Ro 08-2750

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.

Product information

CAS Number: 37854-59-4

Molecular Weight: 270.24

Formula: C13H10N4O3

Synonym:

Ro-08-2750

Ro 08-2750

Ro08-2750

Ro 082750

Ro -082750

Ro082750

Chemical Name: 2,3,4,10-Tetrahydro-7,10-dimethyl-2,4-dioxobenzo[g]pteridine-8-carboxaldehyde

Smiles: CC1=CC2N=C3C(=NC(=O)NC3=O)N(C)C=2C=C1C=O

InChiKey: JDEMVNYMYPJJIM-UHFFFAOYSA-N

InChi: 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)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

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.

In Vivo:

Ro 08-2750 (13.75 mg/kg; i.p.) inhibits leukemogenesis in a myeloid leukemia model in vivo.

References:

1. 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.
2. 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.
3. 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.

Products are for research use only. Not for human use.