| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
Autogramin-2 targets multiple cellular pathways. It inhibits autophagy induced by starvation and mTORC1 inhibition. The compound also targets Aster-A, a protein involved in cholesterol transport from the plasma membrane to the endoplasmic reticulum. Its mechanism involves inhibition of GRAMD1A, which inhibits the biogenesis of the autophagosome.
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| ln Vitro |
Autogramin-2 demonstrates potent in vitro inhibition of autophagy with IC50 values of 0.27 µM for starvation-induced autophagy and 0.14 µM for rapamycin-induced autophagy. It inhibits Aster-A with an IC50 of 1.93 µM and shows selectivity over Aster-B and Aster-C (IC50s >20 µM). These activities make it a valuable tool for studying autophagy and cholesterol transport.
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| ln Vivo |
In vivo activity of autogramin-2 has not been extensively documented. Its potent in vitro inhibition of autophagy and Aster-A suggests potential for in vivo efficacy in models of autophagy-related diseases and cholesterol metabolism disorders. Further in vivo studies are needed to evaluate its pharmacokinetic properties, efficacy, and safety profile.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for autogramin-2 involve measuring its inhibition of Aster-A activity. The compound's ability to inhibit autophagy can be assessed by measuring autophagy markers such as LC3-II and p62 levels using Western blotting. IC50 values are determined from dose-response curves generated in these assays.
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| Cell Assay |
In vitro cellular assays for autogramin-2 involve treating cells with varying concentrations of the compound and measuring autophagy inhibition. Starvation-induced and rapamycin-induced autophagy are assessed by measuring LC3-II conversion and p62 degradation using Western blotting or immunofluorescence. Aster-A inhibition can be assessed by measuring cholesterol transport from the plasma membrane to the endoplasmic reticulum.
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| Animal Protocol |
In vivo animal experiments for autogramin-2 are not extensively documented. If used in animal models, typical protocols would involve administering the compound to models of autophagy-related diseases or cholesterol metabolism disorders and evaluating efficacy by measuring disease progression and autophagy markers in tissues.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for autogramin-2 are limited. The compound has a molecular weight of 417.52. It is soluble in DMSO (up to at least 25 mg/ml) or ethanol (25 mg/ml). Purity is >98% by HPLC. The compound should be stored at room temperature. Its ADME properties have not been fully characterized.
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| Toxicity/Toxicokinetics |
Toxicological data for autogramin-2 are limited. As a research compound, comprehensive toxicological studies have not been reported. The compound is intended for research use only. Standard laboratory safety precautions should be followed when handling this compound.
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| References |
[1]. Laraia L, et al. The cholesterol transfer protein GRAMD1A regulates autophagosome biogenesis. Nat Chem Biol. 2019 Jul;15(7):710-720.
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| Additional Infomation |
Autogramin-2 (CAS#: 2375541-45-8) has the molecular formula C21H27N3O4S and a molecular weight of 417.52. Its IUPAC name is tert-butyl 2-(4-isopropoxybenzamido)-6,7-dihydrothiazolo[5,4-c]pyridine-5(4H)-carboxylate. The compound inhibits autophagy (IC50=0.27 µM for starvation; 0.14 µM for rapamycin) and Aster-A (IC50=1.93 µM). It is for research use only.
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| Molecular Formula |
C21H27N3O4S
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|---|---|
| Molecular Weight |
417.52
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| Exact Mass |
417.172
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| CAS # |
2375541-45-8
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| PubChem CID |
36765911
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.598
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| LogP |
4.33
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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 |
6
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| Heavy Atom Count |
29
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| Complexity |
587
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1C(NC(C2C=CC(=CC=2)OC(C)C)=O)=NC2=C1CN(C(=O)OC(C)(C)C)CC2
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| InChi Key |
PNSFNXURLSDVRV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H27N3O4S/c1-13(2)27-15-8-6-14(7-9-15)18(25)23-19-22-16-10-11-24(12-17(16)29-19)20(26)28-21(3,4)5/h6-9,13H,10-12H2,1-5H3,(H,22,23,25)
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| Chemical Name |
tert-butyl 2-[(4-propan-2-yloxybenzoyl)amino]-6,7-dihydro-4H-[1,3]thiazolo[5,4-c]pyridine-5-carboxylate
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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 : 83.33 mg/mL (199.58 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.98 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.98 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 20.8 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 | 2.3951 mL | 11.9755 mL | 23.9509 mL | |
| 5 mM | 0.4790 mL | 2.3951 mL | 4.7902 mL | |
| 10 mM | 0.2395 mL | 1.1975 mL | 2.3951 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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