RAD140 (Synonyms: Testolone) |
| Catalog No.GC19305 |
RAD140 (RAD140) is a potent, orally active, nonsteroidal selective androgen receptor modulator (SARM) with a Ki of 7 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1182367-47-0
Sample solution is provided at 25 µL, 10mM.
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RAD140 is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM). IC50 value: 7 nM (Ki, fot androgen receptor) [1]Target: androgen receptor in vitro: RAD140 demonstrates excellent affinity for the androgen receptor (Ki = 7 nM) as well as good selectivity over other steroid hormone nuclear receptors, with the closest off target receptor being the progesterone receptor (IC50 = 750 nM). [1] RAD140 is a novel SARM with high affinity and specificity for AR, is orally available, and exhibits potent anabolic effects in rodents and nonhuman primates.[2]in vivo: The stability of RAD140 is high (t1/2 > 2 h) in incubations with rat, monkey, and human microsomes, and it also had good bioavailability in rats and monkeys. [1] RAD140 is also neuroprotective using the rat kainate lesion model. RAD140 is shown to exhibit peripheral tissue-specific androgen action that largely spared prostate, neural efficacy by activation of androgenic gene regulation effects, and neuroprotection of hippocampal neurons against cell death caused by systemic administration of the excitotoxin kainate.[2]
References:
[1]. Miller CP, et al. Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140. ACS Med Chem Lett. 2010 Dec 2;2(2):124-129.
[2]. Jayaraman A, et al. Selective androgen receptor modulator RAD140 is neuroprotective in cultured neurons and kainate-lesioned male rats. Endocrinology. 2014 Apr;155(4):1398-1406.
| Cas No. | 1182367-47-0 | SDF | |
| Synonyms | Testolone | ||
| Canonical SMILES | ClC1=C(C)C(N[C@]([H])([C@@]([H])(O)C)C2=NN=C(O2)C3=CC=C(C#N)C=C3)=CC=C1C#N | ||
| Formula | C20H16ClN5O2 | M.Wt | 393.83 |
| Solubility | DMSO : ≥ 100 mg/mL (253.92 mM);Water : < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5392 mL | 12.6958 mL | 25.3917 mL |
| 5 mM | 507.8 μL | 2.5392 mL | 5.0783 mL |
| 10 mM | 253.9 μL | 1.2696 mL | 2.5392 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)
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