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Purity: ≥98%
Ro 08-2750 is a novel, potent, selective, and reversible non-peptide inhibitor of Nerve growth factor (NGF), binding to the NGF dimer with a KD of ~ 1 μM. It inhibits TRKA binding to p75NTR but not NGF. With an IC50 of 2.7 μM, Ro 08-2750 is a selective MSI RNA-binding activity inhibitor. NGF may have negative effects on IVD cells' catabolic/anabolic balance and matrix turnover activity, which could accelerate the degeneration of IVDs. The IVD degeneration process' progressive tissue breakdown may be ameliorated and the pain may be reduced by anti-NGF therapy.
| Targets |
NGF (IC50 ~1 µM); MSI RNA-binding (IC50 = 2.7 μM)
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|---|---|
| ln Vitro |
By attaching to the NGF dimer, Ro 08-2750 most likely causes a change in conformation that prevents NGF from further attaching to p75NTR[2].
Ro 08-2750 (10 nM) completely prevents NGF-induced cell death in SK-N-MC 103 cells[2]. In myeloid leukemia cells, Ro 08-2750 (5-10 μM; 8 hours) increases differentiation and apoptosis[3]. Ro 08-2750 prevents human AML lines and patient cells from surviving[3]. Ro 08-2750 modifies the MSI2 gene signature and inhibits MSI2 RNA-binding[3]. |
| ln Vivo |
In a myeloid leukemia model, Ro 08-2750 (13.75 mg/kg; i.p.) inhibits leukemogenesis[3].
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| References | |
| Additional Infomation |
7,10-dimethyl-2,4-dioxo-8-benzo[g]pteridinecarboxaldehyde is a flavin.
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| Molecular Formula |
C13H10N4O3
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|---|---|
| Molecular Weight |
270.2435
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| Exact Mass |
270.075
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| Elemental Analysis |
C, 57.78; H, 3.73; N, 20.73; O, 17.76
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| CAS # |
37854-59-4
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| Related CAS # |
37854-59-4
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| PubChem CID |
17756791
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| Appearance |
Orange to red solid powder
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| Density |
1.6±0.1 g/cm3
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| Index of Refraction |
1.754
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| LogP |
-0.81
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
20
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| Complexity |
554
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=CC1C(C)=CC2=C(N(C3=NC(=O)NC(=O)C3=N2)C)C=1
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| InChi Key |
JDEMVNYMYPJJIM-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
7,10-dimethyl-2,4-dioxobenzo[g]pteridine-8-carbaldehyde
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| Synonyms |
Ro-08-2750; Ro 082750; Ro -082750; Ro 08-2750; Ro08-2750; Ro082750
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~4 mg/mL (~14.8 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (18.50 mM) in 50% PEG300 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 5 mg/mL (18.50 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7004 mL | 18.5021 mL | 37.0041 mL | |
| 5 mM | 0.7401 mL | 3.7004 mL | 7.4008 mL | |
| 10 mM | 0.3700 mL | 1.8502 mL | 3.7004 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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