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TCS 1102 is a potent, non-selective dual orexin receptor antagonist with Ki values of 0.2 and 3 nM for OX2 and OX1 receptors respectively. In rats exposed to footshock for 14 days, TCS-1102 (10 and 20 mg/kg, i.p.) was found to reduce fear and anxiety. Moreover, anxiolytic effects specific to HR were observed with TCS-1102 (10 mg/kg, i.p.) when tested in the elevated T-maze. This work shows that rats exposed to a single footshock episode develop anxiety, which is associated with the orexin system. Moreover, it offers preclinical evidence in favor of orexin antagonist therapy for anxiety brought on by a sudden stressful event.
| Targets |
OX1 ( Ki = 3 nM ); OX2 ( Ki = 0.2 nM )
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| ln Vitro |
TCS 1102 (10 μM) suppresses the Ca2+ responses of CHO-hOX2 cells to Orexin A (human, rat, mouse) (HY-106224) and Yan 7874 (an agonist of the Orexin receptor)[2].
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| ln Vivo |
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| Enzyme Assay |
TCS 1102 is a potent, non-selective antagonist of the dual orexin receptor, with Ki values for the OX2 and OX1 receptors of 0.2 and 3 nM, respectively.
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| Animal Protocol |
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| References |
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| Molecular Formula |
C27H26N4O2S
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| Molecular Weight |
470.59
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| Exact Mass |
470.18
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| Elemental Analysis |
C, 68.91; H, 5.57; N, 11.91; O, 6.80; S, 6.81
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| CAS # |
916141-36-1
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
CN1C2=CC=CC=C2N=C1SCC(=O)N3CCC[C@H]3C(=O)NC4=CC=CC=C4C5=CC=CC=C5
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| InChi Key |
YSBGRVXJEMSEQY-DEOSSOPVSA-N
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| InChi Code |
InChI=1S/C27H26N4O2S/c1-30-23-15-8-7-14-22(23)29-27(30)34-18-25(32)31-17-9-16-24(31)26(33)28-21-13-6-5-12-20(21)19-10-3-2-4-11-19/h2-8,10-15,24H,9,16-18H2,1H3,(H,28,33)/t24-/m0/s1
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| Chemical Name |
(2S)-1-[2-(1-methylbenzimidazol-2-yl)sulfanylacetyl]-N-(2-phenylphenyl)pyrrolidine-2-carboxamide
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.31 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 (5.31 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 | 2.1250 mL | 10.6250 mL | 21.2499 mL | |
| 5 mM | 0.4250 mL | 2.1250 mL | 4.2500 mL | |
| 10 mM | 0.2125 mL | 1.0625 mL | 2.1250 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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