LGD-3303 |
| カタログ番号GC32403 |
LGD-3303は選択的アンドロゲン受容体モジュレーター（SARM）です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 917891-35-1
Sample solution is provided at 25 µL, 10mM.
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LGD-3303 is an orally active, non-steroidal selective androgen receptor modulator (SARM) with high affinity for the androgen receptor (Ki=0.9nM)[1, 2]. LGD-3303 binds to the mineralocorticoid receptor, glucocorticoid receptor, and progesterone receptor with much lower affinity than to the androgen receptor (Ki=1261, 581, and 136nM, respectively)[3]. LGD-3303 was designed to selectively activate the androgen receptor (AR) signaling pathway in muscle and other tissues, aiming to maintain anabolic (muscle-building) effects while minimizing androgen-related side effects on tissues such as the prostate[4].
In vivo studies in Sprague-Dawley rats showed that oral administration of LGD-3303 (3 or 30mg/kg/day) for 7 days significantly enhanced sexual preference for males in female rats, but only in sexually experienced females[5].
References:
[1] Vajda E G, López F J, Rix P, et al. Pharmacokinetics and pharmacodynamics of LGD-3303, an orally available nonsteroidalselective androgen receptor modulator[J]. Journal of Pharmacology and Experimental Therapeutics, 2009, 328(2): 663.
[2] Zhang X, Sui Z. Deciphering the selective androgen receptor modulators paradigm[J]. Expert opinion on drug discovery, 2013, 8(2): 191-218.
[3] Vajda E G, Hogue A, Griffiths K N, et al. Combination treatment with a selective androgen receptor modulator q (SARM) and a bisphosphonate has additive effects in osteopenic female rats[J]. Journal of Bone and Mineral Research, 2009, 24(2): 231-240.
[4] Clarke B L, Khosla S. Modulators of androgen and estrogen receptor activity[J]. Critical Reviews™ in Eukaryotic Gene Expression, 2010, 20(4).
[5] Kudwa A E, López F J, McGivern R F, et al. A selective androgen receptor modulator enhances male-directed sexual preference, proceptive behavior, and lordosis behavior in sexually experienced, but not sexually naive, female rats[J]. Endocrinology, 2010, 151(6): 2659-2668.
| Animal experiment [1]: | |
Animal models | Female Sprague Dawley rat |
Preparation Method | Animals were ovariectomized (OVX) and 1 week later randomly assigned to four groups. DHT was administered via a SILASTIC capsule filled with crystalline DHT, implanted subcutaneously in the mid-scapular region under isoflurane anesthesia. In all cases, hormone/drug treatment began 1 week after ovariectomy. All other groups received an empty SILASTIC capsule. LGD-3303 was administered at two doses (3 and 30mg/kg; 4mL/kg) via oral gavage. DHT-treated and sham-operated animals received only vehicle. Briefly, LGD-3303 treatment was administered once daily for 7 days, 5-6h after lights out, 20h before testing. Animals received a pre-test after one dose of LGD-3303 to familiarize them with the testing apparatus. Seven days after treatment onset (2 weeks after OVX), all subjects were tested for sexual preference. To provide sexual experience, 4 days after the second sexual preference test, these animals underwent two sexual behavior tests with a sexually active male. For the sexual behavior tests, all animals received a single injection of Estradiol benzoate (40μg/kg s.c. in oil) 48h before testing. On the day of the sexual behavior test, animals were injected with Progesterone (1mg/kg) 3-4h before testing. Sexual behavior tests were separated by 4 days. Four days after the second sexual behavior test, LGD-3303 treatment was restarted, and all subjects underwent a second series of sexual preference tests: a pre-test on day 1 and a scored sexual preference test 7 days after treatment initiation. |
Dosage form | 3, 30mg/kg/day; 7 days; p.o. |
Applications | LGD-3303 enhances sexual preference of females for males when the females have had previous sexual experience. |
References: | |
| Cas No. | 917891-35-1 | SDF | |
| Canonical SMILES | O=C1NC2=C(C3=C(N(CC(F)(F)F)C(CC)=C3C)C=C2)C(Cl)=C1 | ||
| Formula | C16H14ClF3N2O | M.Wt | 342.74 |
| 溶解度 | DMSO : 6 mg/mL (17.51 mM) | 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 | 2.9177 mL | 14.5883 mL | 29.1766 mL |
| 5 mM | 583.5 μL | 2.9177 mL | 5.8353 mL |
| 10 mM | 291.8 μL | 1.4588 mL | 2.9177 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)
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