Ro 08-2750 is a potent and selective Nerve growth factor (NGF) inhibitor that binds the NGF dimer (KD ~ 1 μM). NGF has potential effects on matrix turnover activity and influences the catabolic/anabolic balance of IVD cells in an adverse way that may potentiate IVD degeneration. Anti-NGF treatment might be beneficial to ameliorate progressive tissue breakdown in IVD degeneration and may lead to pain relief.
Chemical Formula: C13H10N4O3
Exact Mass: 270.07529
Molecular Weight: 270.25
Elemental Analysis: C, 57.78; H, 3.73; N, 20.73; O, 17.76
Chemical Name: 2,3,4,10-Tetrahydro-7,10-dimethyl-2,4-dioxobenzo[g]pteridine-8-carboxaldehyde
InChi Code: InChI=1S/C13H10N4O3/c1-6-3-8-9(4-7(6)5-18)17(2)11-10(14-8)12(19)16-13(20)15-11/h3-5H,1-2H3,(H,16,19,20)
Appearance: Orange to red solid powder
Purity: >95% (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
Ro 08-2750 binds to the NGF dimer thereby probably inducing a change in its conformation such that NGF cannot bind to p75NTR anymore.
Ro 08-2750 (10 nM) completely rescues cells from undergoing NGF-induced SK-N-MC 103 cells death.
Ro 08-2750 (5-10 μM; 8 hours) increases differentiation and apoptosis in myeloid leukemia cells.
Ro 08-2750 inhibits survival of human AML lines and patient cells.
Ro 08-2750 inhibits MSI2 RNA-binding and alters MSI2 gene signature.
Ro 08-2750 (13.75 mg/kg; i.p.) inhibits leukemogenesis in a myeloid leukemia model in vivo.
Kao TH, Peng YJ, Salter DM, Lee HS. Nerve growth factor increases MMP9 activity in annulus fibrosus cells by upregulating lipocalin 2 expression. Eur Spine J. 2015 Sep;24(9):1959-68. doi: 10.1007/s00586-014-3675-2. Epub 2014 Nov 21. PubMed PMID: 25412834.
Kao TH, Peng YJ, Tsou HK, Salter DM, Lee HS. Nerve growth factor promotes expression of novel genes in intervertebral disc cells that regulate tissue degradation: Laboratory investigation. J Neurosurg Spine. 2014 Oct;21(4):653-61. doi: 10.3171/2014.6.SPINE13756. Epub 2014 Jul 25. PubMed PMID: 25062286.
Eibl JK, Strasser BC, Ross GM. Identification of novel pyrazoloquinazolinecarboxilate analogues to inhibit nerve growth factor in vitro. Eur J Pharmacol. 2013 May 15;708(1-3):30-7. doi: 10.1016/j.ejphar.2013.03.029. Epub 2013 Mar 22. PubMed PMID: 23528360.
Niederhauser O, Mangold M, Schubenel R, Kusznir EA, Schmidt D, Hertel C. NGF ligand alters NGF signaling via p75(NTR) and trkA. J Neurosci Res. 2000 Aug 1;61(3):263-72. PubMed PMID: 10900073.
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