| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg |
| ln Vitro |
A potent (Ki=51 nM) and selective TDO inhibitor, 680C91 exhibits no inhibitory activity at concentrations of 10 μM against indoleamine 2,3-dioxygenase, monoamine oxidases A and B, 5-HT uptake, and 5-HT1A,1D,2A, and 2C receptors[2].
Rat liver perfusion in situ and rat liver cells' ability to catabolize tryptophan is inhibited by 680C91[2]. Tdo2 may control cell division and promote the expression of the decidual marker Dtprp in decidual and uterine stromal cells. At 24 hours, the uterine decidual cells' ability to proliferate is likewise inhibited by the Tdo2 inhibitor 680C91[3]. The expression of collagen type I (COL1A1) and type III (COL3A1) is significantly suppressed in a dose-dependent manner when 680C91 (25 and 50 μM) is applied to spheroids of leiomyoma smooth muscle cell (LSMC) and myometrial smooth muscle cell (MSMC)[4]. |
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| ln Vivo |
In acute treatment, a dose of 15 mg/kg of 680C91 raises tryptophan levels in the brain[5].
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| Cell Assay |
Cell Line: Uterine stromal cells
Concentration: 0.01, 0.05, 0.1, 0.5, 1, 5, and 10 μM Incubation Time: 24 hours Result: The stromal cells' proliferation activity was considerably reduced at 5 and 10 μM. |
| Animal Protocol |
Animal Model: C57Bl6/NCrl male mice, 13–18 weeks of age[5]
Dosage: 15 mg/kg Administration: Administered per os Result: caused a notable rise in tryptophan in the brain. |
| References |
| Molecular Formula |
C15H11FN2
|
|---|---|
| Molecular Weight |
238.26
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| CAS # |
163239-22-3
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| SMILES |
C1=CC(=CN=C1)/C=C/C2=CNC3=C2C=CC(=C3)F
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| InChi Key |
YBSDQTBCNYWBMX-ONEGZZNKSA-N
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| InChi Code |
InChI=1S/C15H11FN2/c16-13-5-6-14-12(10-18-15(14)8-13)4-3-11-2-1-7-17-9-11/h1-10,18H/b4-3+
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| Chemical Name |
6-fluoro-3-[(E)-2-pyridin-3-ylethenyl]-1H-indole
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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 : 48~125 mg/mL ( 201.46~524.64 mM )
Ethanol : 25 mg/mL |
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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 | 4.1971 mL | 20.9855 mL | 41.9710 mL | |
| 5 mM | 0.8394 mL | 4.1971 mL | 8.3942 mL | |
| 10 mM | 0.4197 mL | 2.0985 mL | 4.1971 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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