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| 5mg |
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| 100mg |
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| 250mg |
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ACP-105 (ACP105; ACP 105) is a novel, nonsteroidal and orally bioactive SARM (selective androgen receptor modulator) that has been investigated for the treatment of age-related cognitive decline. It activates AR wild type and AR mutatant T877A with pEC50 of 9.0 and 9.4, respectively.
| ln Vitro |
The selective androgen receptor modulator (SARM) ACP-105 is available for oral administration. Its pEC50 values for the AR wild type and T877A mutant are 9.0 and 9.3, respectively. In human hepatocytes, ACP-105 (Compound 1) has a half-life of 5.0 hours [1].
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| ln Vivo |
In both irradiated and sham-irradiated mice, ACP-105 increased cryogenic capacity (effect of ACP-105: F=5.44; p=0.028). There was a brain region × ACP-105 interaction for MAP-2 immunoreactivity in the cortex of sham-irradiated mice (F=6.655; p=0.0027). There is a tendency toward higher MAP-2 immunoreactivity in the entorhinal cortex, despite the fact that ACP-105 reduces MAP-2 immunoreactivity in the sensorimotor cortex [2].
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| References |
[1]. Schlienger N, et al. Synthesis, structure-activity relationships, and characterization of novel nonsteroidal and selective androgen receptor modulators. J Med Chem. 2009 Nov 26;52(22):7186-91.
[2]. Dayger C, et al. Effects of the SARM ACP-105 on rotorod performance and cued fear conditioning in sham-irradiated and irradiated female mice. Brain Res. 2011 Mar 24;1381:134-40 |
| Molecular Formula |
C16H19CLN2O
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| Molecular Weight |
290.79
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| Exact Mass |
290.1186
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| CAS # |
899821-23-9
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| SMILES |
N#CC1=CC=C(N2[C@@]3([H])CC(C)(O)C[C@@]2([H])CC3)C(C)=C1Cl
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| InChi Key |
OUEODVPKPRQETQ-CHWSQXEVSA-N
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| InChi Code |
InChI=1S/C16H19ClN2O/c1-10-14(6-3-11(9-18)15(10)17)19-12-4-5-13(19)8-16(2,20)7-12/h3,6,12-13,20H,4-5,7-8H2,1-2H3/t12-,13-/m1/s1
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| Chemical Name |
2-Chloro-4-[(1R,5R)-3-hydroxy-3-methyl-8-azabicyclo[3.2.1]octan-8-yl]-3-methylbenzonitrile
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| Synonyms |
ACP 105 ACP-105ACP105
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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 : ≥ 103 mg/mL (~354.21 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 | 3.4389 mL | 17.1945 mL | 34.3891 mL | |
| 5 mM | 0.6878 mL | 3.4389 mL | 6.8778 mL | |
| 10 mM | 0.3439 mL | 1.7195 mL | 3.4389 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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