| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| Other Sizes |
| Targets |
RO7185876 targets gamma-secretase, a key enzyme involved in the cleavage of amyloid precursor protein (APP). Modulation of gamma-secretase activity may help reduce the production of amyloid-beta peptides, which are implicated in Alzheimer's disease pathogenesis.
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|---|---|
| ln Vitro |
RO7185876 is a potent and selective gamma-secretase modulator. It has demonstrated activity in modulating gamma-secretase-mediated APP processing in vitro, potentially shifting the cleavage pattern away from the production of neurotoxic Aβ42 peptides.
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| ln Vivo |
RO7185876 has shown potential for in vivo efficacy in Alzheimer's disease research. As a gamma-secretase modulator, it may reduce the production of amyloid-beta peptides in the brain, offering a therapeutic approach for Alzheimer's disease.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for RO7185876 typically involve cell-free systems using purified gamma-secretase complex or membrane preparations containing gamma-secretase. The compound is incubated with the enzyme and a suitable substrate (such as a fluorescently labeled APP-derived peptide), and gamma-secretase activity is measured by detecting cleavage products. IC₅₀ or EC₅₀ values are determined from dose-response curves.
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| Cell Assay |
For in vitro cellular experiments, RO7185876 is dissolved in DMSO and diluted in cell culture medium. Cells expressing APP or gamma-secretase components are treated with the compound at varying concentrations. Amyloid-beta peptide production (Aβ40, Aβ42) is measured by ELISA or mass spectrometry. The compound's ability to modulate gamma-secretase cleavage specificity is assessed by analyzing the ratio of different Aβ peptide species.
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| Animal Protocol |
For in vivo animal experiments, RO7185876 is formulated in suitable vehicles for administration to mouse or rat models of Alzheimer's disease. The compound may be administered orally, intraperitoneally, or subcutaneously. Pharmacodynamic endpoints include measurement of amyloid-beta peptide levels in brain and cerebrospinal fluid, assessment of amyloid plaque burden, and evaluation of cognitive function using behavioral tests.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of RO7185876 include its ability to cross the blood-brain barrier to reach its target in the central nervous system. The compound has a molecular weight of 483.53 g/mol and a molecular formula of C₂₅H₂₈F₃N₇. Standard PK studies would assess parameters such as half-life, oral bioavailability, and brain penetration.
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| Toxicity/Toxicokinetics |
Toxicological data for RO7185876 is derived from preclinical studies. As a research compound for Alzheimer's disease, its safety profile would be evaluated in standard toxicology studies. The compound is intended for research use only and has not received regulatory approval.
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| References | |
| Additional Infomation |
RO7185876 is a selective gamma-secretase modulator being investigated for the study of Alzheimer's disease. It is a potent and selective compound that modulates gamma-secretase activity to potentially reduce amyloid-beta peptide production. The compound has not yet entered clinical trials or received regulatory approval.
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| Molecular Formula |
C25H28F3N7
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|---|---|
| Molecular Weight |
483.53
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| Exact Mass |
483.235
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| CAS # |
2226038-71-5
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| PubChem CID |
139488755
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| Appearance |
White to off-white solid powder
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| LogP |
4.8
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
35
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| Complexity |
719
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| Defined Atom Stereocenter Count |
3
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| SMILES |
CC1=CC(=NC=N1)N2C[C@H]3CC[C@@H](C2)C3NC4=NN5CCCC[C@H](C5=N4)C6=C(C(=C(C=C6)F)F)F
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| InChi Key |
XGTZKVXMDSWEOE-PLMYHDKJSA-N
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| InChi Code |
InChI=1S/C25H28F3N7/c1-14-10-20(30-13-29-14)34-11-15-5-6-16(12-34)23(15)31-25-32-24-18(4-2-3-9-35(24)33-25)17-7-8-19(26)22(28)21(17)27/h7-8,10,13,15-16,18,23H,2-6,9,11-12H2,1H3,(H,31,33)/t15-,16+,18-,23?/m0/s1
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| Chemical Name |
(9S)-N-[(1S,5R)-3-(6-methylpyrimidin-4-yl)-3-azabicyclo[3.2.1]octan-8-yl]-9-(2,3,4-trifluorophenyl)-6,7,8,9-tetrahydro-5H-[1,2,4]triazolo[1,5-a]azepin-2-amine
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0681 mL | 10.3406 mL | 20.6812 mL | |
| 5 mM | 0.4136 mL | 2.0681 mL | 4.1362 mL | |
| 10 mM | 0.2068 mL | 1.0341 mL | 2.0681 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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