3].References:[1]. Franchetti P, Cappellacci L, Vita P, Petrelli R, et al. N6-Cycloalkyl- and N6-bicycloalkyl-C5"(C2")-modified adenosine derivatives as high-affinity and selective agonists at the human A1 adenosine receptor with antinociceptive effects in mice. J Med Chem, 2009, 52(8): 2393-2406.[2]. Luongo L, Petrelli R, Gatta L, et al. 5"-Chloro-5"-deoxy-(±)-ENBA, a potent and selective adenosine A(1) receptor agonist, alleviates neuropathic pain in mice through functional glial and microglial changes without affecting motor or cardiovascular functions. Molecules, 2012, 17(12): 13712-13726. [3]. Mango D, Bonito-Oliva A, Ledonne A, et al. Adenosine A1 receptor stimulation reduces D1 receptor-mediated GABAergic transmission from striato-nigral terminals and attenuates l-DOPA-induced dyskinesia in dopamine-denervated mice. Exp Neurol, 2014, 261: 733-743.
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