| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
Using CHO-K1 cells expressing GPR142 in the aequorin assay and HEK293 cells expressing GPR142 in the SPA assay, CLP-3094 inhibits the increase of intracellular Ca2+ concentration ([Ca2+]i) induced by L-tryptophan. In the aequorin assay, CLP-3094's IC50 values are 0.2 μM for the mouse receptor against 200 μM L-tryptophan and 2.3 μM for the human receptor against 1 mM L-tryptophan. Moreover, CLP-3094 prevents islets from secreting insulin in response to GPR142 and L-tryptophan agonists[2].
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|---|---|
| ln Vivo |
Compared to mice given with a vehicle, CLP-3094 (30, 100 mg/kg; intraperitoneally every day from Day 0 to Day 11) consistently showed significantly reduced arthritis scores[2].
|
| Animal Protocol |
Animal/Disease Models: CAIA mouse model (Female DBA1/J mice were iv administered with2 mg of anti-collagen antibody, followed by ip administration of 50 μg of LPS)[2]
Doses: 30, 100 mg/kg Route of Administration: Ip daily from Day 0 to Day 11 Experimental Results: Dose-dependently decreased, by not much, the arth-ritis scores. |
| References |
|
| Molecular Formula |
C15H13CLN2OS
|
|---|---|
| Molecular Weight |
304.79
|
| Exact Mass |
304.043
|
| CAS # |
312749-73-8
|
| PubChem CID |
1736098
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| Appearance |
Off-white to brown solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
509.6±56.0 °C at 760 mmHg
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| Flash Point |
262.0±31.8 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.693
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| LogP |
5.08
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
20
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| Complexity |
300
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
KZEWVENYWPSSOZ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C15H13ClN2OS/c16-11-5-7-12(8-6-11)19-9-10-20-15-17-13-3-1-2-4-14(13)18-15/h1-8H,9-10H2,(H,17,18)
|
| Chemical Name |
2-[2-(4-chlorophenoxy)ethylsulfanyl]-1H-benzimidazole
|
| 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)
|
| Solubility (In Vitro) |
DMSO: 100 mg/mL (328.09 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.20 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.20 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2809 mL | 16.4047 mL | 32.8095 mL | |
| 5 mM | 0.6562 mL | 3.2809 mL | 6.5619 mL | |
| 10 mM | 0.3281 mL | 1.6405 mL | 3.2809 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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