| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Targets |
The primary target of NSC-17102 is 11β-hydroxysteroid dehydrogenase (11βHSD) isozymes. It acts as an inhibitor of these enzymes, which catalyze the interconversion of active cortisol and inactive cortisone. By inhibiting 11βHSD, NSC-17102 modulates glucocorticoid action. The compound is also an insulin-like growth factor I (IGF-I) stimulant.
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| ln Vitro |
The LNCaP cell line was used to assess 21-deoxycortisol (21dF) and 21-deoxycortisone (21dE) in order to ascertain whether CYP17A1 lyase activity is responsible for catalyzing this conversion. Following CYP17A1 transfection, the pathway's metabolites increased to include 11-β-hydroxyandrostenedione (11OHA4), and CYP17A1 actually converted 21dF and 21dE into 11-ketoprogesterone (11KP4) and 11-β-hydroxyandrostenedione, respectively. [2].
In vitro, NSC-17102 is an inhibitor of 11β-hydroxysteroid dehydrogenase (11βHSD) isozymes. Its activity is typically measured using enzyme assays that monitor the conversion of cortisol to cortisone or vice versa. IC50 values are determined from dose-response curves. These assays confirm that NSC-17102 inhibits 11βHSD activity. |
| ln Vivo |
Eleven-beta-hydroxyandrostenedione (11beta-hydroxy-4-androstenedion-3,17-dione) in plasma concentrations in adrenaline-derived androgen excess, Cushing's syndrome, and congenital 11-hydroxylase deficiency Extremely high. As a result, when plasma 4-androstenedione is increased, identifying the adrenal or ovarian cause of hyperandrogenism can be aided by evaluating plasma 11-beta-hydroxyandrostenedione levels [1].
In vivo, NSC-17102 is a steroid mainly found in the adrenal gland. Along with increases in 4-androstenedione, measurement of plasma 11-Beta-hydroxyandrostenedione can help distinguish adrenal or ovarian origin of hyperandrogenemia. The compound's role as an 11βHSD inhibitor suggests that it may modulate glucocorticoid action in vivo. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for NSC-17102 involve 11β-hydroxysteroid dehydrogenase (11βHSD) enzyme assays using purified enzyme or tissue homogenates. The compound's inhibitory activity is measured by monitoring the conversion of cortisol to cortisone or vice versa in the presence of NADPH or NAD+. IC50 values are determined from dose-response curves. Selectivity profiling against other steroid dehydrogenases is performed to assess the compound's specificity.
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| Cell Assay |
In vitro cellular assays for NSC-17102 are conducted in cells that express 11βHSD, such as adrenal cells or other steroidogenic cells. Cells are treated with varying concentrations of NSC-17102, and 11βHSD activity is assessed by measuring the conversion of cortisol to cortisone or vice versa using LC-MS or other analytical techniques. These assays confirm that NSC-17102 engages its target in a cellular context and produces the expected inhibition of 11βHSD activity.
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| Animal Protocol |
In vivo animal studies for NSC-17102 are not extensively documented, as the compound is an endogenous steroid rather than a therapeutic agent. However, its role as an 11βHSD inhibitor and IGF-I stimulant suggests that it could be studied in animal models of metabolic and endocrine disorders.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of NSC-17102 indicate that it has a molecular weight of 302.41 and a molecular formula of C19H26O3. As an endogenous steroid, it is naturally present in the body and is metabolized through standard steroid metabolic pathways.
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| Toxicity/Toxicokinetics |
The toxicological profile of NSC-17102 is derived from its role as an endogenous steroid. As an 11βHSD inhibitor, it may affect glucocorticoid action and could have effects on metabolism, immune function, and stress response. Comprehensive toxicology studies would be required for therapeutic development.
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| References |
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| Additional Infomation |
11β-hydroxyandrostenedione-4-ene-3,17-dione is an 11β-hydroxy steroid, 3-oxo steroid, 17-oxo steroid, and androstane compound. It is a metabolite in both humans and mice. Reports indicate that 11β-hydroxyandrostenedione exists in humans, and relevant data are available.
NSC-17102 is a steroid mainly found in the adrenal gland and is an inhibitor of 11β-hydroxysteroid dehydrogenase isozymes. It is also known as 11-Beta-hydroxyandrostenedione or 4-Androsten-11β-ol-3,17-dione. The compound is an insulin-like growth factor I (IGF-I) stimulant. NSC-17102 is not approved for clinical use and is available from research chemical suppliers for research applications. |
| Molecular Formula |
C19H26O3
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| Molecular Weight |
302.414
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| Exact Mass |
302.188
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| CAS # |
382-44-5
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| Related CAS # |
11-Beta-hydroxyandrostenedione-d4;2687960-98-9
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| PubChem CID |
94141
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
475.3±45.0 °C at 760 mmHg
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| Melting Point |
197-199℃
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| Flash Point |
255.4±25.2 °C
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| Vapour Pressure |
0.0±2.7 mmHg at 25°C
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| Index of Refraction |
1.569
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| LogP |
1.27
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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 |
0
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| Heavy Atom Count |
22
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| Complexity |
577
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| Defined Atom Stereocenter Count |
6
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| SMILES |
C[C@]12CCC(=O)C=C1CC[C@@H]3[C@@H]2[C@H](C[C@]4([C@H]3CCC4=O)C)O
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| InChi Key |
WSCUHXPGYUMQEX-KCZNZURUSA-N
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| InChi Code |
InChI=1S/C19H26O3/c1-18-8-7-12(20)9-11(18)3-4-13-14-5-6-16(22)19(14,2)10-15(21)17(13)18/h9,13-15,17,21H,3-8,10H2,1-2H3/t13-,14-,15-,17+,18-,19-/m0/s1
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| Chemical Name |
(8S,9S,10R,11S,13S,14S)-11-hydroxy-10,13-dimethyl-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthrene-3,17-dione
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| Synonyms |
NSC-17102; NSC-17102; NSC-17102
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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 : ~100 mg/mL (~330.68 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3068 mL | 16.5338 mL | 33.0677 mL | |
| 5 mM | 0.6614 mL | 3.3068 mL | 6.6135 mL | |
| 10 mM | 0.3307 mL | 1.6534 mL | 3.3068 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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