| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
AT-130 suppresses rtL180M (IC50=9.8 μM), rtM204I (IC50=35.6 μM), and Wt (IC50=2.4 μM) HBV [1]. HepG2 cells transduced with HBV baculovirus showed dose-dependent suppression of wt HBV replication when treated with AT-130 (0.1, 1, 5, 10, 100 μM) for 7 days. When AT-130 is present, encapsidated HBV DNA is reduced by 50% (IC50) at 2.5 μM and by 90% (IC90) at 18.5 μM [1]. At concentrations as high as 250 μM, AT-130 does not cause harm to HepG2 or Huh-7 cells [1]. By directly inhibiting the HBV endogenous DNA polymerase reaction in Huh 7 or HepG2 cells, AT-130 (0.005, 0.05, 0.5, 5, 50 μM) does not inhibit HBV DNA synthesis. While AT-130 has no effect on viral DNA polymerase activity or core protein translation, it suppresses the replication of HBV DNA in liver cancer cells [3]. While it decreases encapsidated RNA, AT-130 (2.5, 18.5 μM) had little effect on total HBV RNA. The activity of protein expression vectors and the synthesis of nucleocapsids or core proteins are unaffected by AT-130 [3].
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| References |
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| Molecular Formula |
C22H22BRN3O5
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|---|---|
| Molecular Weight |
488.3312
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| Exact Mass |
487.074
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| CAS # |
211364-06-6
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| PubChem CID |
3002812
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| Appearance |
White to off-white solid powder
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| LogP |
4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
31
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| Complexity |
694
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC=CC=C1/C(=C(/C(=O)N2CCCCC2)\NC(=O)C3=CC=C(C=C3)[N+](=O)[O-])/Br
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| InChi Key |
OQIUTYABZMBBME-FMQUCBEESA-N
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| InChi Code |
InChI=1S/C22H22BrN3O5/c1-31-18-8-4-3-7-17(18)19(23)20(22(28)25-13-5-2-6-14-25)24-21(27)15-9-11-16(12-10-15)26(29)30/h3-4,7-12H,2,5-6,13-14H2,1H3,(H,24,27)/b20-19+
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| Chemical Name |
N-[(E)-1-bromo-1-(2-methoxyphenyl)-3-oxo-3-piperidin-1-ylprop-1-en-2-yl]-4-nitrobenzamide
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| Synonyms |
AT-130 AT130 AT 130
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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) |
DMSO : ~25 mg/mL (~51.19 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.12 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 | 2.0478 mL | 10.2390 mL | 20.4780 mL | |
| 5 mM | 0.4096 mL | 2.0478 mL | 4.0956 mL | |
| 10 mM | 0.2048 mL | 1.0239 mL | 2.0478 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00929539 | COMPLETED | Drug: JTT-130 Drug: JTT-130 Placebo |
Type II Diabetes Mellitus | Akros Pharma Inc. | 2009-06 | Phase 2 |
| NCT04584125 | NOT YET RECRUITING | Drug: Riboflavin 5'-phosphate in 20% dextran ophthalmic solution) 0.146% with UV light Drug: Riboflavin 5'-phosphate in 20% dextran ophthalmic solution) 0.146% without UV light |
Keratoconus | Joseph B. Ciolino, MD | 2023-12-01 | Not Applicable |
| NCT02191566 | TERMINATED | Drug: S-1 (452500ACH) Drug: OXALIPLATIN (205803BIJ) |
Stomach Cancer | Kangbuk Samsung Hospital | 2015-05 | Phase 2 |
| NCT01969955 | UNKNOWN STATUS | Drug: nanoparticle albumin-bound paclitaxel | Squamous Cell Carcinoma of Lung | Chinese Academy of Medical Sciences | 2013-09 | Phase 2 |
| NCT06509711 | RECRUITING | Other: PLYOMETRICS jump training with HIIT (4 weeks,3 sessions per week) Other: PLYOMETRICS JUMP TRAINING WITHOUT HIIT (4weeks, 3sessions Per week) |
Sports Physical Therapy | Riphah International University | 2024-06-26 | Not Applicable |
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