| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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| ln Vitro |
On Drosophila with Huntington's disease, AK-1 at 10 μM had a strong neuroprotective effect, increasing the number of striated muscles from 5.2 to 5.6 [1]. With an IC50 of 12.5 μM, AK-1 is a powerful, selective, and cell-permeable inhibitor of SIRT2 [2]. By blocking the NF-κB/CSN2 pathway, AK-1 therapy causes the Snail transcription factor to be broken down by proteases. Decreased snail levels cause p21 to be overexpressed, which slows down wound healing, G1 arrest, and proliferation. In HT-29 colon cancer cells, AK-1 also regulates the Snail-p21 axis [3]. In hypoxic environments, AK-1 enhances HIF-1α's ubiquitination in a VHL-dependent manner, which triggers HIF-1α's destruction via the proteasomal route. Downregulating HIF-1α expression in AK-1-treated cells lowers its transcriptional activity, which in turn lowers the expression of BNIP3, one of the HIF-1 target genes [4].
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| References |
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| Exact Mass |
403.12
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|---|---|
| CAS # |
330461-64-8
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| PubChem CID |
1341463
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.630
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| LogP |
4.11
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
28
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| Complexity |
650
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C1=C([H])C([H])=C([H])C(C(N([H])C2C([H])=C([H])C([H])=C(C=2[H])[N+](=O)[O-])=O)=C1[H])(N1C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H])(=O)=O
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| InChi Key |
HAYBKCHPEBZNGW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H21N3O5S/c23-19(20-16-8-6-9-17(14-16)22(24)25)15-7-5-10-18(13-15)28(26,27)21-11-3-1-2-4-12-21/h5-10,13-14H,1-4,11-12H2,(H,20,23)
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| Chemical Name |
3-(azepan-1-ylsulfonyl)-N-(3-nitrophenyl)benzamide
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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 : ≥ 50 mg/mL (~123.93 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.20 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.) |
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 |
| NCT03210740 | COMPLETED | Drug: AM001 Cream, 7.5% Drug: Vehicle Cream |
Actinic Keratosis | AmDerma | 2017-06-06 | Phase 2 |
| NCT06092346 | RECRUITING | AK1, OMIM *103000, Adenylate Kinase Deficiency ADA2, OMIM *607575,Sneddon Syndrome; VAIHS ADSL, OMIM *608222, Adenylosuccinate Lyase Deficiency AICDA, OMIM *605257, Immunodeficiency With Hyper-IgM, Type 2; HIGM2 |
2023-12-19 | |||
| NCT05865730 | RECRUITING | Other: Live Bacterial Product - Akkermansia muciniphila | Carcinoma, Non-Small-Cell Lung Carcinoma, Renal Cell |
EverImmune | 2022-10-01 | Phase 2 |
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