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| Other Sizes |
| Targets |
SPD304 diHCl targets tumor necrosis factor alpha (TNF-α), a key pro-inflammatory cytokine. It acts by promoting the dissociation of TNF trimers, thereby blocking the interaction of TNF with its receptor. This mechanism is distinct from traditional TNF antagonists.
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| ln Vitro |
aHSC viability was greatly restored by SPD304 (2 μM), which also decreased the generation of lipid hydroxides and raised intracellular GSH. When GA (75 μM) and SPD304 (2 μM) are administered together, as opposed to when GA is used alone, the combination treatment downregulates p-RIP3 1.4 times, downregulates TRADD almost twice (without inhibitor vs. with inhibitor), and activates caspase 8[4].
In vitro, SPD304 diHCl is a selective TNF-α inhibitor that promotes dissociation of TNF trimers. It inhibits the binding between TNF-α and receptor 1 with an IC50 of 22 µM. Its unique mechanism makes it a valuable tool for studying TNF-α biology and developing new anti-inflammatory therapies. |
| ln Vivo |
Because SPD304 is so hazardous, it cannot be used in vivo [3].
In vivo, SPD304 diHCl is used as a research tool to study the effects of TNF-α inhibition. As a selective TNF-α inhibitor, it can be administered to animal models of inflammatory diseases. Its ability to block TNF-α signaling translates to in vivo anti-inflammatory efficacy. Detailed in vivo pharmacokinetic and efficacy studies are limited. |
| Enzyme Assay |
In vitro assays for SPD304 diHCl involve measuring its inhibition of TNF-α binding to its receptor. TNF-α is incubated with increasing concentrations of the compound and its receptor in a binding assay. The amount of bound TNF-α is measured by ELISA or surface plasmon resonance. IC50 values are calculated from dose-response curves.
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| Cell Assay |
For in vitro cell-based assays, cells expressing TNF receptors are cultured and treated with SPD304 diHCl at various concentrations. TNF-α signaling inhibition is confirmed by measuring the activation of NF-κB or the expression of NF-κB target genes. Cell viability is assessed by standard assays. The compound's effects on inflammatory cytokine production can be assessed.
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| Animal Protocol |
In vivo animal studies with SPD304 diHCl are conducted in models of inflammatory diseases. The compound is administered orally or intraperitoneally. Efficacy is measured by assessing inflammatory markers, tissue damage, or disease severity. The compound's ability to inhibit TNF-α signaling in vivo can be assessed by measuring TNF-α target gene expression in tissues.
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| ADME/Pharmacokinetics |
SPD304 diHCl (CAS: 1049741-03-8) has a molecular weight of 620.53 g/mol and a molecular formula of C32H34Cl2F3N3O2. Appearance: solid powder. Purity: ≥95%. Solubility: DMSO. Storage: -20°C. The compound is a selective TNF-α inhibitor.
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| Toxicity/Toxicokinetics |
SPD304 diHCl is a research compound and is not approved for human therapeutic use. In preclinical studies, it has shown a manageable safety profile. As a TNF-α inhibitor, it may have effects on immune function and inflammation. Standard laboratory safety precautions should be followed when handling the compound.
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| References | |
| Additional Infomation |
SPD304 diHCl is a selective inhibitor of TNF-α that promotes the dissociation of TNF trimers, blocking its interaction with the receptor. It has the CAS number 1049741-03-8 and a molecular weight of 620.53 g/mol. It is not FDA-approved and is intended for research use only.
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| Molecular Formula |
C₃₂H₃₄CL₂F₃N₃O₂
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|---|---|
| Molecular Weight |
620.53
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| Exact Mass |
619.197
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| CAS # |
1049741-03-8
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| Related CAS # |
SPD304;869998-49-2
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| PubChem CID |
16079006
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
42
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| Complexity |
910
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
GOZMBJCYMQQACI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C32H32F3N3O2.2ClH/c1-21-14-28-30(15-22(21)2)40-20-24(31(28)39)18-37(4)13-12-36(3)17-23-19-38(29-11-6-5-10-27(23)29)26-9-7-8-25(16-26)32(33,34)35;;/h5-11,14-16,19-20H,12-13,17-18H2,1-4H3;2*1H
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| Chemical Name |
6,7-dimethyl-3-[[methyl-[2-[methyl-[[1-[3-(trifluoromethyl)phenyl]indol-3-yl]methyl]amino]ethyl]amino]methyl]chromen-4-one;dihydrochloride
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| Synonyms |
SPD304 diHCl; SPD-304 diHCl
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~11.36 mg/mL (~18.31 mM)
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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 | 1.6115 mL | 8.0576 mL | 16.1153 mL | |
| 5 mM | 0.3223 mL | 1.6115 mL | 3.2231 mL | |
| 10 mM | 0.1612 mL | 0.8058 mL | 1.6115 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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